Revista y Edición

AHEAD OF PRINT

Volumen 69 (2022): Edición 2 (August 2022)

Volumen 69 (2022): Edición s1 (July 2022)

Volumen 69 (2022): Edición 1 (January 2022)

Volumen 68 (2021): Edición 2 (December 2021)

Volumen 68 (2021): Edición 1 (January 2021)

Volumen 67 (2020): Edición 2 (May 2020)

Volumen 67 (2020): Edición 1 (January 2020)

Volumen 66 (2019): Edición 2 (November 2019)

Volumen 66 (2019): Edición 1 (June 2019)

Volumen 65 (2018): Edición 2 (November 2018)

Volumen 65 (2018): Edición 1 (June 2018)

Volumen 64 (2017): Edición 2 (November 2017)

Volumen 64 (2017): Edición 1 (September 2017)

Volumen 63 (2016): Edición s12 (December 2016)

Volumen 63 (2016): Edición 2 (December 2016)

Volumen 63 (2016): Edición 1 (September 2016)

Volumen 62 (2015): Edición s10 (September 2015)

Volumen 62 (2015): Edición s9 (June 2015)

Volumen 62 (2015): Edición 2 (December 2015)

Volumen 62 (2015): Edición 1 (June 2015)

Volumen 61 (2014): Edición 2 (December 2014)

Volumen 61 (2014): Edición 1 (August 2014)

Volumen 60 (2013): Edición Supplementum-VIII (March 2013)
Rare disease day in Slovakia, Europlan national conference

Volumen 60 (2013): Edición 2 (December 2013)

Volumen 60 (2013): Edición 1 (June 2013)

Volumen 59 (2012): Edición Supplement-VII (February 2012)
Conference abstracts, Rare disease day, conference 29.2.2012, First Slovak conference about rare diseases

Volumen 59 (2012): Edición Supplement-VI (January 2012)
Clinical Pharmacy in the Slovak Republic, dedicated to the associated professor Lívia Magulová, PhD.

Volumen 59 (2012): Edición 2 (November 2012)

Volumen 59 (2012): Edición 1 (June 2012)

Volumen 58 (2011): Edición 1 (January 2011)

Detalles de la revista
Formato
Revista
eISSN
2453-6725
Publicado por primera vez
25 Nov 2011
Periodo de publicación
2 veces al año
Idiomas
Inglés

Buscar

Volumen 68 (2021): Edición 1 (January 2021)

Detalles de la revista
Formato
Revista
eISSN
2453-6725
Publicado por primera vez
25 Nov 2011
Periodo de publicación
2 veces al año
Idiomas
Inglés

Buscar

21 Artículos

Regular Articles

access type Acceso abierto

Sedative Effect and Standardization Parameters of Herbal Medicinal Product Obtained from the Ocimum americanum L. Herb

Publicado en línea: 14 Apr 2021
Páginas: 1 - 9

Resumen

Abstract

Sedative phytomedications continue to play an important role in the management of a considerable amount of anxiety symptoms because of the various side effects of synthetic sedatives and tranquilizers. However, developing new herbal drugs needs their appropriate quality control according to the relevant requirements. The aim of the study was to determine the sedative properties of the tinctures obtained from the American basil (Ocimum americanum L., Lamiaceae Martinov family) herb and to develop the standardization parameters for the promising herbal medicinal product. The open field test was used to evaluate the sedative effect of the prepared tinctures: (1) with the added of O. americanum essential oil (OATEs) and (2) without adding O. americanum essential oil (OAT). The standardization parameters for the OATEs were developed using validated High-Performance Thin Layer Chromatography (HPTLC) and High-Performance Liquid Chromatography (HPLC) methods. The HPTLC analysis was used for the chromatographic fingerprints of polyphenols and for identifying linalool in the OATEs. The HPLC analysis found the significant content of rosmarinic acid (RA) (0.26%) in the OATEs. In conclusion, the developed OATEs can be considered as the new herbal medicinal product with significant sedative properties.

Palabras clave

  • American basil
  • herb
  • tincture
  • sedative activity
  • polyphenols
  • linalool
  • chromatographic analysis
access type Acceso abierto

Synthesis and Correlation of Aggregation and Antimicrobial Properties of Homochiral Quaternary Ammonium Bromides Derived from Camphoric Acid

Publicado en línea: 23 Apr 2021
Páginas: 10 - 16

Resumen

Abstract

A group of homochiral quaternary ammonium salts bearing hydrophobic camphoric acid-derived moiety was synthesized and characterized. The aggregation properties of the prepared compounds were evaluated by surface tension measurements, and the critical micelle concentration (CMC) was calculated. The novel quaternary ammonium bromides were tested as antimicrobial and antifungal agents, and their minimal inhibitory concentration (MIC) was evaluated and compared to clinically used benzalkonium bromide (BAB). Correlation of MIC with CMC reveals that monomers of prepared cationic surfactants, instead of micelles, are primarily responsible for antimicrobial activity.

Palabras clave

  • quaternary ammonium salts
  • antimicrobial activity
  • camphoric acid
  • critical micelle concentration
access type Acceso abierto

Study of the solubilisation process of bacterial model membranes induced by DDAO

Publicado en línea: 11 May 2021
Páginas: 17 - 23

Resumen

Abstract

Solubilisation of two bacterial model membranes induced by N,N-dimethyl-1-dodecanamine-N-oxide (DDAO) was studied. The first model membrane consisted of a mixture of palmitoyloleoylphosphatidylethanolamine (POPE) and palmitoyloleoylphosphatidylglycerol (POPG) in a molar ratio 0.6:0.4 mol/mol, and a second model membrane was enriched with tetraoleoylcardiolipin (TOCL) with a composition POPE-POPG-TOCL = 0.67:0.23:0.1 mol/mol/mol. Solubilisation of these model membranes was studied by static light scattering (nephelometry). Effective ratio Re (the amount of DDAO integrated into the bilayer to the amount of lipid) at different steps of the solubilisation process was determined. The molar partition coefficient of DDAO was calculated – in case of the POPE-POPG membrane, Kp = 5,300 ± 400, for the POPE-POPG-TOCL membrane, Kp = 6,500 ± 500.

Palabras clave

  • N,N-dimethyl-1-dodecanamine-N-oxide
  • solubilisation
  • bacterial model membranes
  • cardiolipin
access type Acceso abierto

Characterization of bioactive substances MHGF-68 on tumour cell lines with LiveFlow In Vitro Technology

Publicado en línea: 18 Jun 2021
Páginas: 24 - 29

Resumen

Abstract

As part of experimental research, growth factor-like substances associated with MHV-68, named MHGF-68, were discovered in our laboratory. MHGF-68 activity was manifested by the ability to alter cell morphology, that is, normal phenotype to transformed, resp. suppresses the transformed phenotype of tumour cells. The aim of the experiments was to monitor the effect of MHGF-68 on the change of the cell actin cytoskeleton in the tumour cell line Hepa1c1c7, as well as the normal cell line NIH3T3, and compare conventional stationary cultivation and dynamic cultivation conditions using a LiveFlow system (In Vitro Technologies). LiveFlow is an advanced system to test the impact of different compounds on the cell cultures, which allows simulation of in vivo conditions thanks to continuous flow of cultivation medium. MHGF-68 was prepared with the infection of BHK-21 cells with MHV-68 virus under non-permissive conditions (41°C). After dynamic cultivation with MHGF-68, we observed changes in morphology on Hepa1c1c7 cells. In cells cultured in a dynamic environment, we observed more pronounced changes in cell morphology in comparison with cells cultured statically. We observed no changes in the cytoskeletal structures in the NIH 3T3 cell line affected by MHGF-68 in both types of cultivation. The advantage of LiveFlow in comparison to in vivo testing is that the experiments performed in this system are less time and money consuming. Dynamic cultivation in the LiveFlow system is suitable for optimizing experiments before testing substances in vivo.

Palabras clave

  • MHV-68
  • bioactive substances MHGF-68
  • cytoskeletal structure
  • LiveFlow system
  • tumour cell line
access type Acceso abierto

Nephroprotective Effect of Coenzyme Q10 alone and in Combination with N-acetylcysteine in Diabetic Nephropathy

Publicado en línea: 18 Jun 2021
Páginas: 30 - 39

Resumen

Abstract Aim

Oxidative stress due to chronic hyperglycaemia is a key factor in the development and progression of various microvascular complications including diabetic nephropathy (DN) and associated renal injury. Treatment with antioxidants is one of the strategies to protect the kidney from oxidative tissue damage to improve renal physiology during DN. The investigation, therefore, was designed to assess the nephroprotective effect of coenzyme Q10 (CoQ10) and N-acetylcysteine (NAC), either alone or in combination in streptozotocin (STZ)-nicotinamide (NAD) induced diabetic nephropathy (DN) in rats.

Methods

T2DM induced by STZ (55 mg/kg, i.p.)-NAD (110 mg/kg, i.p.) in Sprague-Dawley rats (220–250 g) was confirmed by the elevated blood glucose level and glycated haemoglobin. DN was assessed by renal function tests. The diabetic rats were treated with CoQ10 (10 mg/kg, p.o.) and/or NAC (300 mg/kg, p.o.) for 8 weeks after confirmation of DN. Oxidative tissue damage due to STZ-NAD was estimated by malondialdehyde (MDA), superoxide dismutase (SOD) and catalase (CAT), reduced glutathione (GSH), myeloperoxidase (MPO) and nitric oxide (NO) in the renal homogenate.

Results

Data showed significant alteration in serum and urinary creatinine, total protein, albumin, serum urea, blood urea nitrogen (BUN) and uric acid in diabetic animals as compared to the control rats. CoQ10 and/or NAC effectively alleviated the disturbances in renal function. Diabetic rats showed increased MDA, decreased SOD and CAT activities and decreased GSH along with a significant increase in MPO activity and nitrite content. Treatment with the aforementioned antioxidants and their combination ameliorated the kidney damage as indicated by the reduced OS with improved renal function.

Conclusion

The investigation suggests that the chronic hyperglycaemia-induced OS leads to the development and progression of DN. The combined treatment with CoQ10 and NAC has shown a remarkable nephroprotective effect suggesting that combined antioxidant therapy with CoQ10 and NAC may be useful in the attenuation of DN.

Palabras clave

  • Diabetic nephropathy
  • oxidative stress
  • streptozotocin
  • coenzyme Q10
  • N-acetylcysteine
access type Acceso abierto

Evaluation of variability of silymarin complex in Silybi mariani fructus harvested during two production years

Publicado en línea: 09 Jul 2021
Páginas: 40 - 45

Resumen

Abstract

Milk thistle [Silybum marianum (L.) Gaertn.], a member of Asteraceae family, is one of the most cultivated medicinal plants widespread throughout the world. The pharmacological drug is a ripe fruit without pappus – Silybi mariani fructus – containing flavonolignans and generating silymarin complex. In folk medicine, it is used for the treatment of liver disorders, kidney problems, rheumatism as well as gastronomic disturbances, cardiac and neurotic disorders, and fever. The components of silymarin complex are useful in cancer prevention and treatment. The aim of the study was to determine the amount of silymarin complex contained in the fruit of the harvest of two consecutive years and how much they differ from one another. Representative samples of fruit were collected in 2015 and 2016 and distributed by a company Agrofos (Slovakia). Regarding the analytical method, we used a high-performance liquid chromatography (HPLC); the method was approved by the European Pharmacopoeia 10. The statistical significance was on the level P < 0.05. The total content of silymarin complex was 15.28 ± 0.06 g.kg−1 (in 2015) and 16.65 ± 0.09 g.kg−1 (in 2016). In both studied years, the highest representation of silybin B was observed (7.04 ± 0.07 g.kg−1 versus 5.92 ± 0.08 g.kg−1). The differences between the individual fractions of the silymarin complex were statistically significant. There was also a significant difference of 9% in the total silymarin content between 2015 and 2016. In conclusion, we can state that both samples of Silybi mariani fructus meet the requirements of the European Pharmacopoeia.

Palabras clave

  • Silybum marianum
  • silymarin complex
  • HPLC
access type Acceso abierto

Antimicrobial activity and cytotoxicity of transition metal carboxylates derived from agaric acid

Publicado en línea: 25 Jul 2021
Páginas: 46 - 53

Resumen

Abstract

Carboxylato-type transition metal complexes with agaric acid, a bioactive natural compound derived from citric acid, were prepared, and tested in vitro for their antimicrobial activity and cytotoxicity. The products as well as agaric acid itself are amphiphilic compounds containing a hydrophilic head (citric acid moiety) and a hydrophobic tail (non-polar alkyl chain). The putative composition of the carboxylates was assigned on grounds of elemental analysis, infrared (IR) and high-resolution mass spectra (HR-MS), as well as in analogy with known complexes containing the citrate moiety. The metal carboxylates showed interesting activity in several microbial strains, especially against S. aureus (vanadium complex; MIC = 0.05 mg/ml). They were also tested for their cytotoxic activity in hepatocytes, the highest activity having been found in the copper(II) and manganese(II) complexes. Further research based on these preliminary results is needed in order to evaluate the influence of parameters like stability of the metal complexes in solution on the bioactivity of the complexes.

Palabras clave

  • Bioinorganic chemistry
  • metallodrugs
  • agaric acid
  • anticancer
  • antimicrobial
  • amphiphilic compounds
access type Acceso abierto

Iridoids from Stachys byzantina K. Koch (Lamb's Ears) and Stachys germanica L. (Downy Woundwort)

Publicado en línea: 25 Jul 2021
Páginas: 54 - 58

Resumen

Abstract

Iridoids are a class of secondary metabolites found in a wide variety of plants. Iridoids are typically found in plants as glycosides, most often found to glucose. The genus Stachys L. is one of the largest genera of the Lamiaceae family, containing iridoids.

Aim

The aim of this study was the isolation and identification of iridoids from the aerial parts of Stachys byzantina K. Koch and Stachys germanica L.

Methods

For the isolation and identification of the iridoids, different chromatographic methods (NP-TLC, CPC and RP-HPLC) were used. The structures were established by one- and two-dimensional NMR and mass spectrometry, also.

Results

Iridoids (aucubin, harpagide, ajugoside and harpagoside) were isolated and identified by combination of different chromatographic methods from S. byzantina and S. germanica.

Conclusion

Stachys species may also be used as a potential source of iridoids.

Palabras clave

  • Stachys germanica
  • Stachys byzantina
  • iridoids
  • harpagide
  • aucubin
  • ajugoside
  • harpagoside
access type Acceso abierto

Thin-layer hydration method to prepare a green tea extract niosomal gel and its antioxidant performance

Publicado en línea: 13 Oct 2021
Páginas: 125 - 135

Resumen

Abstract

This study aimed to prepare a niosomal gel of green tea (Camellia sinensis) extract containing catechins, mostly epigallocatechin-3-gallate (ECGC), as a potent antioxidant. Niosomes can increase EGCG's stability and penetration into the skin for a better therapeutic effect. Niosomes were prepared by a thin-layer hydration method, were evaluated for their vesicle shape, particle size, polydispersity index, zeta potential and entrapment efficiency, and then incorporated into gels using sodium alginate as a gelling agent. Three niosomal gel formulations were prepared with different concentrations of niosomes green tea extract. Afterwards, organoleptic properties, chemical and physical characteristics, antioxidant activity, and stability and irritability of the niosomal gels were investigated. The different concentrations of green tea extract had a significant effect on the physical characteristics, but not on the chemical ones. Its antioxidant activity was determined using the 1,1-diphenyl-2-picrylhydrazyl (DPPH) scavenging method. The 50% extract green tea niosomes gel showed the highest inhibition value (25.13%). The stability was determined by freeze–thaw and real-time methods; they showed a decrease in pH, but still within the pH range of skin. The irritability test used was the Hen's Egg Test-Chorioallantoic Membrane (HET-CAM) method, which showed no irritation for all formulas. In conclusion, 50% green tea extract niosomes gel results showed it to be the best formulation with optimal antioxidant results.

Palabras clave

  • green tea extract
  • niosomes gel
  • antioxidant activity
  • stability
  • irritability
access type Acceso abierto

The Effect of Sulphoraphane on Brain Glucose Uptake during Neonatal Hypoxic-Ischemic Encephalopathy in Newborn Rats

Publicado en línea: 25 Nov 2021
Páginas: 136 - 138

Resumen

Abstract

Neonatal hypoxic-ischemic insult (HII) is one of the leading causes of morbidity and mortality in newborns. It has long-term consequences and represents a socioeconomic burden. It is an urgent issue in current neonatology. The aim of the present pilot study was to evaluate the possible effect of sulforaphane on brain glucose uptake expressed as 18F-fluorodeoxyglucose (18F-FDG) activity at the acute, subacute, and subchronic time intervals after the experimental perinatal HII in rats. Significant protection has been observed in the hippocampus 5 weeks after the insult as represented by normalisations of interhemispheric ratio of measured 18F-FDG activity. In conclusion, positron emission tomography (PET) with 18F-FDG revealed a protective effect of SFN on glucose metabolism in the subchronic phase after HII. Further research within the field of neonatal HII in newborn rats will be necessary.

Palabras clave

  • hypoxic-ischemic insult
  • 18F-FDG (fluorodeoxyglucose) activity
  • oxidative stress
  • glucose metabolism
  • sulforaphane

Special Issue: 38 Technology Days

access type Acceso abierto

Book of Abstracts 38th Technology Days 9th and 10th September 2021

Publicado en línea: 21 Sep 2021
Páginas: 98 - 124

Resumen

access type Acceso abierto

Purification of Murine Gammaherpesvirus 68 With Use of Differential Centrifugation

Publicado en línea: 30 Jul 2021
Páginas: 76 - 79

Resumen

Abstract

The method for separation of viral particles in a concentrated form from the environment is called virus purification. Viruses are required to be purified for a range of studies in which it is necessary to distinguish the properties or structure of a virus from the host cells or culture media, including analysis of viral polypeptide structures and membrane glycoprotein function. Our objective was to purify murine gammaherpesvirus 68 (MHV-68, MuHV-4) using the centrifuge, equipment and other materials available in our laboratory. After infection of baby hamster kidney 21 (BHK-21) cells with MHV-68 with the multiplicity of infection (MI) of 0.01 and following virus multiplication, we repeatedly froze and thawed the cell culture to disrupt the cells and release the virus particles into the culture medium. We used low-speed centrifugation (3000 rpm at 4°C) to separate the viral particles from cell debris. Subsequently, we transferred the supernatant containing virus particles to a fresh centrifuge tube and centrifuged at a speed of 8000 rpm (8801 g) and 11,000 rpm (=16,639 g) and at 4°C. We tested different centrifugation durations of 2, 4, 6 and 8 hours. To evaluate the quality of the obtained purified MHV-68 virus by this method and compare it to purified MHV-68 sample acquired by conventional ultracentrifugation on sucrose cushion (30%, w/v), we used the SDS-PAGE separation method using a 4%–20% (w/v) and 6%–14% (w/v) gradient gel. We obtained the best results with 6-hour-long centrifugation at 11,000 rpm. In conclusion, we managed to optimise virus purification method using the equipment available in our laboratory and prepared purified MHV-68 virus in sufficient concentration for determination of MHV-68 virus proteins.

Palabras clave

  • MHV-68
  • purification
  • virus proteins
  • SDS-PAGE
access type Acceso abierto

Formulation and Evaluation of Tablets Compressed from Granules Prepared by Thermoplastic Granulation

Publicado en línea: 30 Jul 2021
Páginas: 72 - 75

Resumen

Abstract

The aim of this formulation study was to determine the effect of the binder used in the preparation of granules by thermoplastic granulation on the release of propranolol from experimental tablets. Another aim was to select suitable excipients and their ratio in the granules to ensure a trouble-free formulation of the tablets. This study proved that the binder affects the flow properties of the granules, disintegration of the tablets and, subsequently, also the method of drug release, which can be used for the preparation of tablets with modified or prolonged drug release.

Palabras clave

  • thermoplastic granulation
  • propranolol dissolution
  • polyethylene glycol
  • cetyl stearyl alcohol
access type Acceso abierto

Drug Technology in Hunting Practice

Publicado en línea: 30 Jul 2021
Páginas: 63 - 65

Resumen

Abstract

Antiparasitic therapy in living ratites is based on the right dose and efficacy is only when the drug is pharmaceutically stable and safe. Ivermectin is considered to be the most widely used drug in the treatment of parasitosis in ruminants worlwide. For these reasons, in our study, we focused on the pharmaceutical investigation of ivermectin by SEM analysis of its powder particle shape and size, flow properties of solids (angle of repose, compressibility index, Hausner ratio) and zeta potential.

Palabras clave

  • wild ruminants
  • Galmectin premix
  • ivermectin
  • flow properties
access type Acceso abierto

EPR study of effect of ascorbic acid on hair and feather samples in relation to eumelanins and pheomelanins

Publicado en línea: 23 Aug 2021
Páginas: 89 - 91

Resumen

Palabras clave

  • hair melanin
  • feather melanin
  • eumelanin
  • pheomelanin
  • ascorbic acid
  • EPR (electron paramagnetic resonance spectroscopy)
access type Acceso abierto

Nanoscience – from manipulation of atoms to human needs

Publicado en línea: 23 Aug 2021
Páginas: 84 - 88

Resumen

Abstract

Nanoscience and nanotechnology are an extrapolation from the field of microtechnology to the atomic level. The development is based on the 60-year-old message of R. Feynman, ‘There's plenty of room at the bottom’. His vision has fertilised at the turn of the millennium with the announcement of generously funded nanotechnology initiatives. The journey was paved by seven Nobel Prizes (1986–2016) for new microscopes, low-dimensional materials (fullerenes, graphene), theories and computer methods up to the building of molecular engines. However, the enthusiasm for this technically and IT-oriented ‘business as usual’ partly dissolves in the problems of a planet burdened by climate change, depletion of raw materials, new diseases and pandemics. It is a challenge for nanoscience to adapt to these goals. Therefore, after a brief recapitulation of the history and achievements of nanotechnology, the paper will focus on its new directions. Among them, nanomedicine and pharmacy are of the topmost interest. Moreover, in the interaction of the nanoworld with humans, cross-sectional topics such as nanoethics and nanotoxicology (hampered by commercial interests) must be placed at a higher level at the same time as addressing specific applications. The world counts on nanomedicine at first in areas where overcoming of physiological barriers is not so difficult. These are dentistry and dermatology. In pharmacy, promising is the administration of drugs by methods of a ‘Trojan horse’ – their introduction directly to a therapeutic target. We also provide examples of gas nanosensors for diagnostics. These topics will be processed in such a way as to highlight the importance of nanoscience for human health.

Palabras clave

  • nanoscience
  • pioneers
  • breakthroughs
  • nanomedicine
  • pharmacy
access type Acceso abierto

Rapid and simple CZE-UV method for quality control of B1 and B6 vitamins in drugs and dietary supplements

Publicado en línea: 25 Jul 2021
Páginas: 59 - 62

Resumen

Abstract

The application of hydrodynamically closed capillary zone electrophoresis combined with convenient ultraviolet (UV) detection allows fast, simple, environmentally friendly and cost-effective analysis of ions or ionisable molecules. This technique has been used to determine two selected B vitamins (thiamine, pyridoxine) in various drug formulations. The developed method was characterised by excellent validation parameters, such as linearity, precision, accuracy, limit of detection and limit of quantification. The total time of analysis was lower than 13.5 min. The results indicate that the method is suitable for implementation in routine quality control of selected B vitamins in pharmaceutical and food samples.

Palabras clave

  • capillary zone electrophoresis
  • hydrodynamically closed system
  • ultraviolet detection
  • thiamine
  • pyridoxine
  • quality control
access type Acceso abierto

Transdermal Patches for Delivery of Beta-Blockers

Publicado en línea: 30 Jul 2021
Páginas: 80 - 83

Resumen

Abstract

Transdermal matrices containing 1.258 mg/cm2 of propranolol and consisting of ethylcellulose (EC), castor oil, and hydroxypropylmethylcellulose (HPMC) or halloysite (HA) were prepared. They were evaluated by tests such as folding endurance, moisture content and absorption, and paddle dissolution test. Of the total amount of propranolol in the samples (20 mg), 28.41% ± 3.30% was released from the EC film after 24 hours, the addition of HA 20.94% ± 1.52% (f1 = 61.82 ± 7.70, f2 = 53.61 ± 4.25) or HPMC 36.05% ± 6.18% (f1 = 34.48 ± 8.79, f2 = 65.02 ± 5.33). The dissolution profiles of HA and HPMC films were compared with each other (f1 = 51.35 ± 12.56, f2 = 59.20 ± 9.43).

Palabras clave

  • ethylcellulose
  • halloysite
  • hypromellose
  • propranolol
  • transdermal therapeutic system
access type Acceso abierto

Phospholipid bilayers in model membranes and drug delivery systems: from physics to pharmacy

Publicado en línea: 30 Jul 2021
Páginas: 66 - 71

Resumen

Abstract

Lipids spontaneously aggregate in an aqueous environment forming supramolecular structures of various architectures known as liquid crystalline mesophases. Their thermodynamic properties determined by dual polar/apolar nature coupled with the possibility to modulate the structural parameters, phase geometry and stability are challenging for applications in drug delivery systems. We review a few examples of functionality of lipid bilayers.

Palabras clave

  • lipid bilayer
  • non-lamellar phases
  • antimicrobial peptides
  • lipoplexes
  • pulmonary surfactant
access type Acceso abierto

Possibilities of microemulsion application in rectal administration of indomethacin

Publicado en línea: 02 Sep 2021
Páginas: 94 - 97

Resumen

Abstract

Rectal administration is a suitable route of administration for drugs that are either very irritating to the intestine (e.g., indomethacin) or are more effective when the first-pass effect in the liver is circumvented. Microemulsions are a tool for the improvement of penetration of sparingly soluble drugs. They are mainly used in topical and transdermal drug delivery. However, they find application also in other routes of administration, mainly due to their ability to solubilize sparingly soluble drugs. The selection of a suppository base depends on the physical properties of the drug. The study focused on evaluating the effect of the microemulsion as the solubilizer of sparingly soluble indomethacin in hydrophilic and lipophilic suppository bases compared with Polysorbate 80 as the excipient contained in the microemulsion. The reference suppositories were prepared by the traditional moulding technique from Adeps solidus or Macrogol suppository base without the previous drug solubilization. The microemulsion-based suppositories were prepared after the initial solubilization of the drug in the microemulsion or Polysorbate 80, followed by the addition of suppository base to maintain the same drug/solubilizer ratio. The suppositories were tested for softening time, hardness, and uniformity of mass. The dissolution test was performed using the dialysis tubing method in the basket apparatus. The amount of indomethacin released into the dissolution medium was determined spectrophotometrically at 320 nm. The results indicate that solubilization of indomethacin in the microemulsion had a positive effect on in vitro drug release but not as significant as in the case of Polysorbate 80 used alone. The enhancement ratio for Polysorbate 80 in Adeps suppositories was 2.9, for the microemulsion in Adeps suppositories was 1.1, and for Polysorbate 80 in Macrogol suppositories was 7.4 after 3 hours. The test of uniformity of mass had shown that all suppositories (reference, solubilizer-containing) are within the permitted limits. The softening time was reduced by adding the solubilizer to each type of suppository base.

Palabras clave

  • microemulsion
  • indomethacin
  • suppository
  • Polysorbate 80
  • macrogol
  • Adeps solidus
access type Acceso abierto

Suspension of Glycosaminoglycans in Oleogel Environment and Application Perspective in GcMAF Immunotherapy

Publicado en línea: 02 Sep 2021
Páginas: 92 - 93

Resumen

Abstract

The aim of this work was to find out the optimal concentration of gelling agents or their optimal combination in the olive oil environment to stabilise the suspension of chondroitin sulphate. Purified olive oil was structured with rice bran wax or a combination of gelators – soy lecithin and sorbitan tristearate. Rice bran wax creates a viscous fluid without a gel structure. The combination of soy lecithin and sorbitan tristearate forms a gel structure from 5 wt.% of the concentration. The optimal ratio of soy lecithin and sorbitan tristearate was found to be 3:2 wt.%. Oleogel was immobile at temperatures below 8°C; on increasing the temperature, it changed to a viscous liquid. The oleogel environment opens new possibilities for creating oral route immunotherapy approaches such as glycoprotein-derived macrophage activating factor-derived immunotherapy.

Palabras clave

  • oleogel
  • edible oleogelators
  • lecithin
  • chondroitin sulphate suspension
21 Artículos

Regular Articles

access type Acceso abierto

Sedative Effect and Standardization Parameters of Herbal Medicinal Product Obtained from the Ocimum americanum L. Herb

Publicado en línea: 14 Apr 2021
Páginas: 1 - 9

Resumen

Abstract

Sedative phytomedications continue to play an important role in the management of a considerable amount of anxiety symptoms because of the various side effects of synthetic sedatives and tranquilizers. However, developing new herbal drugs needs their appropriate quality control according to the relevant requirements. The aim of the study was to determine the sedative properties of the tinctures obtained from the American basil (Ocimum americanum L., Lamiaceae Martinov family) herb and to develop the standardization parameters for the promising herbal medicinal product. The open field test was used to evaluate the sedative effect of the prepared tinctures: (1) with the added of O. americanum essential oil (OATEs) and (2) without adding O. americanum essential oil (OAT). The standardization parameters for the OATEs were developed using validated High-Performance Thin Layer Chromatography (HPTLC) and High-Performance Liquid Chromatography (HPLC) methods. The HPTLC analysis was used for the chromatographic fingerprints of polyphenols and for identifying linalool in the OATEs. The HPLC analysis found the significant content of rosmarinic acid (RA) (0.26%) in the OATEs. In conclusion, the developed OATEs can be considered as the new herbal medicinal product with significant sedative properties.

Palabras clave

  • American basil
  • herb
  • tincture
  • sedative activity
  • polyphenols
  • linalool
  • chromatographic analysis
access type Acceso abierto

Synthesis and Correlation of Aggregation and Antimicrobial Properties of Homochiral Quaternary Ammonium Bromides Derived from Camphoric Acid

Publicado en línea: 23 Apr 2021
Páginas: 10 - 16

Resumen

Abstract

A group of homochiral quaternary ammonium salts bearing hydrophobic camphoric acid-derived moiety was synthesized and characterized. The aggregation properties of the prepared compounds were evaluated by surface tension measurements, and the critical micelle concentration (CMC) was calculated. The novel quaternary ammonium bromides were tested as antimicrobial and antifungal agents, and their minimal inhibitory concentration (MIC) was evaluated and compared to clinically used benzalkonium bromide (BAB). Correlation of MIC with CMC reveals that monomers of prepared cationic surfactants, instead of micelles, are primarily responsible for antimicrobial activity.

Palabras clave

  • quaternary ammonium salts
  • antimicrobial activity
  • camphoric acid
  • critical micelle concentration
access type Acceso abierto

Study of the solubilisation process of bacterial model membranes induced by DDAO

Publicado en línea: 11 May 2021
Páginas: 17 - 23

Resumen

Abstract

Solubilisation of two bacterial model membranes induced by N,N-dimethyl-1-dodecanamine-N-oxide (DDAO) was studied. The first model membrane consisted of a mixture of palmitoyloleoylphosphatidylethanolamine (POPE) and palmitoyloleoylphosphatidylglycerol (POPG) in a molar ratio 0.6:0.4 mol/mol, and a second model membrane was enriched with tetraoleoylcardiolipin (TOCL) with a composition POPE-POPG-TOCL = 0.67:0.23:0.1 mol/mol/mol. Solubilisation of these model membranes was studied by static light scattering (nephelometry). Effective ratio Re (the amount of DDAO integrated into the bilayer to the amount of lipid) at different steps of the solubilisation process was determined. The molar partition coefficient of DDAO was calculated – in case of the POPE-POPG membrane, Kp = 5,300 ± 400, for the POPE-POPG-TOCL membrane, Kp = 6,500 ± 500.

Palabras clave

  • N,N-dimethyl-1-dodecanamine-N-oxide
  • solubilisation
  • bacterial model membranes
  • cardiolipin
access type Acceso abierto

Characterization of bioactive substances MHGF-68 on tumour cell lines with LiveFlow In Vitro Technology

Publicado en línea: 18 Jun 2021
Páginas: 24 - 29

Resumen

Abstract

As part of experimental research, growth factor-like substances associated with MHV-68, named MHGF-68, were discovered in our laboratory. MHGF-68 activity was manifested by the ability to alter cell morphology, that is, normal phenotype to transformed, resp. suppresses the transformed phenotype of tumour cells. The aim of the experiments was to monitor the effect of MHGF-68 on the change of the cell actin cytoskeleton in the tumour cell line Hepa1c1c7, as well as the normal cell line NIH3T3, and compare conventional stationary cultivation and dynamic cultivation conditions using a LiveFlow system (In Vitro Technologies). LiveFlow is an advanced system to test the impact of different compounds on the cell cultures, which allows simulation of in vivo conditions thanks to continuous flow of cultivation medium. MHGF-68 was prepared with the infection of BHK-21 cells with MHV-68 virus under non-permissive conditions (41°C). After dynamic cultivation with MHGF-68, we observed changes in morphology on Hepa1c1c7 cells. In cells cultured in a dynamic environment, we observed more pronounced changes in cell morphology in comparison with cells cultured statically. We observed no changes in the cytoskeletal structures in the NIH 3T3 cell line affected by MHGF-68 in both types of cultivation. The advantage of LiveFlow in comparison to in vivo testing is that the experiments performed in this system are less time and money consuming. Dynamic cultivation in the LiveFlow system is suitable for optimizing experiments before testing substances in vivo.

Palabras clave

  • MHV-68
  • bioactive substances MHGF-68
  • cytoskeletal structure
  • LiveFlow system
  • tumour cell line
access type Acceso abierto

Nephroprotective Effect of Coenzyme Q10 alone and in Combination with N-acetylcysteine in Diabetic Nephropathy

Publicado en línea: 18 Jun 2021
Páginas: 30 - 39

Resumen

Abstract Aim

Oxidative stress due to chronic hyperglycaemia is a key factor in the development and progression of various microvascular complications including diabetic nephropathy (DN) and associated renal injury. Treatment with antioxidants is one of the strategies to protect the kidney from oxidative tissue damage to improve renal physiology during DN. The investigation, therefore, was designed to assess the nephroprotective effect of coenzyme Q10 (CoQ10) and N-acetylcysteine (NAC), either alone or in combination in streptozotocin (STZ)-nicotinamide (NAD) induced diabetic nephropathy (DN) in rats.

Methods

T2DM induced by STZ (55 mg/kg, i.p.)-NAD (110 mg/kg, i.p.) in Sprague-Dawley rats (220–250 g) was confirmed by the elevated blood glucose level and glycated haemoglobin. DN was assessed by renal function tests. The diabetic rats were treated with CoQ10 (10 mg/kg, p.o.) and/or NAC (300 mg/kg, p.o.) for 8 weeks after confirmation of DN. Oxidative tissue damage due to STZ-NAD was estimated by malondialdehyde (MDA), superoxide dismutase (SOD) and catalase (CAT), reduced glutathione (GSH), myeloperoxidase (MPO) and nitric oxide (NO) in the renal homogenate.

Results

Data showed significant alteration in serum and urinary creatinine, total protein, albumin, serum urea, blood urea nitrogen (BUN) and uric acid in diabetic animals as compared to the control rats. CoQ10 and/or NAC effectively alleviated the disturbances in renal function. Diabetic rats showed increased MDA, decreased SOD and CAT activities and decreased GSH along with a significant increase in MPO activity and nitrite content. Treatment with the aforementioned antioxidants and their combination ameliorated the kidney damage as indicated by the reduced OS with improved renal function.

Conclusion

The investigation suggests that the chronic hyperglycaemia-induced OS leads to the development and progression of DN. The combined treatment with CoQ10 and NAC has shown a remarkable nephroprotective effect suggesting that combined antioxidant therapy with CoQ10 and NAC may be useful in the attenuation of DN.

Palabras clave

  • Diabetic nephropathy
  • oxidative stress
  • streptozotocin
  • coenzyme Q10
  • N-acetylcysteine
access type Acceso abierto

Evaluation of variability of silymarin complex in Silybi mariani fructus harvested during two production years

Publicado en línea: 09 Jul 2021
Páginas: 40 - 45

Resumen

Abstract

Milk thistle [Silybum marianum (L.) Gaertn.], a member of Asteraceae family, is one of the most cultivated medicinal plants widespread throughout the world. The pharmacological drug is a ripe fruit without pappus – Silybi mariani fructus – containing flavonolignans and generating silymarin complex. In folk medicine, it is used for the treatment of liver disorders, kidney problems, rheumatism as well as gastronomic disturbances, cardiac and neurotic disorders, and fever. The components of silymarin complex are useful in cancer prevention and treatment. The aim of the study was to determine the amount of silymarin complex contained in the fruit of the harvest of two consecutive years and how much they differ from one another. Representative samples of fruit were collected in 2015 and 2016 and distributed by a company Agrofos (Slovakia). Regarding the analytical method, we used a high-performance liquid chromatography (HPLC); the method was approved by the European Pharmacopoeia 10. The statistical significance was on the level P < 0.05. The total content of silymarin complex was 15.28 ± 0.06 g.kg−1 (in 2015) and 16.65 ± 0.09 g.kg−1 (in 2016). In both studied years, the highest representation of silybin B was observed (7.04 ± 0.07 g.kg−1 versus 5.92 ± 0.08 g.kg−1). The differences between the individual fractions of the silymarin complex were statistically significant. There was also a significant difference of 9% in the total silymarin content between 2015 and 2016. In conclusion, we can state that both samples of Silybi mariani fructus meet the requirements of the European Pharmacopoeia.

Palabras clave

  • Silybum marianum
  • silymarin complex
  • HPLC
access type Acceso abierto

Antimicrobial activity and cytotoxicity of transition metal carboxylates derived from agaric acid

Publicado en línea: 25 Jul 2021
Páginas: 46 - 53

Resumen

Abstract

Carboxylato-type transition metal complexes with agaric acid, a bioactive natural compound derived from citric acid, were prepared, and tested in vitro for their antimicrobial activity and cytotoxicity. The products as well as agaric acid itself are amphiphilic compounds containing a hydrophilic head (citric acid moiety) and a hydrophobic tail (non-polar alkyl chain). The putative composition of the carboxylates was assigned on grounds of elemental analysis, infrared (IR) and high-resolution mass spectra (HR-MS), as well as in analogy with known complexes containing the citrate moiety. The metal carboxylates showed interesting activity in several microbial strains, especially against S. aureus (vanadium complex; MIC = 0.05 mg/ml). They were also tested for their cytotoxic activity in hepatocytes, the highest activity having been found in the copper(II) and manganese(II) complexes. Further research based on these preliminary results is needed in order to evaluate the influence of parameters like stability of the metal complexes in solution on the bioactivity of the complexes.

Palabras clave

  • Bioinorganic chemistry
  • metallodrugs
  • agaric acid
  • anticancer
  • antimicrobial
  • amphiphilic compounds
access type Acceso abierto

Iridoids from Stachys byzantina K. Koch (Lamb's Ears) and Stachys germanica L. (Downy Woundwort)

Publicado en línea: 25 Jul 2021
Páginas: 54 - 58

Resumen

Abstract

Iridoids are a class of secondary metabolites found in a wide variety of plants. Iridoids are typically found in plants as glycosides, most often found to glucose. The genus Stachys L. is one of the largest genera of the Lamiaceae family, containing iridoids.

Aim

The aim of this study was the isolation and identification of iridoids from the aerial parts of Stachys byzantina K. Koch and Stachys germanica L.

Methods

For the isolation and identification of the iridoids, different chromatographic methods (NP-TLC, CPC and RP-HPLC) were used. The structures were established by one- and two-dimensional NMR and mass spectrometry, also.

Results

Iridoids (aucubin, harpagide, ajugoside and harpagoside) were isolated and identified by combination of different chromatographic methods from S. byzantina and S. germanica.

Conclusion

Stachys species may also be used as a potential source of iridoids.

Palabras clave

  • Stachys germanica
  • Stachys byzantina
  • iridoids
  • harpagide
  • aucubin
  • ajugoside
  • harpagoside
access type Acceso abierto

Thin-layer hydration method to prepare a green tea extract niosomal gel and its antioxidant performance

Publicado en línea: 13 Oct 2021
Páginas: 125 - 135

Resumen

Abstract

This study aimed to prepare a niosomal gel of green tea (Camellia sinensis) extract containing catechins, mostly epigallocatechin-3-gallate (ECGC), as a potent antioxidant. Niosomes can increase EGCG's stability and penetration into the skin for a better therapeutic effect. Niosomes were prepared by a thin-layer hydration method, were evaluated for their vesicle shape, particle size, polydispersity index, zeta potential and entrapment efficiency, and then incorporated into gels using sodium alginate as a gelling agent. Three niosomal gel formulations were prepared with different concentrations of niosomes green tea extract. Afterwards, organoleptic properties, chemical and physical characteristics, antioxidant activity, and stability and irritability of the niosomal gels were investigated. The different concentrations of green tea extract had a significant effect on the physical characteristics, but not on the chemical ones. Its antioxidant activity was determined using the 1,1-diphenyl-2-picrylhydrazyl (DPPH) scavenging method. The 50% extract green tea niosomes gel showed the highest inhibition value (25.13%). The stability was determined by freeze–thaw and real-time methods; they showed a decrease in pH, but still within the pH range of skin. The irritability test used was the Hen's Egg Test-Chorioallantoic Membrane (HET-CAM) method, which showed no irritation for all formulas. In conclusion, 50% green tea extract niosomes gel results showed it to be the best formulation with optimal antioxidant results.

Palabras clave

  • green tea extract
  • niosomes gel
  • antioxidant activity
  • stability
  • irritability
access type Acceso abierto

The Effect of Sulphoraphane on Brain Glucose Uptake during Neonatal Hypoxic-Ischemic Encephalopathy in Newborn Rats

Publicado en línea: 25 Nov 2021
Páginas: 136 - 138

Resumen

Abstract

Neonatal hypoxic-ischemic insult (HII) is one of the leading causes of morbidity and mortality in newborns. It has long-term consequences and represents a socioeconomic burden. It is an urgent issue in current neonatology. The aim of the present pilot study was to evaluate the possible effect of sulforaphane on brain glucose uptake expressed as 18F-fluorodeoxyglucose (18F-FDG) activity at the acute, subacute, and subchronic time intervals after the experimental perinatal HII in rats. Significant protection has been observed in the hippocampus 5 weeks after the insult as represented by normalisations of interhemispheric ratio of measured 18F-FDG activity. In conclusion, positron emission tomography (PET) with 18F-FDG revealed a protective effect of SFN on glucose metabolism in the subchronic phase after HII. Further research within the field of neonatal HII in newborn rats will be necessary.

Palabras clave

  • hypoxic-ischemic insult
  • 18F-FDG (fluorodeoxyglucose) activity
  • oxidative stress
  • glucose metabolism
  • sulforaphane

Special Issue: 38 Technology Days

access type Acceso abierto

Book of Abstracts 38th Technology Days 9th and 10th September 2021

Publicado en línea: 21 Sep 2021
Páginas: 98 - 124

Resumen

access type Acceso abierto

Purification of Murine Gammaherpesvirus 68 With Use of Differential Centrifugation

Publicado en línea: 30 Jul 2021
Páginas: 76 - 79

Resumen

Abstract

The method for separation of viral particles in a concentrated form from the environment is called virus purification. Viruses are required to be purified for a range of studies in which it is necessary to distinguish the properties or structure of a virus from the host cells or culture media, including analysis of viral polypeptide structures and membrane glycoprotein function. Our objective was to purify murine gammaherpesvirus 68 (MHV-68, MuHV-4) using the centrifuge, equipment and other materials available in our laboratory. After infection of baby hamster kidney 21 (BHK-21) cells with MHV-68 with the multiplicity of infection (MI) of 0.01 and following virus multiplication, we repeatedly froze and thawed the cell culture to disrupt the cells and release the virus particles into the culture medium. We used low-speed centrifugation (3000 rpm at 4°C) to separate the viral particles from cell debris. Subsequently, we transferred the supernatant containing virus particles to a fresh centrifuge tube and centrifuged at a speed of 8000 rpm (8801 g) and 11,000 rpm (=16,639 g) and at 4°C. We tested different centrifugation durations of 2, 4, 6 and 8 hours. To evaluate the quality of the obtained purified MHV-68 virus by this method and compare it to purified MHV-68 sample acquired by conventional ultracentrifugation on sucrose cushion (30%, w/v), we used the SDS-PAGE separation method using a 4%–20% (w/v) and 6%–14% (w/v) gradient gel. We obtained the best results with 6-hour-long centrifugation at 11,000 rpm. In conclusion, we managed to optimise virus purification method using the equipment available in our laboratory and prepared purified MHV-68 virus in sufficient concentration for determination of MHV-68 virus proteins.

Palabras clave

  • MHV-68
  • purification
  • virus proteins
  • SDS-PAGE
access type Acceso abierto

Formulation and Evaluation of Tablets Compressed from Granules Prepared by Thermoplastic Granulation

Publicado en línea: 30 Jul 2021
Páginas: 72 - 75

Resumen

Abstract

The aim of this formulation study was to determine the effect of the binder used in the preparation of granules by thermoplastic granulation on the release of propranolol from experimental tablets. Another aim was to select suitable excipients and their ratio in the granules to ensure a trouble-free formulation of the tablets. This study proved that the binder affects the flow properties of the granules, disintegration of the tablets and, subsequently, also the method of drug release, which can be used for the preparation of tablets with modified or prolonged drug release.

Palabras clave

  • thermoplastic granulation
  • propranolol dissolution
  • polyethylene glycol
  • cetyl stearyl alcohol
access type Acceso abierto

Drug Technology in Hunting Practice

Publicado en línea: 30 Jul 2021
Páginas: 63 - 65

Resumen

Abstract

Antiparasitic therapy in living ratites is based on the right dose and efficacy is only when the drug is pharmaceutically stable and safe. Ivermectin is considered to be the most widely used drug in the treatment of parasitosis in ruminants worlwide. For these reasons, in our study, we focused on the pharmaceutical investigation of ivermectin by SEM analysis of its powder particle shape and size, flow properties of solids (angle of repose, compressibility index, Hausner ratio) and zeta potential.

Palabras clave

  • wild ruminants
  • Galmectin premix
  • ivermectin
  • flow properties
access type Acceso abierto

EPR study of effect of ascorbic acid on hair and feather samples in relation to eumelanins and pheomelanins

Publicado en línea: 23 Aug 2021
Páginas: 89 - 91

Resumen

Palabras clave

  • hair melanin
  • feather melanin
  • eumelanin
  • pheomelanin
  • ascorbic acid
  • EPR (electron paramagnetic resonance spectroscopy)
access type Acceso abierto

Nanoscience – from manipulation of atoms to human needs

Publicado en línea: 23 Aug 2021
Páginas: 84 - 88

Resumen

Abstract

Nanoscience and nanotechnology are an extrapolation from the field of microtechnology to the atomic level. The development is based on the 60-year-old message of R. Feynman, ‘There's plenty of room at the bottom’. His vision has fertilised at the turn of the millennium with the announcement of generously funded nanotechnology initiatives. The journey was paved by seven Nobel Prizes (1986–2016) for new microscopes, low-dimensional materials (fullerenes, graphene), theories and computer methods up to the building of molecular engines. However, the enthusiasm for this technically and IT-oriented ‘business as usual’ partly dissolves in the problems of a planet burdened by climate change, depletion of raw materials, new diseases and pandemics. It is a challenge for nanoscience to adapt to these goals. Therefore, after a brief recapitulation of the history and achievements of nanotechnology, the paper will focus on its new directions. Among them, nanomedicine and pharmacy are of the topmost interest. Moreover, in the interaction of the nanoworld with humans, cross-sectional topics such as nanoethics and nanotoxicology (hampered by commercial interests) must be placed at a higher level at the same time as addressing specific applications. The world counts on nanomedicine at first in areas where overcoming of physiological barriers is not so difficult. These are dentistry and dermatology. In pharmacy, promising is the administration of drugs by methods of a ‘Trojan horse’ – their introduction directly to a therapeutic target. We also provide examples of gas nanosensors for diagnostics. These topics will be processed in such a way as to highlight the importance of nanoscience for human health.

Palabras clave

  • nanoscience
  • pioneers
  • breakthroughs
  • nanomedicine
  • pharmacy
access type Acceso abierto

Rapid and simple CZE-UV method for quality control of B1 and B6 vitamins in drugs and dietary supplements

Publicado en línea: 25 Jul 2021
Páginas: 59 - 62

Resumen

Abstract

The application of hydrodynamically closed capillary zone electrophoresis combined with convenient ultraviolet (UV) detection allows fast, simple, environmentally friendly and cost-effective analysis of ions or ionisable molecules. This technique has been used to determine two selected B vitamins (thiamine, pyridoxine) in various drug formulations. The developed method was characterised by excellent validation parameters, such as linearity, precision, accuracy, limit of detection and limit of quantification. The total time of analysis was lower than 13.5 min. The results indicate that the method is suitable for implementation in routine quality control of selected B vitamins in pharmaceutical and food samples.

Palabras clave

  • capillary zone electrophoresis
  • hydrodynamically closed system
  • ultraviolet detection
  • thiamine
  • pyridoxine
  • quality control
access type Acceso abierto

Transdermal Patches for Delivery of Beta-Blockers

Publicado en línea: 30 Jul 2021
Páginas: 80 - 83

Resumen

Abstract

Transdermal matrices containing 1.258 mg/cm2 of propranolol and consisting of ethylcellulose (EC), castor oil, and hydroxypropylmethylcellulose (HPMC) or halloysite (HA) were prepared. They were evaluated by tests such as folding endurance, moisture content and absorption, and paddle dissolution test. Of the total amount of propranolol in the samples (20 mg), 28.41% ± 3.30% was released from the EC film after 24 hours, the addition of HA 20.94% ± 1.52% (f1 = 61.82 ± 7.70, f2 = 53.61 ± 4.25) or HPMC 36.05% ± 6.18% (f1 = 34.48 ± 8.79, f2 = 65.02 ± 5.33). The dissolution profiles of HA and HPMC films were compared with each other (f1 = 51.35 ± 12.56, f2 = 59.20 ± 9.43).

Palabras clave

  • ethylcellulose
  • halloysite
  • hypromellose
  • propranolol
  • transdermal therapeutic system
access type Acceso abierto

Phospholipid bilayers in model membranes and drug delivery systems: from physics to pharmacy

Publicado en línea: 30 Jul 2021
Páginas: 66 - 71

Resumen

Abstract

Lipids spontaneously aggregate in an aqueous environment forming supramolecular structures of various architectures known as liquid crystalline mesophases. Their thermodynamic properties determined by dual polar/apolar nature coupled with the possibility to modulate the structural parameters, phase geometry and stability are challenging for applications in drug delivery systems. We review a few examples of functionality of lipid bilayers.

Palabras clave

  • lipid bilayer
  • non-lamellar phases
  • antimicrobial peptides
  • lipoplexes
  • pulmonary surfactant
access type Acceso abierto

Possibilities of microemulsion application in rectal administration of indomethacin

Publicado en línea: 02 Sep 2021
Páginas: 94 - 97

Resumen

Abstract

Rectal administration is a suitable route of administration for drugs that are either very irritating to the intestine (e.g., indomethacin) or are more effective when the first-pass effect in the liver is circumvented. Microemulsions are a tool for the improvement of penetration of sparingly soluble drugs. They are mainly used in topical and transdermal drug delivery. However, they find application also in other routes of administration, mainly due to their ability to solubilize sparingly soluble drugs. The selection of a suppository base depends on the physical properties of the drug. The study focused on evaluating the effect of the microemulsion as the solubilizer of sparingly soluble indomethacin in hydrophilic and lipophilic suppository bases compared with Polysorbate 80 as the excipient contained in the microemulsion. The reference suppositories were prepared by the traditional moulding technique from Adeps solidus or Macrogol suppository base without the previous drug solubilization. The microemulsion-based suppositories were prepared after the initial solubilization of the drug in the microemulsion or Polysorbate 80, followed by the addition of suppository base to maintain the same drug/solubilizer ratio. The suppositories were tested for softening time, hardness, and uniformity of mass. The dissolution test was performed using the dialysis tubing method in the basket apparatus. The amount of indomethacin released into the dissolution medium was determined spectrophotometrically at 320 nm. The results indicate that solubilization of indomethacin in the microemulsion had a positive effect on in vitro drug release but not as significant as in the case of Polysorbate 80 used alone. The enhancement ratio for Polysorbate 80 in Adeps suppositories was 2.9, for the microemulsion in Adeps suppositories was 1.1, and for Polysorbate 80 in Macrogol suppositories was 7.4 after 3 hours. The test of uniformity of mass had shown that all suppositories (reference, solubilizer-containing) are within the permitted limits. The softening time was reduced by adding the solubilizer to each type of suppository base.

Palabras clave

  • microemulsion
  • indomethacin
  • suppository
  • Polysorbate 80
  • macrogol
  • Adeps solidus
access type Acceso abierto

Suspension of Glycosaminoglycans in Oleogel Environment and Application Perspective in GcMAF Immunotherapy

Publicado en línea: 02 Sep 2021
Páginas: 92 - 93

Resumen

Abstract

The aim of this work was to find out the optimal concentration of gelling agents or their optimal combination in the olive oil environment to stabilise the suspension of chondroitin sulphate. Purified olive oil was structured with rice bran wax or a combination of gelators – soy lecithin and sorbitan tristearate. Rice bran wax creates a viscous fluid without a gel structure. The combination of soy lecithin and sorbitan tristearate forms a gel structure from 5 wt.% of the concentration. The optimal ratio of soy lecithin and sorbitan tristearate was found to be 3:2 wt.%. Oleogel was immobile at temperatures below 8°C; on increasing the temperature, it changed to a viscous liquid. The oleogel environment opens new possibilities for creating oral route immunotherapy approaches such as glycoprotein-derived macrophage activating factor-derived immunotherapy.

Palabras clave

  • oleogel
  • edible oleogelators
  • lecithin
  • chondroitin sulphate suspension

Planifique su conferencia remota con Sciendo