rss_2.0European Pharmaceutical Journal FeedSciendo RSS Feed for European Pharmaceutical Journal Pharmaceutical Journal 's Cover Effect of Coenzyme Q10 alone and in Combination with N-acetylcysteine in Diabetic Nephropathy<abstract> <title style='display:none'>Abstract</title> <sec><title style='display:none'>Aim</title> <p>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.</p> </sec> <sec><title style='display:none'>Methods</title> <p>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.</p> </sec> <sec><title style='display:none'>Results</title> <p>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.</p> </sec> <sec><title style='display:none'>Conclusion</title> <p>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.</p> </sec> </abstract>ARTICLE2021-06-18T00:00:00.000+00:00Study of the solubilisation process of bacterial model membranes induced by DDAO<abstract> <title style='display:none'>Abstract</title> <p>Solubilisation of two bacterial model membranes induced by <italic>N,N-</italic>dimethyl-1-dodecanamine-<italic>N-</italic>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 R<sub>e</sub> (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, K<sub>p</sub> = 5,300 ± 400, for the POPE-POPG-TOCL membrane, K<sub>p</sub> = 6,500 ± 500.</p> </abstract>ARTICLE2021-05-11T00:00:00.000+00:00Possibilities of microemulsion application in rectal administration of indomethacin<abstract> <title style='display:none'>Abstract</title> <p>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 <italic>Adeps solidus</italic> 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 <italic>in vitro</italic> 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.</p> </abstract>ARTICLE2021-09-02T00:00:00.000+00:00Phospholipid bilayers in model membranes and drug delivery systems: from physics to pharmacy<abstract> <title style='display:none'>Abstract</title> <p>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.</p> </abstract>ARTICLE2021-07-30T00:00:00.000+00:00Transdermal Patches for Delivery of Beta-Blockers<abstract> <title style='display:none'>Abstract</title> <p>Transdermal matrices containing 1.258 mg/cm<sup>2</sup> 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% (f<sub>1</sub> = 61.82 ± 7.70, f<sub>2</sub> = 53.61 ± 4.25) or HPMC 36.05% ± 6.18% (f<sub>1</sub> = 34.48 ± 8.79, f<sub>2</sub> = 65.02 ± 5.33). The dissolution profiles of HA and HPMC films were compared with each other (f<sub>1</sub> = 51.35 ± 12.56, f<sub>2</sub> = 59.20 ± 9.43).</p> </abstract>ARTICLE2021-07-30T00:00:00.000+00:00Synthesis and Correlation of Aggregation and Antimicrobial Properties of Homochiral Quaternary Ammonium Bromides Derived from Camphoric Acid<abstract> <title style='display:none'>Abstract</title> <p>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.</p> </abstract>ARTICLE2021-04-23T00:00:00.000+00:00EPR study of effect of ascorbic acid on hair and feather samples in relation to eumelanins and pheomelanins from K. Koch (Lamb's Ears) and L. (Downy Woundwort)<abstract> <title style='display:none'>Abstract</title> <p>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 <italic>Stachys</italic> L. is one of the largest genera of the Lamiaceae family, containing iridoids.</p> <sec><title style='display:none'>Aim</title> <p>The aim of this study was the isolation and identification of iridoids from the aerial parts of <italic>Stachys byzantina</italic> K. Koch and <italic>Stachys germanica</italic> L.</p> </sec> <sec><title style='display:none'>Methods</title> <p>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.</p> </sec> <sec><title style='display:none'>Results</title> <p>Iridoids (aucubin, harpagide, ajugoside and harpagoside) were isolated and identified by combination of different chromatographic methods from <italic>S. byzantina</italic> and <italic>S. germanica</italic>.</p> </sec> <sec><title style='display:none'>Conclusion</title> <p><italic>Stachys</italic> species may also be used as a potential source of iridoids.</p> </sec> </abstract>ARTICLE2021-07-25T00:00:00.000+00:00Formulation and Evaluation of Tablets Compressed from Granules Prepared by Thermoplastic Granulation<abstract> <title style='display:none'>Abstract</title> <p>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.</p> </abstract>ARTICLE2021-07-30T00:00:00.000+00:00Drug Technology in Hunting Practice<abstract> <title style='display:none'>Abstract</title> <p>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.</p> </abstract>ARTICLE2021-07-30T00:00:00.000+00:00Sedative Effect and Standardization Parameters of Herbal Medicinal Product Obtained from the L. Herb<abstract> <title style='display:none'>Abstract</title> <p>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 (<italic>Ocimum americanum</italic> L., <italic>Lamiaceae</italic> 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 <italic>O. americanum</italic> essential oil (OATEs) and (2) without adding <italic>O. americanum</italic> 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.</p> </abstract>ARTICLE2021-04-14T00:00:00.000+00:00Purification of Murine Gammaherpesvirus 68 With Use of Differential Centrifugation<abstract> <title style='display:none'>Abstract</title> <p>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 <italic>g</italic>) and 11,000 rpm (=16,639 <italic>g</italic>) 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.</p> </abstract>ARTICLE2021-07-30T00:00:00.000+00:00Book of Abstracts 38th Technology Days 9th and 10th September 2021 – from manipulation of atoms to human needs<abstract> <title style='display:none'>Abstract</title> <p>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.</p> </abstract>ARTICLE2021-08-23T00:00:00.000+00:00Evaluation of variability of silymarin complex in Silybi mariani fructus harvested during two production years<abstract> <title style='display:none'>Abstract</title> <p>Milk thistle [<italic>Silybum marianum</italic> (L.) Gaertn.], a member of <italic>Asteraceae</italic> 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 <italic>P</italic> &lt; 0.05. The total content of silymarin complex was 15.28 ± 0.06<sup>−1</sup> (in 2015) and 16.65 ± 0.09<sup>−1</sup> (in 2016). In both studied years, the highest representation of silybin B was observed (7.04 ± 0.07<sup>−1</sup> versus 5.92 ± 0.08<sup>−1</sup>). 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.</p> </abstract>ARTICLE2021-07-09T00:00:00.000+00:00Rapid and simple CZE-UV method for quality control of B1 and B6 vitamins in drugs and dietary supplements<abstract> <title style='display:none'>Abstract</title> <p>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.</p> </abstract>ARTICLE2021-07-25T00:00:00.000+00:00Characterization of bioactive substances MHGF-68 on tumour cell lines with LiveFlow In Vitro Technology<abstract> <title style='display:none'>Abstract</title> <p>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 <italic>in vivo</italic> 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 <italic>in vivo</italic> 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 <italic>in vivo</italic>.</p> </abstract>ARTICLE2021-06-18T00:00:00.000+00:00Antimicrobial activity and cytotoxicity of transition metal carboxylates derived from agaric acid<abstract> <title style='display:none'>Abstract</title> <p>Carboxylato-type transition metal complexes with agaric acid, a bioactive natural compound derived from citric acid, were prepared, and tested <italic>in vitro</italic> 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 <italic>S. aureus</italic> (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.</p> </abstract>ARTICLE2021-07-25T00:00:00.000+00:00Suspension of Glycosaminoglycans in Oleogel Environment and Application Perspective in GcMAF Immunotherapy<abstract> <title style='display:none'>Abstract</title> <p>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.</p> </abstract>ARTICLE2021-09-02T00:00:00.000+00:00Study of the Qualitative Composition and Quantitative Content of Parthenolide in the Feverfew (Tanacetum Parthenium) Herb Cultivated in Ukraine<abstract> <title style='display:none'>Abstract</title> <p>Feverfew is a well-known medicinal plant as a source of the sesquiterpene lactones, the main one is a parthenolide (about 85%). Owing to the parthenolide, feverfew herb has anti-inflammatory activity and it is widely used for prevention of migraine. The aim was to study the qualitative composition and quantitative content of the parthenolide in the samples of the feverfew herb cultivated in Ukraine and to study the influence of environmental factors on the accumulation of parthenolide.</p> <sec><title style='display:none'>Methods</title> <p>The identification in the samples of the feverfew herb by the thin-layer chromatography method was carried out on silica gel 60 F254 plates, Merck. For the quantitative determination of the parthenolide, a high-performance liquid chromatography ProStar equipped with a diode-matrix detector, were used.</p> </sec> <sec><title style='display:none'>Results</title> <p>The chromatographic profile of the samples of the feverfew herb was studied using a TLC method. In the chromatograms of test solutions from all samples, the blue zones were detected at the level of parthenolide. The quantitative content of parthenolide ranged between 0.16% and 0.39%. The highest content was observed in the sample from the Central region of Ukraine. The data obtained indicate that the optimal conditions for parthenolide accumulation in feverfew herb are as follows: black soils, solar insolation not higher than 5.25 kWh/m<sup>2</sup>/day, average air temperature from +20°C to +25°C. All the calculated validation parameters of the parthenolide quantitative determination method meet the necessary acceptance criteria.</p> </sec> <sec><title style='display:none'>Conclusion</title> <p>The study of the qualitative composition and quantitative content of parthenolide in the samples of feverfew herb cultivated in different regions of Ukraine has been conducted. According to the methodology of Eur.Ph. and SPhU, a parthenolide was identified in all the samples. HPLC method was used to determine the quantitative content of parthenolide in the samples studied. The optimal conditions for parthenolide accumulation in feverfew herb were established.</p> </sec> </abstract>ARTICLE2021-01-29T00:00:00.000+00:00en-us-1