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Detalles de la revista
Formato
Revista
eISSN
1846-9558
Publicado por primera vez
28 Feb 2007
Periodo de publicación
4 veces al año
Idiomas
Inglés

Buscar

Volumen 68 (2018): Edición 2 (June 2018)

Detalles de la revista
Formato
Revista
eISSN
1846-9558
Publicado por primera vez
28 Feb 2007
Periodo de publicación
4 veces al año
Idiomas
Inglés

Buscar

10 Artículos

Original research paper

Acceso abierto

Hydroxyapatite-ciprofloxacin delivery system: Synthesis, characterisation and antibacterial activity

Publicado en línea: 26 Apr 2018
Páginas: 129 - 144

Resumen

Abstract

The main objective of this study was to synthesize hydroxyapatite-ciprofloxacin composites using a chemical precipitation method and to evaluate the properties and in vitro release profile of the drug from the hydroxyapatite-ciprofloxacin composites. Composite characterization was achieved by FT-IR, XRD and DLS. Ciprofloxacin determination was accomplished by HPLC, resulting in good incorporation efficiency of the drug (18.13 %). The in vitro release study (Higuchi model C = K t1/2 and Ritger-Peppas model, C = K t0.6) showed a diffusion-controlled mechanism. The antibacterial activity showed that the bacterial growth inhibition zones were approximately equal for the synthesis composites and for the mechanical mixture on the Staphylococcus aureus germ.

The use of hydroxyapatite, which is a biocompatible, bioactive and osteoconductive material, with ciprofloxacin, which has good antibacterial activity in this composite, makes it suitable for the development of bone grafts. Furthermore, the synthesis process allows a slow local release of the drug.

Palabras clave

  • hydroxiapatite-ciprofloxacin composites
  • wet precipitation synthesis
  • release profile
  • antibacterial activity
Acceso abierto

Preparation and characterization of simvastatin/DMβCD complex and its pharmacokinetics in rats

Publicado en línea: 26 Apr 2018
Páginas: 145 - 157

Resumen

Abstract

Simvastatin is poorly bioavailable because it is practically insoluble in water and shows dissolution rate-limited absorption. Solubilizing effects of several β-cyclodextrin (βCD) derivatives such as HPβCD, SBEβCD and DMβCD on simvastatin in aqueous solution were investigated using the phase solubility technique. The solubility diagram of simvastatin with each βCD derivative could be classified as AL-type, indicating soluble complex formation of 1:1 stoichiometry. Among the above βCD derivatives DMβCD was found to be the ideal complexing agent for improving drug solubility. The simvastatin complex with DMβCD was prepared using the co-evaporation method and was then characterized by differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FT-IR) and in vitro dissolution. Dissolution and pharmacokinetic studies indicated that the simvastatin/DMβCD complex exhibited an increased dissolution rate, rapid absorption, and improved bioavailability in rats compared to free drug. Maximum plasma concentration (cmax) and the time to reach it (tmax) were 21.86 μg mL−1 and 1.4 h for the drug complex, 8.25 μg mL−1 and 3.0 h for free drug, respectively. Main pharmacokinetic parameters such as tmax, cmax were significantly different (p < 0.01) between the simvastatin complex and free drug. Bioavailability of the simvastatin complex relative to free drug was up to 167.0 %.

Palabras clave

  • simvastatin
  • DMCD
  • complex
  • solubility
  • dissolution rate
  • pharmacokinetics
Acceso abierto

Development and evaluation of orally disintegrating tablets containing the mosapride resin complex

Publicado en línea: 26 Apr 2018
Páginas: 159 - 170

Resumen

Abstract

The purpose of this study was to prepare a mosapride citrate-resin (Amberlite® IRP 88) complex and orally fast-disintegrating tablets of the resin complex. The resinate complex of mosapride-Amberlite® IRP 88, mass ratio 2:1, was prepared in an ethanol-water solution. The effects of alcohol concentration, temperature, and pH of the solution on complex formation were evaluated. The complex physicochemical properties were characterized by differential scanning calorimetry, X-ray diffraction and scanning electron microscopy. Orally disintegrating tablets were prepared by direct compression and were optimized using the response surface method. Optimized orally fast-disintegrating tablets disintegrated within 18 s. The pH dependence of mosapride release from the tablet decreased drug dissolution in simulated saliva, whereas it promptly released in the pH 1.0 solution. The data reported herein clearly demonstrate that tablets containing the mosapride-Amberlite® IRP 88 complex for oral disintegration could be particularly useful for patients with swallowing difficulties.

Palabras clave

  • mosapride citrate
  • Amberlite IRP 88 resin
  • resin complex
  • orally disintegrating tablet
  • physicochemical characterization
  • dissolution
Acceso abierto

Reversed phase HPLC for strontium ranelate: Method development and validation applying experimental design

Publicado en línea: 26 Apr 2018
Páginas: 171 - 183

Resumen

Abstract

A reverse-phase HPLC (RP-HPLC) method was developed for strontium ranelate using a full factorial, screening experimental design. The analytical procedure was validated according to international guidelines for linearity, selectivity, sensitivity, accuracy and precision. A separate experimental design was used to demonstrate the robustness of the method. Strontium ranelate was eluted at 4.4 minutes and showed no interference with the excipients used in the formulation, at 321 nm. The method is linear in the range of 20–320 μg mL−1 (R2 = 0.99998). Recovery, tested in the range of 40–120 μg mL−1, was found to be 96.1–102.1 %. Intra-day and intermediate precision RSDs ranged from 1.0–1.4 and 1.2–1.4 %, resp. The limit of detection and limit of quantitation were 0.06 and 0.20 μg mL−1, resp. The proposed technique is fast, cost-effective, reliable and reproducible, and is proposed for the routine analysis of strontium ranelate.

Palabras clave

  • strontium ranelate
  • HPLC
  • experimental design
  • full factorial design
Acceso abierto

Effect of lemongrass water extract supplementation on atherogenic index and antioxidant status in rats

Publicado en línea: 26 Apr 2018
Páginas: 185 - 197

Resumen

Abstract

Cymbopogon citratus (DC) Stapf., commonly known as lemongrass, possesses strong antioxidant and cardiotonic properties. Lemongrass water extract contains several polyphenolic compounds including gallic acid, isoquercetin, quercetin, rutin, catechin and tannic acid. Rutin, isoquercetin catechin and quercetin are the flavonoids most abundantly found in the extract. The extract significantly decreased total cholesterol, low-density lipoprotein and atherogenic index in rats after treatment (p < 0.05). Expression of genes and protein of sterol regulatory element binding protein-1c (SREBP1c) and HMG-CoA reductase (HMGR) was also lowered significantly in treated groups (p < 0.05). Moreover, serum antioxidant capacity increased in treated rats in comparison with untreated ones (p < 0.05) and was associated with decreased serum lipid peroxidation.

Palabras clave

  • lipid profile
  • antioxidant
  • SREBP1c
  • HMG-CoA reductase
Acceso abierto

TLC determination of some flavanones in the buds of different genus Populus species and hybrids

Publicado en línea: 26 Apr 2018
Páginas: 199 - 210

Resumen

Abstract

Flavonoids in the buds of eight Populus species and hybrids were detected and compared with the aid of an optimized TLC method. Separation of 17 flavonoid aglycones belonging to different groups, namely, flavones, flavonols, flavanones and flavanonols, previously described as constituents of poplar buds, was performed on silica gel plates using a hexane/ethyl acetate/formic acid (60:40:1.3, V/V/V) mixture as the mobile phase. Pinocembrin and pinostrobin were found in the majority of analyzed poplar buds. For quantitative analysis of both compounds, two TLC evaluation modes, densitometric and videodensitometric, were compared and the established methods were validated. Concentrations of flavanones in some extracts differed slightly or significantly due to the analyzed plant matrix complexity and the TLC evaluation mode applied. Poplar buds rich in flavanones originated from P. × canadensis ‘Robusta’ (1.82 and 2.23 g per 100 g, resp.) and P. balsamifera (1.17 and 2.24 g per 100 g, resp.).

Palabras clave

  • poplar buds
  • pinocembrin
  • pinostrobin
  • TLC
  • video-densitometry
  • densitometry
Acceso abierto

Paeoniflorin inhibits the growth of bladder carcinoma via deactivation of STAT3

Publicado en línea: 26 Apr 2018
Páginas: 211 - 222

Resumen

Abstract

Bladder cancer (BCa) is one of the most common urinary cancers. The present study aims to investigate whether Paeoniflorin (Pae) can exert inhibitory effects on BCa. The results showed that Pae inhibited proliferation of human BCa cell lines in a concentration- and time-dependent manner. Pae and cisplatin (Cis) synergistically inhibited the growth of tumours in RT4-bearing mice. Pae treatment neutralized the body loss induced by Cis. Moreover, Pae induced apoptosis in RT4 cells and increased the activities of caspase3, caspase8 and caspase9. Western blotting and immunohistochemical analysis revealed that the phosphorylated signal transducer and activator of transcription-3 (p-STAT3) level were decreased in Pae-treated RT4 cells and Pae-treated tumour-bearing mice. Furthermore, STAT3 transcriptional target B-cell lymphoma-2 was decreased in Pae-treated RT4 cells. Interestingly, Pae prevented translocation of STAT3 to the nucleus in RT4 cells. Collectively, Pae inhibits the growth of BCa, at least in part, via a STAT3 pathway.

Palabras clave

  • bladder cancer
  • Radix
  • paeoniflorin
  • apoptosis
  • STAT3

Short communication

Acceso abierto

Topical antifungal bigels: Formulation, characterization and evaluation

Publicado en línea: 26 Apr 2018
Páginas: 223 - 233

Resumen

Abstract

Bigels with antifungal substances, ciclopirox olamine and terbinafine hydrochloride, were made of hydrogel (poloxamer 407 gel) and oleogel (polyethylene and liquid paraffin mixture). Prepared bigels were found physically stable at room temperature for six months and at least four months at 40 °C. Released amount of drug decreased when oleogel concentration in the formulation increased. Release test results depended on the insertion place of active substances. The amount of released substance was highest when ciclopirox olamine was incorporated in both phases in an equal quantity, and terbinafine hydrochloride in oleogel or in hydrogel. All formulations showed great inhibition of Microsporum canis. Thus, bigels with ciclopirox olamine and terbinafine hydrochloride are a promising dosage form for topical use.

Palabras clave

  • bigel
  • ciclopirox olamine
  • terbinafine hydrochloride
  • poloxamer 407
  • antifungal
Acceso abierto

In vitro oxidative stress regulatory potential of Citrullus colocynthis and Tephrosia apollinea

Publicado en línea: 26 Apr 2018
Páginas: 235 - 242

Resumen

Abstract

The present study investigates the potential role of medicinal plants Citrullus colocynthis and Tephrosia apollinea in ameliorating the oxidative stress developed during the generation of reactive oxygen species. Organic extracts of different organs (leaf, stem and root) of these medicinal plants obtained in n-hexane, chloroform, n-butanol and water were assayed for radical scavenging, total antioxidant capacity, anti-lipid peroxidation and reduced glutathione. The total phenolic content (TPC) of both selected medicinal plants was also evaluated. The results indicated that extracts of T. apollinea leaf, stem and root have higher TPC compared to those of C. colocynthis. Similarly, the results of the present study revealed higher bioactivity of C. colocynthis than that of T. apollinea in various antioxidant assays. Various plant parts of each plant were also compared.

Palabras clave

  • oxidative stress
  • total phenolics
Acceso abierto

Spectrofluorimetric method for atenolol determination based on gold nanoparticles

Publicado en línea: 26 Apr 2018
Páginas: 243 - 250

Resumen

Abstract

A simple and sensitive spectrofluorimetric method for determination of atenolol (ATE) using gold nanoparticles (AuNPs) was developed. The method is based on the quenching effect of atenolol on photoluminescence of AuNPs at λem = 705 nm. Variables affecting luminescence of gold nanoparticles such as the solvent, pH value and surfactant were studied and optimized. The method was preliminarily validated according to ICH guidelines. A linear correlation was recorded within the range of 1.0–10 mg mL−1 ATE with the coefficient of determination R2 of 0.999. The limit of detection and limit of quantitation for atenolol were found to be 0.87 and 2.64 mg mL−1, resp. Good recoveries in the range of 98.7–100.0 % were obtained for spiked samples. The proposed method was applied successfully to assaying atenolol in pharmaceuticals formulations.

Palabras clave

  • atenolol
  • spectrofluorimetry
  • gold nanoparticles
10 Artículos

Original research paper

Acceso abierto

Hydroxyapatite-ciprofloxacin delivery system: Synthesis, characterisation and antibacterial activity

Publicado en línea: 26 Apr 2018
Páginas: 129 - 144

Resumen

Abstract

The main objective of this study was to synthesize hydroxyapatite-ciprofloxacin composites using a chemical precipitation method and to evaluate the properties and in vitro release profile of the drug from the hydroxyapatite-ciprofloxacin composites. Composite characterization was achieved by FT-IR, XRD and DLS. Ciprofloxacin determination was accomplished by HPLC, resulting in good incorporation efficiency of the drug (18.13 %). The in vitro release study (Higuchi model C = K t1/2 and Ritger-Peppas model, C = K t0.6) showed a diffusion-controlled mechanism. The antibacterial activity showed that the bacterial growth inhibition zones were approximately equal for the synthesis composites and for the mechanical mixture on the Staphylococcus aureus germ.

The use of hydroxyapatite, which is a biocompatible, bioactive and osteoconductive material, with ciprofloxacin, which has good antibacterial activity in this composite, makes it suitable for the development of bone grafts. Furthermore, the synthesis process allows a slow local release of the drug.

Palabras clave

  • hydroxiapatite-ciprofloxacin composites
  • wet precipitation synthesis
  • release profile
  • antibacterial activity
Acceso abierto

Preparation and characterization of simvastatin/DMβCD complex and its pharmacokinetics in rats

Publicado en línea: 26 Apr 2018
Páginas: 145 - 157

Resumen

Abstract

Simvastatin is poorly bioavailable because it is practically insoluble in water and shows dissolution rate-limited absorption. Solubilizing effects of several β-cyclodextrin (βCD) derivatives such as HPβCD, SBEβCD and DMβCD on simvastatin in aqueous solution were investigated using the phase solubility technique. The solubility diagram of simvastatin with each βCD derivative could be classified as AL-type, indicating soluble complex formation of 1:1 stoichiometry. Among the above βCD derivatives DMβCD was found to be the ideal complexing agent for improving drug solubility. The simvastatin complex with DMβCD was prepared using the co-evaporation method and was then characterized by differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FT-IR) and in vitro dissolution. Dissolution and pharmacokinetic studies indicated that the simvastatin/DMβCD complex exhibited an increased dissolution rate, rapid absorption, and improved bioavailability in rats compared to free drug. Maximum plasma concentration (cmax) and the time to reach it (tmax) were 21.86 μg mL−1 and 1.4 h for the drug complex, 8.25 μg mL−1 and 3.0 h for free drug, respectively. Main pharmacokinetic parameters such as tmax, cmax were significantly different (p < 0.01) between the simvastatin complex and free drug. Bioavailability of the simvastatin complex relative to free drug was up to 167.0 %.

Palabras clave

  • simvastatin
  • DMCD
  • complex
  • solubility
  • dissolution rate
  • pharmacokinetics
Acceso abierto

Development and evaluation of orally disintegrating tablets containing the mosapride resin complex

Publicado en línea: 26 Apr 2018
Páginas: 159 - 170

Resumen

Abstract

The purpose of this study was to prepare a mosapride citrate-resin (Amberlite® IRP 88) complex and orally fast-disintegrating tablets of the resin complex. The resinate complex of mosapride-Amberlite® IRP 88, mass ratio 2:1, was prepared in an ethanol-water solution. The effects of alcohol concentration, temperature, and pH of the solution on complex formation were evaluated. The complex physicochemical properties were characterized by differential scanning calorimetry, X-ray diffraction and scanning electron microscopy. Orally disintegrating tablets were prepared by direct compression and were optimized using the response surface method. Optimized orally fast-disintegrating tablets disintegrated within 18 s. The pH dependence of mosapride release from the tablet decreased drug dissolution in simulated saliva, whereas it promptly released in the pH 1.0 solution. The data reported herein clearly demonstrate that tablets containing the mosapride-Amberlite® IRP 88 complex for oral disintegration could be particularly useful for patients with swallowing difficulties.

Palabras clave

  • mosapride citrate
  • Amberlite IRP 88 resin
  • resin complex
  • orally disintegrating tablet
  • physicochemical characterization
  • dissolution
Acceso abierto

Reversed phase HPLC for strontium ranelate: Method development and validation applying experimental design

Publicado en línea: 26 Apr 2018
Páginas: 171 - 183

Resumen

Abstract

A reverse-phase HPLC (RP-HPLC) method was developed for strontium ranelate using a full factorial, screening experimental design. The analytical procedure was validated according to international guidelines for linearity, selectivity, sensitivity, accuracy and precision. A separate experimental design was used to demonstrate the robustness of the method. Strontium ranelate was eluted at 4.4 minutes and showed no interference with the excipients used in the formulation, at 321 nm. The method is linear in the range of 20–320 μg mL−1 (R2 = 0.99998). Recovery, tested in the range of 40–120 μg mL−1, was found to be 96.1–102.1 %. Intra-day and intermediate precision RSDs ranged from 1.0–1.4 and 1.2–1.4 %, resp. The limit of detection and limit of quantitation were 0.06 and 0.20 μg mL−1, resp. The proposed technique is fast, cost-effective, reliable and reproducible, and is proposed for the routine analysis of strontium ranelate.

Palabras clave

  • strontium ranelate
  • HPLC
  • experimental design
  • full factorial design
Acceso abierto

Effect of lemongrass water extract supplementation on atherogenic index and antioxidant status in rats

Publicado en línea: 26 Apr 2018
Páginas: 185 - 197

Resumen

Abstract

Cymbopogon citratus (DC) Stapf., commonly known as lemongrass, possesses strong antioxidant and cardiotonic properties. Lemongrass water extract contains several polyphenolic compounds including gallic acid, isoquercetin, quercetin, rutin, catechin and tannic acid. Rutin, isoquercetin catechin and quercetin are the flavonoids most abundantly found in the extract. The extract significantly decreased total cholesterol, low-density lipoprotein and atherogenic index in rats after treatment (p < 0.05). Expression of genes and protein of sterol regulatory element binding protein-1c (SREBP1c) and HMG-CoA reductase (HMGR) was also lowered significantly in treated groups (p < 0.05). Moreover, serum antioxidant capacity increased in treated rats in comparison with untreated ones (p < 0.05) and was associated with decreased serum lipid peroxidation.

Palabras clave

  • lipid profile
  • antioxidant
  • SREBP1c
  • HMG-CoA reductase
Acceso abierto

TLC determination of some flavanones in the buds of different genus Populus species and hybrids

Publicado en línea: 26 Apr 2018
Páginas: 199 - 210

Resumen

Abstract

Flavonoids in the buds of eight Populus species and hybrids were detected and compared with the aid of an optimized TLC method. Separation of 17 flavonoid aglycones belonging to different groups, namely, flavones, flavonols, flavanones and flavanonols, previously described as constituents of poplar buds, was performed on silica gel plates using a hexane/ethyl acetate/formic acid (60:40:1.3, V/V/V) mixture as the mobile phase. Pinocembrin and pinostrobin were found in the majority of analyzed poplar buds. For quantitative analysis of both compounds, two TLC evaluation modes, densitometric and videodensitometric, were compared and the established methods were validated. Concentrations of flavanones in some extracts differed slightly or significantly due to the analyzed plant matrix complexity and the TLC evaluation mode applied. Poplar buds rich in flavanones originated from P. × canadensis ‘Robusta’ (1.82 and 2.23 g per 100 g, resp.) and P. balsamifera (1.17 and 2.24 g per 100 g, resp.).

Palabras clave

  • poplar buds
  • pinocembrin
  • pinostrobin
  • TLC
  • video-densitometry
  • densitometry
Acceso abierto

Paeoniflorin inhibits the growth of bladder carcinoma via deactivation of STAT3

Publicado en línea: 26 Apr 2018
Páginas: 211 - 222

Resumen

Abstract

Bladder cancer (BCa) is one of the most common urinary cancers. The present study aims to investigate whether Paeoniflorin (Pae) can exert inhibitory effects on BCa. The results showed that Pae inhibited proliferation of human BCa cell lines in a concentration- and time-dependent manner. Pae and cisplatin (Cis) synergistically inhibited the growth of tumours in RT4-bearing mice. Pae treatment neutralized the body loss induced by Cis. Moreover, Pae induced apoptosis in RT4 cells and increased the activities of caspase3, caspase8 and caspase9. Western blotting and immunohistochemical analysis revealed that the phosphorylated signal transducer and activator of transcription-3 (p-STAT3) level were decreased in Pae-treated RT4 cells and Pae-treated tumour-bearing mice. Furthermore, STAT3 transcriptional target B-cell lymphoma-2 was decreased in Pae-treated RT4 cells. Interestingly, Pae prevented translocation of STAT3 to the nucleus in RT4 cells. Collectively, Pae inhibits the growth of BCa, at least in part, via a STAT3 pathway.

Palabras clave

  • bladder cancer
  • Radix
  • paeoniflorin
  • apoptosis
  • STAT3

Short communication

Acceso abierto

Topical antifungal bigels: Formulation, characterization and evaluation

Publicado en línea: 26 Apr 2018
Páginas: 223 - 233

Resumen

Abstract

Bigels with antifungal substances, ciclopirox olamine and terbinafine hydrochloride, were made of hydrogel (poloxamer 407 gel) and oleogel (polyethylene and liquid paraffin mixture). Prepared bigels were found physically stable at room temperature for six months and at least four months at 40 °C. Released amount of drug decreased when oleogel concentration in the formulation increased. Release test results depended on the insertion place of active substances. The amount of released substance was highest when ciclopirox olamine was incorporated in both phases in an equal quantity, and terbinafine hydrochloride in oleogel or in hydrogel. All formulations showed great inhibition of Microsporum canis. Thus, bigels with ciclopirox olamine and terbinafine hydrochloride are a promising dosage form for topical use.

Palabras clave

  • bigel
  • ciclopirox olamine
  • terbinafine hydrochloride
  • poloxamer 407
  • antifungal
Acceso abierto

In vitro oxidative stress regulatory potential of Citrullus colocynthis and Tephrosia apollinea

Publicado en línea: 26 Apr 2018
Páginas: 235 - 242

Resumen

Abstract

The present study investigates the potential role of medicinal plants Citrullus colocynthis and Tephrosia apollinea in ameliorating the oxidative stress developed during the generation of reactive oxygen species. Organic extracts of different organs (leaf, stem and root) of these medicinal plants obtained in n-hexane, chloroform, n-butanol and water were assayed for radical scavenging, total antioxidant capacity, anti-lipid peroxidation and reduced glutathione. The total phenolic content (TPC) of both selected medicinal plants was also evaluated. The results indicated that extracts of T. apollinea leaf, stem and root have higher TPC compared to those of C. colocynthis. Similarly, the results of the present study revealed higher bioactivity of C. colocynthis than that of T. apollinea in various antioxidant assays. Various plant parts of each plant were also compared.

Palabras clave

  • oxidative stress
  • total phenolics
Acceso abierto

Spectrofluorimetric method for atenolol determination based on gold nanoparticles

Publicado en línea: 26 Apr 2018
Páginas: 243 - 250

Resumen

Abstract

A simple and sensitive spectrofluorimetric method for determination of atenolol (ATE) using gold nanoparticles (AuNPs) was developed. The method is based on the quenching effect of atenolol on photoluminescence of AuNPs at λem = 705 nm. Variables affecting luminescence of gold nanoparticles such as the solvent, pH value and surfactant were studied and optimized. The method was preliminarily validated according to ICH guidelines. A linear correlation was recorded within the range of 1.0–10 mg mL−1 ATE with the coefficient of determination R2 of 0.999. The limit of detection and limit of quantitation for atenolol were found to be 0.87 and 2.64 mg mL−1, resp. Good recoveries in the range of 98.7–100.0 % were obtained for spiked samples. The proposed method was applied successfully to assaying atenolol in pharmaceuticals formulations.

Palabras clave

  • atenolol
  • spectrofluorimetry
  • gold nanoparticles

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