Journal of Pharmacy Research最新文献

Aim

The objective of the present investigation was to formulate and evaluate microencapsulated Glibenclamide produced by the emulsion–solvent evaporation method.

Methods

Microparticles were prepared using cellulose acetate by emulsion solvent evaporation method and characterized for their micromeritic properties, encapsulation efficiency, particle size, drug loading, FTIR, DSC, SEM analysis. In vitro release studies were performed in phosphate buffer (pH 7.4). Stability studies were conducted as per ICH guidelines.

Results

The resulting microparticles obtained by solvent evaporation method were free flowing in nature. The mean particle size of microparticles ranges from 132.54 to 178.44 μm and encapsulation efficiency ranges from 89.96 to 98.48%. The infrared spectra and differential scanning calorimetry thermographs confirmed the stable character of Glibenclamide in the drug-loaded microparticles. Scanning electron microscopy revealed that the microparticles were spherical in nature. In vitro release studies revealed that the drug release was sustained up to 12 h. The release kinetics of Glibenclamide from optimized formulation followed zero-order and peppas mechanism. The mechanism of drug release from the microparticles was found to be non-Fickian type.

Conclusion

Cellulose Acetate microparticles containing Glibenclamide could be prepared successfully by using an emulsion solvent evaporation technique, which will not only sustain the release of drug but also manage complicacy of the diabetes in a better manner.

Aim

The aim of this work is to design & characterize a collagen based dermal films containing natural extracts such as Terminalia arjuna and Centella asiatica having antioxidant properties for enhancing the quality of wound healing.

Methods

The collagen and cross-linked collagen films were formulated with different concentrations of the selected extracts. The formulated films were subjected to physical, biochemical and histopathological examinations.

Results

Folding endurance reports revealed that the films possessed the desired mechanical strength to withstand the stress observed during handling. Micro shrinkage temperature of the extract impregnated films was found to be above 68 °C indicating their hydrothermal stability. Wound healing studies on male Wistar rats revealed that the groups treated with 1.5% T. arjuna extract impregnated cross-linked collagen dermal films (1.5% TAEICCDF's), 15% extract impregnated collagen dermal films (1.5% TAEICDF's), 1.5% C. asiatica extract impregnated cross-linked collagen dermal films (1.5% CAEICCDF's), 1.5% C. asiatica extract impregnated collagen dermal films (1.5% CAEICDF's) possessed higher amount of hydroxyproline content compared to the marketed formulation – Neuskin™. The cross-linking of the CAEICDF's, TAEICDF's had a significant impact at p > 0.05 from student ‘t’ test on wound healing compared to the non-cross-linked films. Further one-way classification ANOVA studies conducted for all the groups treated with natural extract impregnated films varied significantly (P = 0.05 from one-way ANOVA).

Conclusion

The histopathological studies indicated more production in the collagen content in groups treated with 1.5% TAEICCDF's, 1.5% TAEICDF's, 1.5% CAEICCDF's, 1.5% CAEICDF's which resulted in the epithelial group reduction. Further rise in fibroblasts in these treated groups suggested that the films are fit to productive approach in the improvement of dermal wound healing process.

Background

Diabetes mellitus is one of the most common endocrine disorders accompanied with many metabolic syndromes. Use of herbal medicines has always been an option to treat a great number of diseases such as diabetes and its complications. The aim of the present study is to investigate the liver protective effects of Syzygium cumini seed extract in alloxan induced diabetic Swiss albino mice.

Methods

Eighteen Swiss albino mice (weighing 28–32 g) were randomly divided into control, alloxan treated and S. cumini treated mice group. Diabetes was induced in mice by injecting intraperitoneally alloxan monohydrate at dose of 150 mg/kg body weight. Aqueous extracts of S. cumini seed at dose of 250 mg/kg body weight were given orally in diabetic mice daily for three weeks after established LD₅₀ value.

Results

In diabetic mice, the SGOT, SGPT, Bilirubin and serum glucose levels were significantly increased in comparison with the control groups. Statistical analysis (p < 0.05) of the data indicated that aqueous extract of S. cumini were significantly decrease serum contents of liver enzymes (SGOT, SGPT and Bilirubin) as well as serum glucose in treated groups.

Conclusion

The results suggested that aqueous extracts of S. cumini seed possesses liver protective effect against alloxan induced diabetic mice.

Background

The aim of this study is to isolate and structurally elucidate the flavone glycoside: 5,4-dihydroxy–3-(3-methyl-but-2-enyl) 3,5,6-trimethoxy-flavone-7-O-β-d-glucopyranoside from Feronia limonia L.

Methods

The air dried, powdered and defatted material of F. limonia L. fruits were extracted with rectified spirit extract was concentrated under reduced pressure to get a brown viscous mass, which was successively partitioned with petroleum ether, benzene, chloroform, ethyl acetate, acetone and methanol respectively. The ethyl acetate soluble part was concentrated under reduced pressure to get a brown syrupy mass, which when examined by TLC on silica-gel G using chloroform:methanol:water (8:5:3) and iodine vapors as visualizing agent displayed two spots. As such it was subjected to column chromatography on silica-gel Emerk and eluted by with acetone:methanol in various proportions. On removal of the solvent of fraction (7:4), light yellow needles (RS-2) were separated out. RS-2 was found to be homogenous on TLC (MeOH:H₂O:ACOH, 4:6:1).

Results

RS-2 responded to all the following characteristic color reactions for flavonoids (Shibata test and reaction with 5% FeCl₃) and also responded positively to Molisch test of glycoside; spectral analysis of the sample clearly showed the characteristic peaks of flavone glycoside as depicted in (Graph 1, Graph 2, Graph 3, Graph 4).

Conclusion

On the basis of spectral data obtained, the compound was identified as 5,4-dihydroxy–3-(3-methyl-but-2-enyl) 3,5,6-trimethoxy-flavone-7-O-β-d-glucopyranoside. Survey of the literature clearly indicated that 5,4-dihydroxy–3-(3-methyl-but-2-enyl) 3,5,6-trimethoxy-flavone-7-O-β-d-glucopyranoside, this is the first report from the fruit pulp of F. limonia L. a novel compound.

Aim

The objective of the investigation was to predict the three dimensional structure of ageing related proteins of Silurana tropicalis Gray 1864.

Methods

The protein sequences were collected from UniProt. Homology modeling of protein structures was generated in SWISS-MODEL workplace. The structures were assessed by ERRAT and RAMPAGE.

Results

In S. tropicalis Gray 1864, ageing related total 5 proteins sequences namely prohibitin-2 (301 aa), serum response factor-binding protein 1 (535 aa), reactive oxygen species modulator 1 (79 aa), CDGSH iron-sulfur domain-containing protein 2 (135 aa) and an uncharacterized protein (668 aa) were found (UniProt). SWISS-MODEL workspace generated reliable 3D structures of only two proteins prohibitin-2 (301 aa) and CDGSH iron-sulfur domain-containing protein 2 (135 aa), while it failed to give proper structures for other proteins due to lack of templates. In ERRAT assessment, prohibiin-2 and CDGSH iron-sulfur domain-containing protein 2 scored 51.82% and 97.48% respectively. While in RAMPAGE, prohibitin 2 and CDGSH iron-sulfur domain-containing protein 2 scored 90.7% and 97.7% respectively.

Conclusion

The present study demonstrated the 3D structures of prohibitin-2 and CDGSH iron-sulfur domain-containing protein 2.

Background

The present study explicates the effect of metals ion (Ca²⁺) on the in vitro availability of Amlodipine besylate owing to drug–metal interaction.

Methods

Spectral studies were performed in an aqueous system at a fixed temperature (37 ± 0.5)°C and under different pH by UV spectrophotometric method at various concentrations of drug and metal. A Job plot was used to determine the stoichiometry of a binding event and The Ardon's method confirmed the complexation. An in vitro study of protein binding of Amlodipine besylate and their 1:1 mixture with Ca²⁺ ion had been conducted by equilibrium dialysis method at (37 ± 0.5)°C and at pH 7.4 by using Bovine Serum Albumin (BSA).

Results

Spectral studies detected the initial complexation. By Job's plot it was found that the interaction of Amlodipine besylate with metal ion (Ca²⁺) form one complex with metal at composition of 1:1. The Ardon's spectrophotometric method confirmed the 1:1 complexation and the value of stability constant was higher at pH 7.4 (0.11). The percentage of protein binding of Amlodipine besylate with BSA was found to be 86% and 42% at high and low concentration range respectively. In presence of Ca²⁺ the percentage of protein binding of drug increased 46% at lower concentration range and 94% at higher concentration zone. The results were statistically significant (p < 0.05).

The Scatchard plots showed that in class I binding sites, the value of affinity constant and number of binding sites of 1:1 complexes with Ca²⁺ was 1.04 and 20.8 respectively.

Conclusion

Drug–metal complex might, therefore, decrease the free drug in plasma and tissue systems. This may change the pharmacokinetic properties of the drug and may affect the pharmacological effects. It is thus inferred that care and monitoring must be taken during combination therapy of Amlodipine besylate and Ca²⁺.

Novel 3,4,5-triarylisoxazole derivatives were synthesised by Suzuki reaction of 4-bromo-3, 5-diaryl isoxazoles with various boronic acid under microwave condition. The structures of the newly synthesised compounds are characterised by ¹H NMR, ¹³C NMR, LC-MS and screened for their antifungal activity against Aspergillus flavus (NCIM No. 524), Fusarium oxysporum (NCIM No. 1072) and Candida albicans (NCIM No. 3102).

Objective

The present study was aimed to evaluate phytochemical constituents and the safety of methanolic extract of root parts of Curculigo orchioides (MECO) by determining their potential toxicity after acute and 28-day repeated dose administration in Wistar Albino rats.

Methods

The phytochemical analysis was done by standard laboratory grade reagents. Acute and 28-day repeated dose oral toxicity studies were performed by the following OECD test guidelines 423 and 407 respectively.

Results

The present study reveals the presence of complex phytochemical constituents like flavonoids, saponins, glycosides, terpenoids, steroids and phenols. In acute toxicity study no treatment related death or toxic signs were observed with MECO administration. In repeated dose study no significant differences in body weight changes and hematology was observed between control and MECO groups. Conversely there was a decrease in serum glucose and cholesterol levels and an increase in protein levels in treated rats compared to control. No gross pathological findings and difference in relative organ weights were observed between control and treated rats. Histopathological examination revealed no abnormalities with the test drug treatment.

Conclusion

In conclusion C. orchioides was found to be non toxic in tested doses and experimental conditions.

Aim

Didanosine, a nucleoside reverse transcriptase inhibitor, is used to treat HIV infection in patients with or without acquired immunodeficiency syndrome. The objective of this study is to prepare didanosine loaded bovine serum albumin nanoparticles by desolvation technique and coated with 1% polysorbate 80 to improve antiretroviral therapy.

Method

Bovine serum albumin nanoparticles containing didanosine were prepared by desolvation technique and cross linked with 8% v/v glutaraldehyde solution. Ethanol and mannitol were used as a desolvating agent and cryoprotectant respectively. The formulated nanoparticles were characterized, evaluated and were subjected to stability studies over a period of three months. Biodistribution studies were investigated for the best formulation (D1).

Results

Nanoparticle size was averaged below 270 nm with 0.2 PDI and zeta potential was in the range of −23.0 to −36.6. Encapsulation efficiency ranges from 66 to 85.71% and % drug loading ranges from 9.48 to 28.34. Cumulative percent drug release was in range of 60–80% and release kinetics suggested that drug release was Fickian diffusion controlled. The stability studies over period of 3 months confirmed the stability of BSA nanoparticles. Biodistribution studies demonstrated that the drug level in macrophage organs can be enhanced by coating of nanoparticles with 1% polysorbate 80.

Conclusion

The method adopted is simple and able to prepare stable, spherical shaped nanoparticles which exhibit slow and sustained release.

Background

Plant-based foods provide, not only essential nutrients needed for life, but also other bioactive compounds for health promotion and disease prevention. Standardization is an essential measure of quality, purity and authenticity. The present study focuses on the investigation of physiochemical parameters and to identify and quantify Stigmasterol from the leaves of Dipteracanthus patulus (Jacq.) Nees.

Methods

Physiochemical analyses like total ash, acid insoluble ash, water soluble ash, moisture content (Loss on Drying) and extractive values were calculated by standard procedures. High performance liquid chromatography with photo diode array detector (HPLC-PDA) was used to quantify Stigmasterol in the methanolic leaves extract of D. patulus.

Results

The percentage of the total ash, acid insoluble ash, water soluble ash and moisture content (Loss on Drying) were 9.1%, 1.3%, 6.2% and 4.1% respectively. The methanolic extractive value was found to be higher (13.4%). HPLC analysis revealed that the methanolic leaves extract showed the presence of Stigmasterol and the content was 0.22 mg/g dry weight which supports the biological potency of the plant.

Conclusion

Physiochemical analyses have shown the purity and quality of crude drug. Quantitative estimation by HPLC-PDA revealed the presence of good percentage of stigmasterol in D. patulus. This study has grasped the importance since stigmasterol possesses lipid peroxidation inhibitory action and anticancer activity. These features make this plant a promising candidate for the further studies on isolation and pharmacological studies of this compound from D. patulus.