Objective: A validated liquid chromatography–tandem mass spectrometry (LC–MS/MS) method was developed for canagliflozin in human plasma along with stability studies.
Methods: The chromatographic separation of canagliflozin was performed on Zorbax XDB phenyl (75 × 4.6 mm, 3.5 mm) using methanol:acetate buffer (80:20 v/v) at a flow rate of 1.0 ml/min. The LC–MS/MS system consists of API 4000 triple quadrupole mass spectrometer equipped with turbospray ionization and an AS8020 automatic sample injector.
Results: The retention time of canagliflozin was 1.15 min and total runtime was 2 min. The multiple reaction monitoring was 462.5/267.1 (m/z) for canagliflozin and 466.4/267.2 (m/z) for internal standard (canagliflozin D4), respectively. The method was linear over the range of 10–7505 ng/ml. The calculated slope ranged from 0.0451 to 0.0502 and intercepts from 0.0102 to 0.0456 with coefficients of the determination of 0.9970. The overall mean recovery of internal standard and canagliflozin was 76.66 and 79.77, respectively.
Conclusion: The method was successfully validated and it was found to be within the limits for accuracy, precision, and linearity and it is stable under analytical conditions used.
Objective: Antimicrobial drug resistance is the foremost problem faced worldwide with the current antibiotic therapy in treating infectious diseases. Marine algae were considered as a potential source of biologically active compounds with antibacterial, antifungal, antiviral, and anticancer activities.
Materials and Methods:In the present investigation, the purified fractions of marine algal crude extracts of different solvents such as aqueous, ethyl acetate (EtAc), and ethanol for antioxidant (1,1-diphenyl-2-picrylhydrazyl radical scavenging assay) and antimicrobial activities (agar well diffusion assay) were evaluated.
Results:The extracts of EtAc, ethanol, and water showed minimum inhibitory concentration values of 3.125, 6.25, and 12.25 µg/ml, respectively, for tested bacterial pathogens. The active fractions showed very little activity against Klebsiella pneumonia and Salmonella Typhi, and no activity was observed against Pseudomonas aeruginosa. The results of our screening showed that the EtAc marine algal fractions were active against some Grampositive, Gram-negative bacteria and Candida albicans. The phytochemical analysis of aqueous, ethanolic, and EtAc extracts of marine algae showed the presence of the various phytochemical constituents such as carbohydrates, phenols, and amino acids. The ethanolic extracts showed the highest antioxidant activity as compared to aqueous and EtAc extracts.
Conclusion:This work can be extended further to isolate, characterize, and discover more bioactive metabolites from marine algae, which can be exploited for the production of lead molecules in pharmaceuticals for the treatment of chronic diseases.
Objectives: The present objective for the study was to prepare proliposomal gel bearing an antifungal agent, fluconazole (FLZ) intended for topical application.Methods: Various proliposome formulations were prepared using thin-film hydration technique by varying the lipid phase composition (phosphatidylcholine/cholesterol). Proliposome formulations were characterized for vesicle size, vesicle size distribution, vesicle morphology, drug content, entrapment efficiency, percentage yield value, storage stability analysis, Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), in vitro diffusion study, release kinetic studies, and antifungal activity. Topical proliposomal gels were prepared by incorporation of lyophilized proliposome into a structured vehicle carbopol 934 (2.5%).Results: A spherical shape of reconstituted FLZ liposome with an average vesicle about 5–8 μm was observed in photomicrographs. The percentage entrapment of drug was increased with increase in phospholipid composition in the range of 55.13–69.61%. The FTIR and DSC studies showed no possible drug-excipient interaction. Proliposomal gel showed the prolonged release of FLZ than the lyophilized liposomes. The release kinetic values of regression coefficients confirmed the diffusion-dependent release of the drug. Stability studies indicated that product is stable and should be stored at low temperature.Conclusion: The proposed FLZ proliposomal gel showed sustained release with enhanced antifungal activity implicating its potential in effective transdermal delivery for the topical pharmacotherapy.
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