BIOAVAILABILITY AND DISSOLUTION ENHANCEMENT OF GLYBURIDE NANOSUSPENSION
Journal Title: Asian Journal of Pharamceutical and Clinical Research - Year 2019, Vol 12, Issue 4
Abstract
Objective: The main objective was to develop nanosuspension of glyburide (GLY) by quasi emulsification solvent diffusion method and to enhance dissolution and bioavailability characteristics of the drug GLY, an antidiabetic drug which belongs to Biopharmaceutical Classification System-II category. Materials and Methods: In this work, nanoparticles were prepared using polyvinyl alcohol, hydroxypropyl methyl cellulose, and Eudragit RL100. Twelve formulations of GLY (GLY-1–GLY-12) were formulated using the excipients at various compositions. Drug and excipient compatibility studies were conducted using Fourier transform infrared and differential scanning calorimeter. The prepared nanosuspension was analyzed using scanning electron microscopy for surface of the particle analysis, melting point, solubility, particle charge zeta (mv), percentage drug entrapment efficiency (%), and in vitro drug release. The optimized formulations of nanosuspension were further studied for in vivo pharmacokinetic evaluation. Reverse-phase high-performance liquid chromatography method was developed, validated, and used for the study of these formulations in rat plasma. Results: From these studies, it was confirmed that drugs and excipients chosen were compatible with each other. GLY-8 was the best formulation with a particle size of 85–96 nm with 168.7°C melting point, freely soluble in phosphate buffer pH 7.4, 93.53% drug entrapment, and 90.26±1 mV of zeta potential. This formulation shows percentage drug release of 99.85% in 24 h. In vivo pharmacokinetic study for optimized formulation (GLY -8) suggested that there was no reaction with the rat plasma. From the results, it was shown that Cmax and Tmax were found to be 0.604±0.03 μg/ml and 2±1.01 h, respectively. The values of t1/2 (h), area under the curve (AUC) (0-t), and AUC (0-∞) were found to be 10.04 h, 2.562±0.41 μg.h/ml, and 2.147±0.45 μg.h/ml, respectively. Conclusion: Based on the results obtained, oral administration of nanosuspension could not only provide the better absorption of poorly water soluble drugs but may also reduce toxicity and provide a new tool in drug delivery system.
Authors and Affiliations
PRADEEP KUMAR M
Keywords
Related Articles
- EP ID EP604665
- DOI -
- Views 130
- Downloads 0
IN VITRO MASS PROPAGATION AND SYNTHETIC SEED PRODUCTION COMBINED WITH PHYTOCHEMICAL AND ANTIOXIDANT ANALYSIS OF BACOPA CHAMAEDRYOIDES: AN ETHNO-MEDICINALLY IMPORTANT PLANT
Objective: This study was carried out to optimize adventitious shoot buds induction from the surface of the leaf and internode explants along withinvestigation of the phytochemical constituents and in vitro antioxidant p...
CONTROLLED VESTIBULAR STIMULATION: PHYSIOLOGICAL INTERVENTION IN DIABETES CARE
ABSTRACTObjective: The present study was aimed to assess the role of vestibular stimulation in the management of diabetes care.Methods: We carried out the present study in 83-year-old man with 20 years history of Type 2...
MELOXICAM-PECTIN-β-CYCLODEXTRIN TERNARY COMPLEX BY KNEADING FOR ENHANCEMENT OF SOLUBILITY AND DISSOLUTION RATE
Objective: The objective of the present investigation was to improve the solubility and dissolution rate of poorly soluble drug meloxicam by its ternary inclusion complexation with natural polymers and beta-cyclodextrin...
GAS CHROMATOGRAPHY-MASS SPECTROMETRY ANALYSIS, IN VITRO ACTIVITIES, AND IN SILICO MOLECULAR DOCKING OF MAJOR COMPONENTS OF MICHELIA ALBA DC ESSENTIAL OIL AND SCENTED EXTRACTS
Objective: The essential oil and scented extracts of Michelia alba DC. were analyzed by gas chromatography–mass spectrometry (GC–MS) and investigated for antidiabetic activities in vitro and in silico. Methods: The...
IN VITRO ANTIOXIDANT AND ANTICANCER ACTIVITIES OF ETHANOLIC FRUITS EXTRACT OF Ziziphus jujube Mill.
Objective: Antioxidant and anticancer studies of the ethanolic fruit extract of Ziziphus jujuba were aimed at detecting the phytochemicals and ascertain the antioxidant and anticancer activities using in vitro experiment...