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 144
- Downloads 0
CHRONOTHERAPEUTIC DRUG DELIVERY SYSTEM: AN EMERGING APPROACH TO TREAT CIRCADIAN RHYTHMIC RELATED DISEASE
The research on chronotherapy has garnered interest from scientists to understand circadian rhythms and their applications in the biological system. The area of chronotherapeutics covers essential information which is he...
PREPARATION AND EVALUATION OF ULTRASOUND TRANSMISSION GEL
Objective: Formulation of an alternative ultrasound transmission gel that is of good quality using the available chemicals in Iraqi market and without any harmful effects to skin. Methods: Four formulas G1, G2, G3, and G...
The ROLE OF HERBAL ANTIFUNGAL AGENTS FOR THE MANAGEMENT OF FUNGAL DISEASES: A SYSTEMATIC REVIEW
Nowadays, fungal infection of skin is one of the most common dermatological problems worldwide. It has been investigated that 40 million people suffer from fungal infections. Superficial and subcutaneous fungal infection...
RP-HPLC METHOD DEVELOPMENT AND VALIDATION FOR THE SIMULTANEOUS ESTIMATION OF ATORVASTATIN AND EZETIMIBE IN PHARMACEUTICAL DOSAGE FORM
 Objective: The aim was to develop a simple, selective, linear, precise, and accurate reverse phase high performance liquid chromatography methodfor simultaneous estimation of atorvastatin and ezetimibe in tablet dosage...
IN VITRO EVALUATION OF THE ANTHELMINTIC ACTIVITY OF RHIZOME EXTRACTS OF CURCUMA LONGA (LINN.)
Objective: The current study was carried out to evaluate the anthelmintic activity of the rhizome extract of Curcuma longa as an alternative source of effective remedies for nematodiasis.Methods: The anthelmintic activit...