BIOAVAILABILITY ENHANCEMENT OF ACYCLOVIR USING HIGH-DENSITY GASTRO-RETENTIVE PELLETSAbstract
The objective of the present study was to improve the oral bioavailability using high-density gastro-retentive pellets containing solid dispersion of acyclovir. Solid dispersion prepared with polyvinylpyrrolidone (PVP K30) and hydroxypropyl methylcellulose (HPMC) using different ratios 1:1, 1:2, 1:3, 1:4, and 1:5 by solvent evaporation method and characterized for solubility study, dissolution study, FT-IR, DSC, and XRD. High-density gastro-retentive pellets containing solid dispersion of acyclovir was prepared by extrusion/spheronization technique using solid dispersion of acyclovir with PVP K30 (1:3), Barium sulphate as high-density material, microcrystalline cellulose (MCC) as extrusion aid, ethylcellulose (EC) as release retarding polymer and HPMC as swellable gel-forming polymer. The formulation was optimized based on in-vitro release profile and characterized for pellets morphology, micro-meritics properties, FT-IR, DSC, XRD, and in-vivo study. The optimized formulation F8f showed the release for 12 h with an increase in retention at the absorption site. Release kinetic studies of optimized formulation showed that the data best fit in Higuchi’s model. The in-vivo studies like pharmacokinetic parameters and X-ray transmission were investigated in Wistar rats. The pharmacokinetic study shows that the bioavailability of high-density gastroretentive pellets containing solid dispersion of acyclovir can be increased as compared to a plain drug, marketed formulation, and solid dispersion. The X-ray analysis further ensures that the optimized formulation is retained at the bottom of the stomach, which is essential to improve the absorption window of acyclovir.
N. Gupta, V. K. Rai, T. S. Markandeywar and G. D. Gupta *
Department of Pharmaceutics, ISF College of Pharmacy, Moga, Punjab, India.
02 June 2020
11 October 2020
02 May 2021
01 June 2021