POLYMERIC NANOPARTICULATE FORMULATION TOIMPROVE BIOAVAILABILITY OF METFORMIN IN RATS

摘要

Metformin (MTF) is a biguanide antidiabetic drug administered orally for the treatment of type-2 diabetes mellitus. The aim of this study was to enhance MTF bioavailability through the formulation of MTF as nanoparticles utilizing Eudragit RS100 and Ethyl cellulose as matrix polymers. Nano-precipitation method was used for the preparation of MTF nanoparticles with drug to polymer ratios (1:1, 1:3, and 1:5) for both investigated polymers. The prepared formulations were characterized for particle size, zeta potential, scanning electron microscope (SEM), and in-vitro MTF diffusion. The selected formula, according to the characterization data, was subjected to in vivo Pharmacokinetic studies compared with the marketed MTF product in a randomized parallel pharmacokinetics study. MTF-EudragitRS100 formula (1:3) have shown improved drug loading and encapsulation efficiency with smaller particulate sizes compared with Ethyl cellulose formulae. SEM images shows rounded, homogeneous particle size distribution, and smooth surface for MTF-Eudragit RS100 nanoparticles. Pharmacokinetic results revealed that the selected MTF-Eudragit RS100 nanoparticulate formula improved the bioavailability of MTF by 1.4 fold compared with the marketed MTF tablets.