Novel carrier system for enhancing oral delivery of metformin

Abstract

This study was designed to evaluate the potential of PEGylated lipospheres as carriers for improved oral delivery of metformin hydrochloride. Lipospheres were prepared by melt-emulsification method using Phospholipon^® 90H in beeswax (30%w/w) as the lipid matrix containing increasing quantities of PEG 4000 and characterized. The in vitro and in vivo release of the formulations was evaluated. Results show that the particle size and encapsulation efficiency ranged from 33.18±1.75 - 83.23±6.05 μm and 85 to 93%, respectively. Drug release showed a biphasic pattern and was found to follow the Higuchi square root model. Metformin hydrochloride -loaded lipospheres lowered basal blood glucose levels by 60% and sustained antihyperglycemia for over 20 h. This study suggests that encapsulation of metformin hydrochloride into PEGylated lipospheres could reduce its dosing frequency and the associated side effects resulting from high doses of metformin hydrochloride as seen in conventional tablet formulations.

Keywords: PEGylated, lipospheres, metformin hydrochloride, anti-diabetic

African Journal of Biotechnology, Vol 13(50) 4568-4576