Synthesis of Metformin Hydrochloride nanoliposomes: Evaluation of physicochemical characteristics and release kinetics

Abstract

Metformin hydrochloride, a drug group of biguanides, with significant efficacy in the treatment of diabetes type II, is decomposed before reaching to the stomach and is wasted in great losses. In this study, the nanoliposomes of metformin hydrochloride were prepared with Bingham method. At first, the single factor test is done. Design variables are: lecithin to cholesterol ratio, organic solvent phase to aqueous solvent phase and formation time. The optimal ratios <em>in vitro</em> are obtained 7:1, 4:1, and 2.20, respectively. Entrapment efficiency is obtained 89.74. Then, by design of expert software, RSM method is used in five areas for evaluating the data. Optimum conditions were 6.97:1, 4.46:1, and 151.29, respectively and entrapment efficiency is obtained 90.9. Finally, phosphatidylethanolamine has replaced the lecithin and the entrapment efficiency was obtained as 93.04. So, using of phosphatidylethanolamine has been better than lecithin in pH=7.4. Various physicochemical characteristics of Metformin Hydrochloride nanoliposomes were determined and evaluated. The mean size of metformin hydrochloride nanoliposomes based on phosphatidylethanolamine and lecithin with well-defined spherical shape was 52nm and 83nm, respectively. Based upon the <em>in vitro</em> release profiles, Metformin hydrochloride nanoliposomes exhibited a sustained-releasing potential in addition to the release behavior followed the Weibull equation. Release ratio for nanoliposomes based on phosphatidylethanolamine and lecithin are obtained 20% and 36.66%, respectively. The results indicated that the encapsulation of metformin hydrochloride into nanoliposomes proved to be a promising technology for more widespread uses. Encapsulation by phosphatidylethanolamine nanoliposome and release ratio by lecithin nanoliposome has been desired conditions.