Abstract

The study was undertaken to formulate and evaluate PEGylated-mucin matrices-based solid microparticles for oral administration of metformin hydrochloride (MTH). PEGylated-mucin matrices formulated with PEG-2000 and Mucin were used to prepare metformin-loaded PEGylated-mucin using solvent interaction method. Characterizations based on size and morphology, zeta potential and polydispersity index, loading and encapsulation efficiency (EE%) were carried out on the PEGylated matrices. In vitro release of metformin from the preparation was performed in phosphate buffer while in vivo release as a function of the antidiabetes effects were conducted in alloxan induced diabetes rats. Maximum and minimum EE% of 81.0 and 44.0% were obtained for matrices formed with PEG-Mucin ratio of 3:1(D) and 0:1(B), respectively. Irregular and rough matrices of size range 58.80 ± 0.21 µm to 124.1 ± 0.1 µm were produced. The release of MTH in phosphate buffer varied widely with the PEG and Mucin contents. Moreover, significant (p<0.005) amount of MTH was released in vivofrom the matrices as demonstrated in the basal glucose reduction than the positive control. These results demonstrated that PEGylated matrices would likely to offer a reliable means of delivering metformin orally.

Key words: PEG–Mucin, diabetics, metformin, bioactivity.