Abstract

FORMULATION, EVALUATION AND OPTIMIZATION OF IN-SITU GEL OF AN ALPHA-GLUCOSIDASE INHIBITOR FOR MANAGEMENT OF NON-INSULIN DEPENDENT DIABETES MELLITUS

Tincy Varghese, Atefeh Shabani, *Agilandeswari D, Ayesha Syed and Mohan Maruga Raja M K.

Abstract

The present study was carried out to develop an effective in-situ proliposomal gel containing Miglitol for treatment of non insulin dependent diabetes. The proliposomes containing Miglitol was prepared by film deposition on carrier method using vacuum rotary evaporator. Proliposomes characterized for vesicle size, surface morphology, drug content, entrapment efficiency, surface charge and yield. Proliposomes containing Miglitol were mixed into the 1%, 2% and 3% gellan gum gel to form proliposomal gels. The gels were characterized for physical appearance, pH, rhelogical properties, drug content, in-vitro and ex-vivo studies. Rheological studies of all proliposomal gels prepared with 1%, 2% and 3% w/w Gellan gum gave clear idea of concentration of Gellan gum (1%) is require for preparation of stable gel formulation. Among all Miglitol proliposomal formulations F1-F9 had maximum vesicle size and entrapment efficiency in the range 72 to 90 % and hence selected for the further study. The percentage yield of formulations was found to be increase with increase in phospholipid concentration in the range of 86.5 ± 0.265 to 95.4 ± 0.221 (mean±SD, n=3). In-vitro studies of proliposomal gels encapsulating drug were found to increase the skin permeation and deposition showing a sustain effect when compared to marketed gel (conventional gel). Results showed that about 43.5% of drug from proliposomal gel and 10.8% of drug from conventional gel deposited on rat skin. This shows that proliposomes not only enhance the penetration of drug molecules but also help to localise the drug within the skin indicating sustain release of drug at site which prevents further inflammation. Hence this study indicated that proliposomal formulations containing Miglitol can be very effective in topical pharmacotherapy.

Keywords: proliposome, gel, Miglitol, gellan gum, stability, penetration.