Formulation and Evaluation of Mucoadhesive Buccal Patch of Saxagliptin Hydrochloride

Abstract

Buccal route offers the advantage of avoiding first pass metabolism. Saxagliptin Hydrochloride in conventional dosage form is extensively metabolized by the liver. The Saxagliptin Hydrochloride is antidiabetic agent used in the treatment of type-II Diabetes mellitus. The oral bioavailability is 67%. The half-life of saxagliptin Hydrochloride is 2.5 hours and it undergoes hepatic metabolism. So, in order to improve the bioavailability and efficacy, we have prepared buccal patches of saxagliptin Hydrochloride. HPMC is one the polymers which is having good mucoadhesive property so therefore various formulations were developed by using release rate controlling HPMC K100M and Eudragit RL-100 by Solvent Casting technique. In addition to this propylene glycol - 400 was used as plasticizer and permeation enhancer respectively. Drug-excipients interaction study was proven if any. Buccal patches were characterized for number of parameters like Mechanical properties and , weight uniformity, thickness, Percent moisture loss, folding endurance, swelling index, surface pH, drug content uniformity, in-vitro residence time, drug-excipients interaction study, Mucoadhesive strength and in-vitro drug release study. 3 2 full factorial design was employed to study the effect of independent variables. The response of design was analyzed using Design Expert® trial version 7.0.0; and the tools of the software were used to draw Contour plot and 3D plot. On the basis of the software analysis, formulation F7 was selected as optimized formulation and evaluated for independent parameters. Optimized formulation showed 98.35 ± 0.52% dug release upto 6 hrs. Optimized formulation fulfils all necessary attributes required for Buccal Patch and can become a promising alternative to present marketed tablet of Saxagliptin Hydrochloride.