Abstract

FORMULATION, DEVELOPMENT AND EVALUATION OF ABACAVIR SUSTAINED RELEASE MICROSPHERES

Yogesh Shendey*, Manju Prajapati, Parul Mehta, J.P. Rai

School of pharmacy, LNCT University, Bhopal (M.P.)

ABSTRACT

The purpose of this study was to develop and evaluate Abacavir loaded mucoadhesive microsphere for sustained drug release at the gastric mucosa. In present investigation Chitosan microspheres of Abacavir were prepared by using ionotropic gelation method. Different formulations F1 to F6 were prepared using varying amount of polymers like chitosan and TPP. The prepared and evaluated for Percentage yield, stability of microspheres, drug entrapment mean particle size, zeta potential and In vitro drug release study. Percentage yield of different formulation was determined by weighing the microspheres after drying. The percentage yield of different formulation was in range of 63.32±0.45–72.23±0.54%. The drug entrapment of different formulations was in range of 65.58±0.45-75.56±0.25% w/w. The maximum percentage yield and entrapment efficiency was found formulation F3 (75.56±0.25). The optimized formulation among other batches subjected to further studies. The stability of all the batches of microspheres was determined by measuring the transmission after the microspheres had been exposed to 0.1N HCl. The In vitro drug release data of the optimized formulation was subjected to goodness of fit test by linear regression analysis according to zero order and first order kinetic equsation, and Korsmeyer’s models in order to determine the mechanism of drug release. When the regression coefficient values of were compared, it was observed that ‘r’ values of Pappas order was maximum i.e 0.978 hence indicating drug release from formulations was found to follow Pappas order release kinetics. Mucoadhesive microspheres can be effectively used for sustained drug release to the gastric mucosa in treatment of upper GIT infection.

Keywords: Floating microsphere, Abacavir, Ionotropic gelation method