Abstract

FORMULATION AND EVALUATION OF NOVEL GASTRORETENTIVE MUCOADHESIVE MICROSPHERES OF CYPROHEPTADINE HYDROCHLORIDE FOR SUSTAINED RELEASE

Clyte Fernandes*, Rasvita Gawas and Rajashree Gude

Abstract

The objective of this study was to formulate and evaluate gastroretentive mucoadhesive microspheres of Cyproheptadine hydrochloride using mucoadhesive polymers. It was expected that gastroretention and mucoadhesion would result in sustained release of the drug thereby providing this formulation as a potential candidate for reducing the dosing frequency of Cyproheptadine hydrochloride. The mucoadhesive microspheres of Cyproheptadine hydrochloride were formulated by orifice ionotropic gelation method using blend of sodium alginate and different concentrations of mucoadhesive microspheres such as carbopol 934P, sodium carboxy methyl cellulose and hydroxy propyl methyl cellulose E5. The microspheres were Evaluated for percentage yield, particle size, shape and surface morphology, entrapment efficiency, swelling index, mucoadhesivity, in-vitro drug release and stability studies. The microspheres formed were discrete, spherical and free-flowing and the size ranged from 500-960 μm. The drug entrapment efficiency was found to be in the range of 54.28% to 90.14%. The IR spectroscopy studies confirmed no major interaction between the drug and the excipients. The optimum formulation was found to be F4 with in-vitro release rate of 92.48% in 10 hours. It was revealed that the drug release from microspheres was diffusion controlled and followed first order kinetics. Stability studies were carried out on the optimum formulation F4 which indicated that there was no change in the particle size and entrapment efficiency of the drug. In the present work it was concluded that gastroretentive mucoadhesive microspheres forms an effective drug delivery system for Cyproheptadine hydrochloride in reducing the dosing frequency and hence improving patient compliance.

Keywords: Cyproheptadine hydrochloride, mucoadhesive microspheres, orifice ionotropic gelation.