Abstract

FORMULATION AND EVALUATION OF MUCOADHESIVE MICROSPHERES OF ANTIHYPERTENSIVE DRUG

*Vandana Verma and Dr. Madhubhai M. Patel

ABSTRACT

The objective of the present investigation is to formulate and evaluate Ramipril mucoadhesive microsphere using hydroxypropyl methylcellulose, ethyl cellulose and Carbopol. Microspheres prepared by solvent evaporation technique using span 80. Ethyl cellulose a release controlling polymer Carbopol as mucoadhesive polymer. The shape and surface morphology of prepared microspheres were characterized by optical and scanning electron microscopy, respectively. In vitro drug release studies were performed and drug release evaluated. Effects of polymer concentration on size of microspheres and drug release were observed. The prepared microspheres exhibited prolonged drug release the mean particle size increased as the concentration of polymer increased. The shape and surface morphology of prepared microspheres were characterized by optical microscope. Scanning electron microscopy showed that the microspheres were spherical with rough shape, dense and less porous in surface. The particle size found within the range 220-392μm. In vitro drug release studies were performed and drug release evaluated. The drug release for formulation F2(68.16%), F6(71.88%) and F10(66.84%) was found better in sustain the drug release. The in vitro wash off test for percentage mucoadhesion after 1 h varied from 65% to 97%. As the amount of polymer (Carbopol) increased the in vitro mucoadhesion increased may be due to the fact the amount of polymer results in a higher amount of free –COOH (carboxyl) groups available for binding with the sialic acid residues in mucus layer increases, results in increase in vitro mucoadhesion.

Keywords: Mucoadhesive microspheres Ramipril, Ethyl cellulose, HPMC, Carbopol, Solvent evaporation method.