Abstract

In present study is to develop Controlled release muco-adhesive microspheres using natural and synthetic polymers. Controlled release microspheres are one of the multi-particulate delivery systems and are prepared to obtain prolonged or controlled drug delivery, to improve bioavailability, stability, reducing side effects. Controlled release muco-adhesive a microsphere of Diltiazem Hydrochloride was successfully prepared using sodium alginate, Chitosan and HPMC K4M as polymer by the emulsification-internal gelation technique. The prepared formulations were subjected to particle size and shape analysis, % drug entrapment efficiency, swelling rate, in vitro muco-adhesion and in vitro drug release studies. The prepared microspheres were discrete, aprrox spherical with a mean particle size in the range of 513.39 ± 1.21 μm to 839.32 ± 2.24 μm. Entrapment efficiency was found to be in the range of 79.71± 1.134% to 86.13 ±1.065%. Optimized Formulation contains 180 mg Diltiazem Hydrochloride, 600 mg sodium alginate, 225 mg HPMC K4M, 225 mg Chitosan, 74 mg Barium carbonate. The result of optimized formulation for Percent yield, Particle size, Drug Entrapment Efficiency, % Cumulative Drug Release are 91.48 %, 801.789 μm, 2.64, 91.23 %, 83.57 % respectively. Formulated muco-adhesive microspheres were stable at the selected temperature and humidity in storage for 3 month. From the stability studies it was found that there was no significant change in the drug content and release characteristics. It was concluded that the prepared Controlled release muco-adhesive microspheres of Diltiazem Hydrochloride may prove to be potential candidate for safe and effective Controlled drug delivery for extended period of time.