Acta Pharm. 63 (2013) 359-372

full paper

Original research paper

Bioadhesive vaginal tablets containing spray dried microspheres loaded with clotrimazole drug for treatment of vaginal Candidiasis

NARESH VISHAL GUPTA, SHIRODKER NATASHA, ANIL GETYALA and RAMNATH SUDEENDRA BHAT

vkguptajss@gmail.com

Department of Pharmaceutics, JSS College of Pharmacy, JSS University, Sri Shivarathreeshwara Nagar, Mysore-570015, Karnataka, India

Accepted May 7, 2013

The aim of the present investigation was to prepare and evaluate novel bioadhesive vaginal tablets containing clotrimazole loaded microspheres in order to provide long-term therapeutic activity at the site of infection. Tablets were prepared by incorporating drug loaded microspheres and using bioadhesive polymers hydroxypropylmethylcellulose, sodium carboxymethylcellulose and Carbopol. Microspheres were prepared by the spray drying technique using Eudragit RS-100 and Eudragit RL-100. Microspheres were characterized by SEM, DSC, FTIR, particle size analysis and evaluated for percentage yield, drug loading, encapsulation efficiency and in vitro drug release. To achieve bioadhesion to the mucosal tissue, optimized microspheres were incorporated into bioadhesive tablets and were evaluated for in vitro drug release, in vitro and in vivo mucoadhesion. FTIR and DSC studies indicated that no chemical interaction occurred between the drug and polymers. The sphericity factor indicated that the prepared microspheres were spherical. Formulation Mt6 showed a controlled in vitro drug release and good bioadhesive strength. The in vivo images confirmed the bioadhesion and retention property of tablet up to 24 h. The results indicated that this drug delivery system can be explored for controlled intravaginal drug release.

Keywords: clotrimazole, microspheres, bioadhesive vaginal tablet