Formulation Design and Evaluation of a Novel Vaginal Delivery System of Clotrimazole

The present investigation was to prepare and evaluate bioadhesive vaginal gel containing clotrimazole loaded microspheres a novel delivery system for vaginal use. Bioadhesive gel was prepared by incorporating drug loaded microspheres using bioadhesive polymer carbopol 934. Microspheres were prepared by spray drying technique using Eudragit RS-100 and RL-100 polymers with different drug/polymer ratios. Microspheres were characterized by SEM, DSC, FT-IR and particle size analysis and evaluated for morphology, drug loading and in vitro drug release in simulated vaginal fluid. The FT-IR and DSC spectra revealed that there was no chemical interaction between drug and polymers used. SEM revealed that microspheres were spherical with a smooth surface morphology indicating that CTZ was well dispersed inside the carrier with a mean particle size ranging from 17 -58 μm. The in vitro drug release from formulation M1 to M6 was found to be 83.10% to 98.88% at the end of 12 h. Among various formulations M4 was found to have good control release pattern as it has shown 99% drug release in 12 hours and hence to achieve bioadhesion to mucosal tissue formulation M4 was incorporated in the bioadhesive gel made of carbopol 934P. Clotrimazole microspheres gel (CTZ-MG) was characterized by in vitro drug release and antifungal activity. The drug release was controlled up to 24 h. Inhibition effect on the C. albicans j1012 growth, suggested their effectiveness in the treatment of vaginal candidiasis. Result of this study suggests that CTZ-MG can be used as a novel controlled delivery system for local therapy of vaginal candidiasis. INTRODUCTION: Microencapsulation is widely used in the pharmaceutical and other sciences to mask tastes or odors, prolong release, impart stability to drug molecules, improve bioavailability, and as multi-particulate dosage forms to produce controlled or targeted drug delivery. QUICK RESPONSE CODE DOI: 10.13040/IJPSR.0975-8232.5(1).220-27 Article can be accessed online on: www.ijpsr.com DOI link: http://dx.doi.org/10.13040/IJPSR.0975-8232.5(1).220-27 It is therefore a rapidly expanding technology for achieving sustained-release dosage forms. Up to now, only few studies reported the use of microspheres for the treatment of vaginal diseases. For instance bioadhesive microparticles, PLGA microspheres and polymer lipid based mucoadhesive microspheres were assessed as vaginal delivery systems. Moreover, chitosan based microspheres loaded with an antimicrobial drug were added to different mucoadhesive excipients (cellulose derivatives, sodium alginate or Carbopol® 974) to prepare mucoadhesive vaginal