EFFERVESCENT BIOADHESIVE VAGINAL TABLET OF METRONIDAZOLE FOR BACTERIAL VAGINOSIS – DESIGN AND IN-VITRO EVALUATION

In the present study, the effort has been made to formulate the effervescent bioadhesive vaginal tablet of Metronidazole for localized treatment of Bacterial vaginosis. Among various bioadhesive polymers carbopol 934P, hydroxyl propyl methylcellulose K4M, methylcellulose, and sodium carboxymethyl cellulose were selected. Eight different formulations were made using a single polymer as well as a combination of two polymers in 1:1 ratio by direct compression technique. Formulations containing carbopol 934P alone (F4), carbopol 934P and sodium CMC in 1:1 ratio (F8) and carbopol 934P and hydroxypropyl methylcellulose K4Min 1:1ratio (F6) showed high, medium and low swelling behavior and bioadhesion property respectively and other formulations were found to disintegrate in 1 h time during swelling study as well as during dissolution study. In-vitro drug release was found to be 51.03% for F4, 42.98% for F8, and 34.87% for F6 at 12 h. F4 was found to release half of the total drug in 12 h. Based on swelling behavior, bioadhesion test, and in-vitro drug release, F4 was selected as the best formulation. In-vitro drug release data were fitted in various kinetic models in which drug release data were found to follow zero order kinetics and Korsmeyer-Peppas model. Stability study was conducted for F4 formulation as per ICH guidelines and showed no significant changes. From the research, it was found that the carbopol 934P can be used to prepare once a daily vaginal tablet for sustaining the localized release of metronidazole in Bacterial vaginosis.