Formulation and Evaluation of Bioadhesive Vaginal Suppositories Containing Miconazole Nitrate

Miconazole nitrate is an imidazole derivative antifungal agent, developed by Janssen Pharmaceutica, commonly applied topically to the skin or to mucous membranes to cure fungal infections. Over 90% of miconazole nitrate is reported to be bound to plasma proteins. In this study, miconazole nitrate was formulated into bioadhesive vaginal suppositories using different suppository bases such as fatty base, emulsion base and water soluble bases. Bioadhesive polymers (e.g Hydroxyethyl cellulose, sodium alginate and carbopol 934) are incorporated into the fatty and emulsion bases by the use of surfactant as tween 80. Studies are carried out to detect the effect of polymer addition at different concentration levels on the physicochemical properties and the in vitro release pattern. Analysis of the release data was carried out to determine the release kinetics of miconazole nitrate from all bases under investigation. Clinical evaluation of the efficacy of a single vaginal daily dose of miconazole nitrate formulated in different bioadhesive suppositories was carried out by selecting three formulations. They are evaluated for their clinical efficacy in treatment of vaginitis using 60 patients where they use 200 mg miconazole nitrate suppositories intra-vaginally once daily for 5 consecutive days and compared with conventional suppositories (Gynozol) which contain 200 mg drug, via trying on extra 20 patients. Bioadhesive vaginal suppositories showed 100% of the cured cases with the patient group received formula F 17, 90% of the cured cases with the patient group received formula F 9 and 85% of the cured cases with the patient group received formula F 4. On the other hand, Gynozol suppositories gave the lowest percentage of the cured cases, 70%.