The Formulation Research Of A Novel Microbicide

Sexual transmission of HIV/AIDS is becoming the leading route of infection. A number of factors contributing to the current threats are the unlikelihood of the success for effective vaccine in the near future, the difficulties with condom use by male sex partners, UNAIDS and WHO raised the urgency to develop new interventions for females protection from infections. Microbicide as an alternative tool for preventing STD including HIV, is a class of product that can be placed into the vagina or anus before sexual intercourse.FB006 is a 34 amino acids peptide, an HIV fusion inhibitor invented by Frontier Biotechnologies. It is soluble with broad spectrum of antiviral efficacy against many strains of HIV in vitro, and stable in the acidic vaginal environment. It showed no irritation to genital tract mucosa, no other toxicity or adverse effect to sperms and lactobacilli. It is an ideal candidate for microbicide to prevent HIV.The purpose of current formulation study was to establish a novel microbicide based on the FB006. By selecting proper formulation, the anti-HIV efficacy of FB006 can be maximized with excellent biocompatibility for preclinical studies. The study emphasized on selection of dosage form, formulation research, preparation process and product evaluation, quality control and the initial stability study of the formulation.The physical and chemical properties of FB006 were analyzed and its stability examined under different pH values. Different dosage forms and formulations with commonly used excipients were screened for future preclinical studies and clinical applications. Based on the characteristics of vaginal commonly used formulations and the clinical compliance, the water-soluble gel (semi-solid) was preferred.The gel matrix, pH adjusting agents, moisturizing agents, preservatives, investigate the influence of pH, different formulation methods were screened to achieve good stability. A new microbicide-FB006 gel, contained 1.0% carbomer CP as gel matrix. The pH was adjusted to 5.6 with triethanolamine. Hydroxyl ethyl benzene ( 0.06%) was used as preservatives.The characteristics of gel, values of pH, viscosity, FB006 content were determined. The final gel product with FB006 added was colorless, transparent, uniform with pH value of 5.5-5.7. The viscosity of gel measured was 5500-6500 mPa ? s. The FB006 contents in prepared gels were uniform.The FB006 gel showed no significant changes in the characteristics of gel after 25 days under 25℃.Current study explored the potential use of an HIV entry inhibitor as an active ingredient for microbicide. The study showed that the preparation process was feasible and FB006 was stability under current study conditionsl.