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J Pharm Sci. 2018 Oct;107(10):2601-2610. doi: 10.1016/j.xphs.2018.06.002. Epub 2018 Jun 11.

Development of a Vaginal Fast-Dissolving Insert Combining Griffithsin and Carrageenan for Potential Use Against Sexually Transmitted Infections.

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PATH, PO Box 900922, Seattle, Washington 98109. Electronic address:
PATH, PO Box 900922, Seattle, Washington 98109.
Population Council, Center for Biomedical Research, New York, New York 10065.
Population Council, Center for Biomedical Research, New York, New York 10065; The City University of New York, Borough of Manhattan Community College, Science Department, New York, New York 10007.


Precoital, on-demand topical microbicides to reduce a woman's risk of sexually transmitted infections have been in development for nearly 3 decades, but no product has been approved due to acceptability issues and poor adherence in clinical trials. We set out to develop a self-administered vaginal fast-dissolving insert (FDI) produced by freeze-drying that would deliver safe and effective amounts of the antiviral agents griffithsin (GRFT) and carrageenan (CG) and would have properties women and their partners find acceptable. We evaluated FDI physical criteria, attributes of the gel produced upon dissolving, and GRFT stability. The lead formulation, FDI-024, was selected from 13 candidates and contains 4 mg of GRFT, 15 mg of CG, and excipients (the cryoprotectant sucrose and bulking agents dextran 40 and mannitol). The FDI exhibits good friability and hardness and is stable for at least 6 months at up to 40°C/75% relative humidity. It disintegrates in less than 60 s in a physiologically relevant volume (∼1 mL) of simulated vaginal fluid, forming a viscous semi-solid gel with favorable mucoadhesive and spreading properties. The formulation retains the antiviral activity of GRFT and CG against HIV type 1 and human papillomavirus, respectively, in cell-based assays.


formulation; freeze-drying/lyophilization; mucosal drug delivery; protein delivery; solid dosage form; solid state stability; stabilization

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