In vitro profiling of the vaginal permeation potential of anti-HIV microbicides and the influence of formulation excipients

► An in vitro strategy to predict the tissue permeation potential of microbicides is described. ► This strategy is based on solubility and permeability profiling of microbicides. ► Tenofovir exhibits the best permeation compared to darunavir, saquinavir and dapivirine. ► Dapivirine permeation can be enhanced by including excipients in HEC-based gels. ► The proposed biopharmaceutical profiling may reduce microbicide failure in vivo.