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Updated: May 12, 2026

Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors
Published on: May 9, 2025
Preformulation and development of a once-daily sustained-release tenofovir vaginal tablet tablet containing a single
Christopher Mcconville1, David R Friend2, Meredith R Clark2
1Department of Pharmacy, School of Applied Sciences, University of Wolverhampton, Wolverhampton WV1 1LY, UK; School of Pharmacy, Medical Biology Centre, Queen's University of Belfast, Belfast BT9 7BL, Northern Ireland, UK.
Abstract:
Tenofovir is a nucleoside reverse-transcriptase inhibitor that is currently being investigated as a potential HIV microbicide candidate, with a recent phase IIb study of a 1% (w/w) tenofovir gel reducing HIV acquisition by 39% in sexually active women. However, not only does a HIV microbicidal product need to be safe and effective, it also needs to be cheap and easy to manufacture. In this study, we report the development of a tenofovir-loaded tablet, manufactured using a single sustained-release polymer, which has an acceptable hardness, friability and tenofovir release rate. Furthermore, by varying both the type and molecular weight of the sustained-release polymer, as well as the particle size of both tenofovir and the sustained-release polymer, we can vary the release rate of tenofovir from the tablets.
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