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.
McConville, C., Friend, D. R., Clark, M. R., & Malcolm, K. (2013). Preformulation and Development of a Once-Daily Sustained-Release Tenofovir Vaginal Tablet Tablet Containing A Single Excipient. Journal of Pharmaceutical Sciences, 102(6), 1859-1868. https://doi.org/10.1002/jps.23528