Preformulation and development of a once-daily sustained-release tenofovir vaginal tablet tablet containing a single excipient

J Pharm Sci. 2013 Jun;102(6):1859-1868. doi: 10.1002/jps.23528. Epub 2013 Apr 9.


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.

MeSH terms

  • Adenine / administration & dosage
  • Adenine / analogs & derivatives*
  • Anti-HIV Agents / administration & dosage*
  • Delayed-Action Preparations / chemistry*
  • Excipients / chemistry*
  • Female
  • Hardness
  • Humans
  • Organophosphonates / administration & dosage*
  • Particle Size
  • Polymers / chemistry*
  • Tenofovir
  • Vaginal Creams, Foams, and Jellies


  • Anti-HIV Agents
  • Delayed-Action Preparations
  • Excipients
  • Organophosphonates
  • Polymers
  • Vaginal Creams, Foams, and Jellies
  • Tenofovir
  • Adenine