title: Preformulation and development of a once-daily sustained-release tenofovir vaginal tablet tablet containing a single excipient.
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.
authors.affiliation: Department 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. Electronic address: c.mcconville@wlv.ac.uk.
authors.forename: Christopher
authors.initials: C
authors.lastname: Mcconville
authors.affiliation: CONRAD, Arlington, Virginia 22209.
authors.forename: David R
authors.initials: DR
authors.lastname: Friend
authors.affiliation: CONRAD, Arlington, Virginia 22209.
authors.forename: Meredith R
authors.initials: MR
authors.lastname: Clark
authors.affiliation: School of Pharmacy, Medical Biology Centre, Queen's University of Belfast, Belfast BT9 7BL, Northern Ireland, UK.
authors.forename: Karl
authors.initials: K
authors.lastname: Malcolm
mesh_terms: D000225:Adenine / Q000008:administration & dosage / Q000031:analogs & derivatives*; D019380:Anti-HIV Agents / Q000008:administration & dosage*; D003692:Delayed-Action Preparations / Q000737:chemistry*; D005079:Excipients / Q000737:chemistry*; D005260:Female; D006244:Hardness; D006801:Humans; D063065:Organophosphonates / Q000008:administration & dosage*; D010316:Particle Size; D011108:Polymers / Q000737:chemistry*; D000068698:Tenofovir; D014622:Vaginal Creams, Foams, and Jellies
chemical_list: D019380:Anti-HIV Agents; D003692:Delayed-Action Preparations; D005079:Excipients; D063065:Organophosphonates; D011108:Polymers; D014622:Vaginal Creams, Foams, and Jellies; D000068698:Tenofovir; D000225:Adenine