Reformulated tenofovir gel for use as a dual compartment microbicide.

The Journal of Antimicrobial Chemotherapy
Charlene S DezzuttiDavid R Friend

Abstract

Coital use of 1% tenofovir gel was shown to be modestly effective at preventing HIV transmission when applied vaginally in the CAPRISA 004 trial. Because the gel is hyperosmolar, which would reduce the integrity of the epithelium and induce fluid movement into the lumen, rectal use may not be acceptable. This study evaluated the pre-clinical safety and efficacy of a reformulated (reduced osmolality) tenofovir gel product. Reduced glycerine (RG)-tenofovir gel was compared with the original tenofovir gel for physiochemical characteristics, product safety and anti-HIV-1 activity. The formulations were similar in all characteristics except for osmolality and spreadability/firmness. The RG-tenofovir gel had a 73% lower osmolality, a 29.6% increase in spreadability and a 27% decrease in firmness as compared with the original tenofovir gel. When applied to epithelial cell monolayers, tenofovir gel showed a transient reduction in the transepithelial resistance while the RG-tenofovir gel did not. Both gels retained ectocervical and colorectal explant viability. However, tenofovir gel treatment resulted in epithelial stripping that was absent after RG-tenofovir gel treatment of the polarized explants. Anti-HIV-1 activity was confirmed by...Continue Reading

Citations

Dec 12, 2012·Current HIV/AIDS Reports·Charlene S Dezzutti, Florian Hladik
Nov 6, 2013·Antiviral Research·Lisa C RohanLin Wang
Jun 4, 2013·Biomaterials·Abhijit A Date, Christopher J Destache
Sep 10, 2013·International Journal of Pharmaceutics·José das NevesBruno Sarmento
Sep 13, 2012·AIDS Research and Human Retroviruses·Patrick F KiserBetsy C Herold
Oct 4, 2012·Current Opinion in HIV and AIDS·Ian McGowan
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Sep 24, 2014·Pharmaceutics·Ana Raquel CunhaRita Palmeira-de-Oliveira
Nov 26, 2013·Expert Opinion on Drug Delivery·Ian McGowan
Jan 28, 2014·Journal of Pharmaceutical Sciences·Ahmed S Zidan, Muhammad J Habib
Sep 18, 2014·Journal of Controlled Release : Official Journal of the Controlled Release Society·Rute NunesJosé das Neves
Mar 26, 2014·Journal of Clinical Pharmacology·Mackenzie L Cottrell, Angela D M Kashuba
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Feb 17, 2015·Advanced Drug Delivery Reviews·Carla M CaramellaGiuseppina Sandri
Dec 30, 2014·Advanced Drug Delivery Reviews·José A Fernández-RomeroMelissa Robbiani
May 23, 2015·Contraception·Lindsay F KramzerLisa C Rohan
May 6, 2015·Journal of Controlled Release : Official Journal of the Controlled Release Society·Katharina MaiselJustin Hanes
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Nov 5, 2015·Journal of the International AIDS Society·Charlene S Dezzutti
Jul 13, 2016·Antimicrobial Agents and Chemotherapy·Lisa M NoguchiRichard H Beigi
Sep 11, 2018·Clinical Pharmacology and Therapeutics·Craig W Hendrix
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Jan 17, 2019·The Journal of Antimicrobial Chemotherapy·Fabian Yuh Shiong KongJane S Hocking
Oct 7, 2017·Journal of Pharmaceutical Innovation·Tiantian GongLisa C Rohan

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