Multipurpose Prevention Approaches with Antiretroviral-Based Formulations

Antimicrob Agents Chemother. 2015 Nov 23;60(2):1141-4. doi: 10.1128/AAC.02468-15. Print 2016 Feb.

Abstract

We compared the preclinical safety and efficacy of tenofovir (TFV) 1% gel with that of MZC gel [containing 50 μM MIV-150, 14 mM Zn(O2CCH3)2(H2O)2, and 3% carrageenan] through a series of in vitro, ex vivo, and in vivo assays. The two gels showed good antiviral therapeutic indexes (50% cytotoxic concentration/50% effective concentration ratios; range, >25 to 800). MZC showed greater anti-simian-human immunodeficiency virus reverse transcriptase (SHIV-RT) activity than TFV 1% gel in rhesus macaque vaginal explants. MZC protected mice from vaginal herpes simplex virus 2 (HSV-2) challenge (P < 0.0001), but the TFV 1% gel did not.

Publication types

  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Administration, Intravaginal
  • Animals
  • Anti-Retroviral Agents / administration & dosage
  • Anti-Retroviral Agents / pharmacology*
  • Carrageenan / chemistry
  • Drug Combinations
  • Female
  • Gels / administration & dosage
  • Gels / chemistry
  • HIV-1 / drug effects
  • Herpesvirus 2, Human / drug effects
  • Herpesvirus 2, Human / pathogenicity
  • Macaca mulatta
  • Mice, Inbred BALB C
  • Pyridines / pharmacology
  • Simian Acquired Immunodeficiency Syndrome / prevention & control
  • Simian Immunodeficiency Virus / drug effects
  • Tenofovir / pharmacology*
  • Urea / analogs & derivatives
  • Urea / pharmacology
  • Vagina / drug effects
  • Vagina / virology
  • Zinc Acetate / administration & dosage
  • Zinc Acetate / pharmacology*

Substances

  • Anti-Retroviral Agents
  • Drug Combinations
  • Gels
  • MIV 150
  • Pyridines
  • Urea
  • Carrageenan
  • Tenofovir
  • Zinc Acetate