Polyurethane intravaginal ring for controlled delivery of dapivirine, a nonnucleoside reverse transcriptase inhibitor of HIV-1

Kavita M. Gupta, Serena M. Pearce, Azadeh E. Poursaid, Hyder A. Aliyar, Patrick A. Tresco, Mark A. Mitchnik, Patrick F. Kiser

Research output: Contribution to journalArticlepeer-review

88 Scopus citations

Abstract

Women-controlled methods for prevention of male-to-female sexual transmission of HIV-1 are urgently needed. Providing inhibitory concentrations of HIV-1 reverse transcriptase inhibitors to impede the replication of the virus in the female genital tissue offers a mechanism for prophylaxis of HIV-1. To this end, an intravaginal ring device that can provide long duration delivery of dapivirine, a nonnucleoside reverse transcriptase inhibitor of HIV-1, was developed utilizing a medical-grade polyether urethane. Monolithic intravaginal rings were fabricated and sustained release with cumulative flux linear with time was demonstrated under sink conditions for a period of 30 days. The release rate was directly proportional to the amount of drug loaded. Another release study conducted for a week utilizing liposome dispersions as sink conditions, to mimic the partitioning of dapivirine into vaginal tissue, also demonstrated release rates constant with time. These results qualify polyether urethanes for development of intravaginal rings for sustained delivery of microbicidal agents.

Original languageEnglish (US)
Pages (from-to)4228-4239
Number of pages12
JournalJournal of Pharmaceutical Sciences
Volume97
Issue number10
DOIs
StatePublished - Oct 2008

Keywords

  • Controlled delivery
  • Dapivirine
  • Diffusion
  • Formulation vehicle
  • Intravaginal ring
  • Long duration microbicide
  • Nonnucleoside reverse transcriptase inhibitor
  • Polymeric drug carrier
  • Release kinetics

ASJC Scopus subject areas

  • Pharmaceutical Science

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