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

  1. Kavita M. Gupta1,
  2. Serena M. Pearce1,
  3. Azadeh E. Poursaid1,
  4. Hyder A. Aliyar1,
  5. Patrick A. Tresco1,
  6. Mark A. Mitchnik2,
  7. Patrick F. Kiser1,3,*

Article first published online: 13 MAR 2008

DOI: 10.1002/jps.21331

Issue

Journal of Pharmaceutical Sciences

Journal of Pharmaceutical Sciences

Volume 97, Issue 10, pages 4228–4239, October 2008

Additional Information

How to Cite

Gupta, K. M., Pearce, S. M., Poursaid, A. E., Aliyar, H. A., Tresco, P. A., Mitchnik, M. A. and Kiser, P. F. (2008), Polyurethane intravaginal ring for controlled delivery of dapivirine, a nonnucleoside reverse transcriptase inhibitor of HIV-1. Journal of Pharmaceutical Sciences, 97: 4228–4239. doi: 10.1002/jps.21331

Author Information

  1. 1

    Department of Bioengineering, University of Utah, Salt Lake City, Utah

  2. 2

    Particle Sciences Inc., Bethlehem, Pennsylvania

  3. 3

    Department of Pharmaceutics and Pharmaceutical Chemistry, University of Utah, Salt Lake City, Utah

*Department of Bioengineering, University of Utah, Salt Lake City, Utah. Telephone: +1-801-587-3681; Fax: +1-801-581-8966.

Publication History

  1. Issue published online: 28 AUG 2008
  2. Article first published online: 13 MAR 2008
  3. Manuscript Accepted: 21 NOV 2007
  4. Manuscript Revised: 5 OCT 2007
  5. Manuscript Received: 17 JUN 2007

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Keywords:

  • intravaginal ring;
  • long duration microbicide;
  • dapivirine;
  • nonnucleoside reverse transcriptase inhibitor;
  • controlled delivery;
  • formulation vehicle;
  • diffusion;
  • polymeric drug carrier;
  • release kinetics

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. © 2008 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 97:4228–4239, 2008

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