Display options
Share it on

Drug Deliv Transl Res. 2012 Dec;2(6):489-97. doi: 10.1007/s13346-012-0101-3.

Development of a UC781 releasing polyethylene vinyl acetate vaginal ring.

Drug delivery and translational research

Christopher McConville, Ian Major, David R Friend, Meredith R Clark, R Karl Malcolm

Affiliations

  1. School of Pharmacy, Medical Biology Centre, Queen's University of Belfast, 97 Lisburn Road, Belfast, BT9 7BL, Northern Ireland, UK, [email protected].

PMID: 25787327 DOI: 10.1007/s13346-012-0101-3

Abstract

UC781 is potent, hydrophobic, non-nucleotide reverse transcriptase inhibitor (NNRTI) against the human immunodeficiency virus (HIV). UC781 is currently being investigated for use as a potential HIV microbicide. A study in rhesus macaques demonstrated that a 100-mg UC781-loaded silicone elastomer vaginal ring released limited amounts of UC781 into the vaginal fluid and tissue after 28 days. The reason for this was due to the hydrophobic nature and limited aqueous solubility of UC781. This study describes the manufacture of UC781-loaded polyethylene vinyl acetate (PEVA) vaginal rings, which have an improved in vitro release rate of UC781 when compared to UC781-loaded silicone elastomer vaginal rings. The study demonstrates that the UC781 in the PEVA rings is mostly in its amorphous form due to the rings being manufactured above UC781's melting point. Furthermore, the rings do not show any signs of UC781 degradation, such as the presence of UC22.

References

  1. J Control Release. 2003 Sep 4;91(3):465-76 - PubMed
  2. J Control Release. 1999 Sep 20;61(3):319-28 - PubMed
  3. Contraception. 2006 Dec;74(6):451-7 - PubMed
  4. Int J Pharm. 2006 Nov 15;325(1-2):82-9 - PubMed
  5. Am J Obstet Gynecol. 1996 Jan;174(1 Pt 1):85-92 - PubMed
  6. AIDS. 2003 Mar 28;17(5):653-61 - PubMed
  7. Eur J Contracept Reprod Health Care. 2008 Mar;13(1):31-8 - PubMed
  8. Eur J Pharm Biopharm. 2000 May;49(3):237-42 - PubMed
  9. Antimicrob Agents Chemother. 2007 May;51(5):1608-15 - PubMed
  10. J Antimicrob Chemother. 2005 Nov;56(5):954-6 - PubMed
  11. J Pharm Sci. 1997 Jan;86(1):1-12 - PubMed
  12. AIDS Res Hum Retroviruses. 1997 Jun 10;13(9):789-96 - PubMed
  13. Drug Deliv Transl Res. 2011 Jun;1(3):247-55 - PubMed
  14. Crit Rev Ther Drug Carrier Syst. 2000;17(5):509-55 - PubMed
  15. AIDS. 1998 Jul 9;12(10):1129-38 - PubMed
  16. Drug Dev Ind Pharm. 2003 Jul;29(6):641-52 - PubMed
  17. Eur J Pharm Biopharm. 2000 Jul;50(1):47-60 - PubMed
  18. J Virol. 1997 Apr;71(4):3023-30 - PubMed
  19. Sex Transm Dis. 2008 Apr;35(4):414-9 - PubMed
  20. Contraception. 2007 Aug;76(2):126-31 - PubMed
  21. Pharm Dev Technol. 1999 May;4(2):241-50 - PubMed

Publication Types