Influence of long-term stability conditions on microbicidal nucleoside prodrug (WHI-07)-loaded gel-microemulsion

AAPS PharmSciTech. 2006 Sep 1;7(3):73. doi: 10.1208/pt070373.

Abstract

The objective of this study was to evaluate the long-term stability of the antiretroviral spermicide WHI-07 (5-bromo-6-methoxy-5,6-dihydro-3'-azidothymidine-5'-(p-bromophenyl)-methoxyalaninyl phosphate) in a polymer-based microemulsion. The recovery and stability of WHI-07 in gel-microemulsion was examined by a validated high-performance liquid chromatography (HPLC) method. The stability was examined over a period of 24 weeks at 3 controlled temperatures (4 degrees C, 25 degrees C, and 40 degrees C). The recovery of the prodrug from 0.5% to 2.0% WHI-07-loaded gel-microemulsion was 99.8%. HPLC analysis revealed that a 2% WHI-07-loaded gel-microemulsion stored at room temperature and cold temperatures for 24 weeks retained >90% of the prodrug, whereas those stored at 40 degrees C maintained 90% of initial WHI-07 for at least 10 weeks. The observed stability of WHI-07 in gel-microemulsion is of great importance for its widespread utility in various climatological conditions.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Dideoxynucleotides
  • Drug Stability*
  • Emulsions
  • Nucleosides / chemistry
  • Prodrugs / chemistry*
  • Temperature
  • Thymidine Monophosphate / analogs & derivatives*
  • Thymidine Monophosphate / chemistry
  • Zidovudine / analogs & derivatives*
  • Zidovudine / chemistry

Substances

  • 5-bromo-6-methoxy-5, 6-dihydro-3'-azidothymidine-5'-(p-bromophenyl) methoxyalaninyl phosphate
  • Dideoxynucleotides
  • Emulsions
  • Nucleosides
  • Prodrugs
  • Thymidine Monophosphate
  • Zidovudine