AAPS PharmSciTech

, 7:E135

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

Article

DOI: 10.1208/pt070373

Cite this article as:
D’Cruz, O.J. & Uckun, F.M. AAPS PharmSciTech (2006) 7: E135. 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 gelmicroemulsion 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°C, 25°C, and 40°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°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.

Keywords

Gel-microemulsion prodrug stability WHI-07 

Copyright information

© American Association of Pharmaceutical Scientists 2006

Authors and Affiliations

  1. 1.Drug Discovery ProgramParker Hughes InstituteSt Paul
  2. 2.Paradigm PharmaceuticalsLLCSt. Paul