Comparative safety evaluation of the candidate vaginal microbicide C31G

Antimicrob Agents Chemother. 2005 Apr;49(4):1509-20. doi: 10.1128/AAC.49.4.1509-1520.2005.

Abstract

C31G is currently the focus of clinical trials designed to evaluate this agent as a microbicidal and spermicidal agent. In the following studies, the in vivo safety of C31G was assessed with a Swiss Webster mouse model of cervicovaginal toxicity and correlated with results from in vitro cytotoxicity experiments and published clinical observations. A single exposure of unformulated 1% C31G resulted in mild-to-moderate epithelial disruption and inflammation at 2 and 4 h postapplication. The columnar epithelium of the cervix was the primary site of damage, while no perturbation of the vaginal mucosa was observed. In contrast, application of unformulated 1.7% C31G resulted in greater levels of inflammation in the cervical epithelium at 2 h postapplication and severe epithelial disruption that persisted to 8 h postapplication. Application of a nonionic aqueous gel formulation containing 1% C31G resulted in no apparent cervicovaginal toxicity at any time point evaluated. However, formulation of 1.7% C31G did not substantially reduce the toxicity associated with unformulated C31G at that concentration. These observations correlate with findings gathered during a recent clinical trial, in which once-daily applications resulted in no adverse events in women receiving the formulation containing 1% C31G, compared to moderate-to-severe adverse events in 30% of women receiving the 1.7% C31G formulation. The Swiss Webster mouse model was able to effectively discriminate between concentrations and formulations of C31G that produced distinct clinical effects in human trials. The Swiss Webster animal model may be a highly valuable tool for preclinical evaluation of candidate vaginal microbicides.

Publication types

  • Comparative Study
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Administration, Intravaginal
  • Animals
  • Anti-Infective Agents, Local
  • Betaine / administration & dosage
  • Betaine / adverse effects*
  • Betaine / analogs & derivatives*
  • Betaine / toxicity
  • Cell Line
  • Cervix Uteri / cytology
  • Cervix Uteri / drug effects*
  • Fatty Acids, Unsaturated / administration & dosage
  • Fatty Acids, Unsaturated / adverse effects*
  • Fatty Acids, Unsaturated / toxicity
  • Female
  • HeLa Cells
  • Humans
  • Mice
  • Nonoxynol / administration & dosage
  • Nonoxynol / adverse effects*
  • Nonoxynol / toxicity
  • Vagina / cytology
  • Vagina / drug effects*
  • Vaginal Creams, Foams, and Jellies / administration & dosage
  • Vaginal Creams, Foams, and Jellies / adverse effects
  • Vaginal Creams, Foams, and Jellies / toxicity

Substances

  • Anti-Infective Agents, Local
  • Fatty Acids, Unsaturated
  • Vaginal Creams, Foams, and Jellies
  • Nonoxynol
  • Betaine
  • C 31G