Development of intra-vaginal matrices from polycaprolactone for sustained release of antimicrobial agents

Abstract

Microporous poly(ɛ-caprolactone) matrices were loaded with an antibacterial agent, ciprofloxacin and an antifungal agent, miconazole nitrate, respectively, for investigations of their potential as controlled vaginal delivery devices. Ciprofloxacin loadings up to 15% w/w could be obtained by increasing the drug content of the poly(ɛ-caprolactone) solution, while the actual loadings of miconazole were much lower (1–3% w/w) due to drug partition into methanol during the solvent extraction. The kinetics of ciprofloxacin release in simulated vaginal fluid at 37℃ were characterised by a small burst release phase in the first 24 h, low drug release up to 7 days (10%) and gradual release of up to 80% of the drug content by day 30. Meanwhile, the release kinetics of miconazole-loaded matrices could be effectively described by the Higuchi model with 100% drug release from the highest loaded matrices (3.2% w/w) in 13 days. Ciprofloxacin or miconazole released over 30 and 13 days, respectively, from poly(ɛ-caprolactone) matrices into simulated vaginal fluid retained high levels of antimicrobial activity in excess of 80% of the activity of the free drug. This study confirms the potential of poly(ɛ-caprolactone) matrices for delivering antimicrobial agents in the form of an intra-vaginal device.