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

作者：Dang Nhung T T; Turner Mark S; Coombes Allan G A^*

来源：Journal of Biomaterials Applications, 2013, 28(1): 74-83.

DOI：10.1177/0885328212437393

• Intra-vaginal devices
• ciprofloxacin
• miconazole
• release kinetics
• antimicrobial activity
• Neisseria gonorrhoea
• Candida albicans

Microporous poly(e-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(e-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 degrees C 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(e-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(e-caprolactone) matrices for delivering antimicrobial agents in the form of an intra-vaginal device.

• 出版日期2013-7