Development of intra-vaginal matrices from polycaprolactone for sustained release of antimicrobial agents.
Microporous poly(ε-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(ε-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(ε-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(ε-caprolactone) matrices for delivering antimicrobial agents in the form of an intra-vaginal device.
Pharmacy Australia Centre of Excellence, The University of Queensland, 20 Cornwall Street, Wooloongabba, QLD, Australia.
Nhung T T
NT
Dang
Mark S
MS
Turner
Allan G A
AG
Coombes
D000282:Administration, Intravaginal; D000890:Anti-Infective Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics; D001672:Biocompatible Materials / Q000008:administration & dosage / Q000737:chemistry; D002939:Ciprofloxacin / Q000008:administration & dosage / Q000493:pharmacokinetics; D003692:Delayed-Action Preparations; D016503:Drug Delivery Systems; D005260:Female; D006801:Humans; D008422:Materials Testing; D008825:Miconazole / Q000008:administration & dosage / Q000493:pharmacokinetics; D008855:Microscopy, Electron, Scanning; D011091:Polyesters / Q000737:chemistry*; D012749:Sexually Transmitted Diseases / Q000188:drug therapy / Q000517:prevention & control
D000890:Anti-Infective Agents; D001672:Biocompatible Materials; D003692:Delayed-Action Preparations; D011091:Polyesters; C016240:polycaprolactone; D002939:Ciprofloxacin; D008825:Miconazole