Sustained ex vivo skin antiseptic activity of chlorhexidine in poly(ϵ-caprolactone) nanocapsule encapsulated form and as a digluconate

• Published in: Journal of controlled release 2002-08, Vol.82 (2), p.319-334
• Main Authors: Lboutounne, Hassan, Chaulet, Jean-François, Ploton, Christine, Falson, Françoise, Pirot, Fabrice
• Format: Article
• Language: English
• Subjects: Animals; Anti-Infective Agents, Local - chemistry; Anti-Infective Agents, Local - pharmacokinetics; Anti-Infective Agents, Local - pharmacology; Anti-Infective Agents, Local - therapeutic use; Antibiotics. Antiinfectious agents. Antiparasitic agents; Antiseptics; Biological and medical sciences; Chlorhexidine; Chlorhexidine - analogs & derivatives; Chlorhexidine - chemistry; Chlorhexidine - pharmacokinetics; Chlorhexidine - pharmacology; Chlorhexidine - therapeutic use; Delayed-Action Preparations; Drug Compounding; Ear; General pharmacology; Gram-Negative Bacteria - drug effects; Gram-Positive Cocci - drug effects; Medical sciences; Microbial Sensitivity Tests; Microscopy, Electron; Microscopy, Electron, Scanning; Nanocapsules; Nanotechnology; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Polyesters - chemistry; Porcine ear skin; Skin Absorption; Staphylococcal Skin Infections - drug therapy; Staphylococcus epidermidis; Staphylococcus epidermidis - drug effects; Stratum corneum, Tape-stripping; Swine
• ISSN: 0168-3659; 1873-4995
• DOI: 10.1016/S0168-3659(02)00142-6

In this work, the sustained bactericidal activity of chlorhexidine base loaded poly(ϵ-caprolactone), PCL, nanocapsules against Staphylococcus epidermidis inoculated onto porcine ear skin was investigated. Drug loaded nanocapsules were prepared by the interfacial polymer deposition following solvent displacement method, then characterized by photon correlation spectroscopy, electrophoretic measurements, transmission and scanning electron microscopy. Antimicrobial activity of these colloidal carriers was evaluated (i) in vitro against eight strains of bacteria, and (ii) ex vivo against Staphylococcus epidermidis inoculated for 12 h onto porcine ear skin surface treated for 3 min either with 0.6% chlorhexidine base loaded or unloaded nanocapsules suspended in hydrogel, or 1% chlorhexidine digluconate aqueous solution. Chlorhexidine absorption into the stratum corneum (SC) was evaluated by the tape-stripping method. The results showed that chlorhexidine nanocapsules in aqueous suspension having a 200–300 nm size and a positive charge exhibited similar minimum inhibitory concentrations against several bacteria with chlorhexidine digluconate aqueous solution. Ex vivo, there was a significant reduction in the number of colony forming units (CFUs) from 3-min treated skin with chlorhexidine nanocapsule suspension (5 to