Encapsulation of amphotericin B in poly(ethylene glycol)-block-poly(ɛ-caprolactone- co-trimethylenecarbonate) polymeric micelles

• Published in: International journal of pharmaceutics Vol. 309; no. 1; pp. 234 - 240
• Main Authors: Vandermeulen, G., Rouxhet, L., Arien, A., Brewster, M.E., Préat, V.
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier B.V 17.02.2006; Elsevier
• Subjects: Amphotericin B; Amphotericin B - chemistry; Amphotericin B - pharmacology; Animals; Antifungal Agents - chemistry; Antifungal Agents - pharmacology; Biological and medical sciences; Candida albicans - drug effects; Candida albicans - growth & development; Drug Compounding; General pharmacology; Hemolysis - drug effects; Lactones - chemistry; Medical sciences; Micelles; Microbial Sensitivity Tests; mmePEG750-block-poly(ɛ-caprolactone- co-trimethylenecarbonate); Particle Size; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Polyesters; Polyethylene Glycols - chemistry; Polymeric micelles; Polymers - chemistry; Rats; Solubility; Water - chemistry; Amphotericin B; mmePEG750-block-poly(ɛ-caprolactone- co-trimethylenecarbonate); Polymeric micelles; Encapsulation; Pharmaceutical technology; Control release polymer; Micelle; Ethylene oxide polymer; Antiprotozoal agent; Antibiotic; Antifungal agent; Polyenic compound; Parasiticide; mmePEG750-block-poly(e-caprolactone-co-trimethylenecarbonate); Polycaprolactone
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2005.11.031

The aim of this work was to evaluate the potential of self-assembling poly(ethyleneglycol) 750-block-poly(ɛ-caprolactone- co-trimethylenecarbonate) 4500 50/50 copolymers (PEG-p(CL- co-TMC)) to solubilize amphotericin B in polymeric micelles and to disaggregate the drug to the less toxic monomeric form. Amphotericin B was encapsulated in the micelles upon dilution of a mixture of the liquid polymer and the drug in water. Its solubility was increased by two orders of magnitude depending on polymer concentration. The aggregation state of amphotericin B was decreased by PEG-p(CL- co-TMC). The preparation method and the loading of the polymeric micelles influenced it. The antifungal activity of the drug was reduced by encapsulation in the polymeric micelles whereas the onset of amphotericin B-induced hemolysis was delayed. PEG-p(CL- co-TMC) micelles could be an easy method for amphotericin B encapsulation.