title: Encapsulation of amphotericin B in poly(ethylene glycol)-block-poly(epsilon-caprolactone-co-trimethylenecarbonate) polymeric micelles.
abstract: The aim of this work was to evaluate the potential of self-assembling poly(ethyleneglycol)(750)-block-poly(epsilon-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.
authors.affiliation: Université catholique de Louvain, Unité de pharmacie galénique, Avenue Mounier, 73 UCL 7320, 1200 Brussels, Belgium.
authors.forename: G
authors.initials: G
authors.lastname: Vandermeulen
authors.forename: L
authors.initials: L
authors.lastname: Rouxhet
authors.forename: A
authors.initials: A
authors.lastname: Arien
authors.forename: M E
authors.initials: ME
authors.lastname: Brewster
authors.forename: V
authors.initials: V
authors.lastname: Préat
mesh_terms: D000666:Amphotericin B / Q000737:chemistry* / Q000494:pharmacology; D000818:Animals; D000935:Antifungal Agents / Q000737:chemistry* / Q000494:pharmacology; D002176:Candida albicans / Q000187:drug effects / Q000254:growth & development; D004339:Drug Compounding; D006461:Hemolysis / Q000187:drug effects; D007783:Lactones / Q000737:chemistry*; D008823:Micelles; D008826:Microbial Sensitivity Tests; D010316:Particle Size; D011091:Polyesters; D011092:Polyethylene Glycols / Q000737:chemistry*; D011108:Polymers / Q000737:chemistry*; D051381:Rats; D012995:Solubility; D014867:Water / Q000737:chemistry
chemical_list: D000935:Antifungal Agents; D007783:Lactones; D008823:Micelles; D011091:Polyesters; D011108:Polymers; C410438:TMC-ECL copolymer; D014867:Water; D011092:Polyethylene Glycols; D000666:Amphotericin B