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

The aim of this work was to evaluate the potential of self-assembling poly(ethyleneglycol)(750)-block-poly(epsilon-caprolactone-co-trimethyl-enecarbonate)(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. (c) 2005 Published by Elsevier B.V.