1: Int J Pharm. 2006 Feb 17;309(1-2):234-40. Epub 2006 Jan 6. 

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

Vandermeulen G, Rouxhet L, Arien A, Brewster ME, Preat V.

Universite catholique de Louvain, Unite de pharmacie galenique, Avenue Mounier,
73 UCL 7320, 1200 Brussels, Belgium.

The aim of this work was to evaluate the potential of self-assembling
poly(ethyleneglycol)(750)-block-poly(epsilon-caprolactone-co-trimethylenecarbona
te)(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.

PMID: 16406402 [PubMed - in process]