Journal
ADVANCED DRUG DELIVERY REVIEWS
Volume 54, Issue 2, Pages 191-202Publisher
ELSEVIER
DOI: 10.1016/S0169-409X(02)00016-9
Keywords
poly(D,L-lactide)-b-methoxypolyethylene glycol; paclitaxel; micelles
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A number of hypersensitivity reactions have been attributed to the presence of Cremophor(R) EL in the current formulation for paclitaxel. This has led to the development of formulations for paclitaxel employing polyether-polyester diblock copolymers as micelle forming carriers. Diblock copolymers of methoxypolyethylene glycol-block-poly(D,L-lactide) (MePEG:PDLLA) were synthesized from monomers of D,L-lactide and MePEG by a ring opening bulk polymerization in the presence of stannous octoate. Up to 25% paclitaxel could be loaded into matrices of MePEG:PDLLA (60:40, MePEG molecular weight of 2000) using the solution casting method. Dissolution of paclitaxel/copolymer matrices in aqueous media resulted in complete solubilization of paclitaxel within the hydrophobic PDLLA core of the micelles. This review article describes the synthetic reaction conditions influencing the degree of conversion of monomer to copolymer, thermal properties, critical micelle concentrations of copolymers, methods of incorporation of paclitaxel into copolymer matrices and subsequent constitution in aqueous media and biological evaluations of micellar paclitaxel. (C) 2002 Elsevier Science B V All rights reserved.
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