Aqueous Solubilization of Paclitaxel Using Hydrotropic Polymer Micelle

摘要

Hydrotropic block copolymers, consisting of a hydrophilic poly(ethylene glycol) (PEG) block and a hydrotropic polymer, poly(2-(4-(vinyl benzyloxy)-N, N-diethylnicotinamide)) [P(VBODENA)], block, were synthesized by atom transfer radical polymerization (ATRP) for aqueous solubiiization of paclitaxel, a representative poorly water-soluble drug. These polymers showed an excellent solubilizing effect for paclitaxel in aqueous media in comparison with the corresponding hydrotropic agent and a control micelle (PEG-PLA) and such effect was significantly dependent on the polymer concentration and composition. Paclitaxel could be solubilized into polymer micelles in aqueous media without use of an organic solvent. Due to their promising properties such as micellar characteristics and hydrotropic solubilization, the hydrotropic polymer micelle system can be useful for formulation of paclitaxel and other poorly soluble drugs.