基于β-环糊精的两亲性聚合物包载紫杉醇的研究

Objective：To obtain an amphiphilic polymeric drug delivery system for effective loading of paclitaxel. Method: a series of amphiphilic polymers based on β-CD were synthesized by linking the methoxyl poly (ethylene glycol)-polylactide (mPEL) diblock copolymer to the primary hydroxyl group of β-CD, namely PEL/CDs. The chemical structures of these polymers were characterized by 1H NMR. The particle size of polymeric micelles was determined by dynamic light scattering (DLS). Paclitaxel was loaded into polymers by film dispersion method. The effects of methods on drug loading content (LC) and entrapment efficiency (EE) were investigated through HPLC. Results: PEL/CDs were successfully synthesized, they had different molecular weights and the particle size generally decreased with the growth of the hydrophobic chain. Film dispersion method was used for preparing paclitaxel-loaded micelles which exhibited high drug loading capacity (above 15%) and encapsulation efficiency (above 90%). Sizes of drug-loaded micelles mainly distributed between 100-300nm, and the particle size was roughly reduced with the growth of hydrophobic chain. Conclusion: The amphiphilic polymers based on β-CD exhibited potentials as carriers for anti-cancer drug delivery system, and it is worth in-depth study.