Amphiphilic Block Copolymer And Preparation Method Thereof And Micellar Drug-Loading System Formed By Same With Antitumor Drug

摘要

The present invention relates to a novel amphiphilic block copolymer and the preparation method thereof, as well as a micellar drug-loaded system formed by said copolymer and an anti-tumor drug. Said amphiphilic block copolymer comprises a hydrophilic segment and a hydrophobic segment, and the end group of said hydrophobic segment is end-capped with a hydrophobic group. Methoxypolyethylene glycol (or polyethylene glycol)-polyester block copolymer which has recognized safety is used as a fundamental material of the amphiphilic block copolymer of the present invention, and the terminal hydroxyl group of the polyester segment is modified with a hydrophobic group, whereby the compatibility between the drug molecule and the hydrophobic segments of the block copolymer is improved, and the interaction therebetween is enhanced. Moreover, a larger space for accommodating the drug molecules is provided. Said micelles are more effective in restricting the drug molecules inside the micellar core and preventing the drug from dissolved out of the micelles. Therefore, a drug-loaded micelle with high stability is obtained.

主权项

1. An amphiphilic block copolymer, comprising a hydrophilic segment and a hydrophobic segment; wherein said hydrophilic segment is polyethylene glycol or methoxypolyethylene glycol with the number-average molecular weight in the range of 750 to 5000; said hydrophobic segment is selected from the group consisting of polylactide, polyglycolide, poly(lactic-co-glycolic acid), polycaprolactone, polycarbonate and polydioxanone, each has a number-average molecular weight in the range of 1000 to 50000 and is end-capped with a hydrophobic group, wherein said hydrophobic group is t-butoxycarbonyl phenylalanine.