초록 |
Heparin, a water-soluble high sulfated polysaccharide, is well-known for its anticoagulant property. There is also an increasing interest in the development of heparin as anticancer agent due to its multiple antitumor activities. Integrated the anticancer activity of heparin, a multifunctional heparin-based polymeric micelle with folate-mediated tumor targeting and intracellular pH-triggered drug release capacity was designed as anticancer drug carrier. The amphiphilic random-copolymer with heparin as hydrophilic backbone, Folate-Heparin-poly(β-benzyl-L-aspartate), was synthesized for the platform of the micelle. Anticancer drugs, adriamycin, were conjugated to the side chains of the core-forming poly(aspartic acid) block through hydrazone linkage, which can be selectively cleaved under the acidic condition with pH range 5-6, corresponding to the intracellular microenvironment such as the endosomes and lysosomes. The profile of pH dependence drug release was examined in this study. |