作者： Yang Yang, Ying-Ming Zhang, Yong Chen, Jia-Tong Chen & Yu Liu

1Department of Chemistry, State Key Laboratory of Elemento-Organic Chemistry, Nankai University, Tianjin,300071, P. R. China. 

2Collaborative Innovation Center of Chemical Science and Engineering (Tianjin), Nankai University, Tianjin, 300071, P. R. China. 

3School of Chemical Engineering and Technology, Hebei University of Technology, Tianjin, 300130, P. R. China. 

4Department of Biochemistry and Molecular Biology, College of Life Sciences, Nankai University, Tianjin, 300071, P. R. China. 

 

摘要：The construction of synthetic straightforward, biocompatible and biodegradable targeted drug delivery system with fluorescent tracking abilities, high anticancer activities and low side effects is still a challenge in the field of biochemistry and material chemistry. In this work, we constructed targeted paclitaxel (Taxol) delivery nanoparticles composed of permethyl-β-cyclodextrin modified hyaluronic acid (HApCD) and porphyrin modified paclitaxel prodrug (PorTaxol), through host-guest and amphiphilic interactions. The obtained nanoparticles (HATXP) were biocompatible and enzymatic biodegradable due to their hydrophilic hyaluronic acid (HA) shell and hydrophobic Taxol core, and exhibited specific targeting internalization into cancer cells via HA receptor mediated endocytosis effects. The cytotoxicity experiments showed that the HATXP exhibited similar anticancer activities to, but much lower side effects than commercial anticancer drug Taxol. The present work would provide a platform for targeted paclitaxel drug delivery and a general protocol for the design of advanced multifunctional nanoscale biomaterials for targeted drug/gene delivery.