Folic Acid Modified Polymeric Micelles for Intravesical Instilled Chemotherapy

作     者：Dan-Hua Zhou Guan Zhang Qing-Song Yu Zhi-Hua Gan 

作者机构：National University of Singapore Environmental Research Institute(NERI)National University of SingaporeSingapore 117576Singapore Beijing Advanced Innovation Center for Soft Matter Science and EngineeringState Key Laboratory of Organic-inorganic Composite MaterialsCollege of Life Science and TechnologyBeijing University of Chemical TechnologyBeijing 100029China Department of UrologyChina-Japan Friendship HospitalBeijing 100029China 

出 版 物：《Chinese Journal of Polymer Science》 (高分子科学（英文版）)

年 卷 期：2018年第36卷第4期

页      面：479-487页

核心收录：

学科分类：081704[工学-应用化学] 07[理学] 08[工学] 070305[理学-高分子化学与物理] 100702[医学-药剂学] 1007[医学-药学(可授医学、理学学位)] 1006[医学-中西医结合] 0817[工学-化学工程与技术] 080501[工学-材料物理与化学] 0805[工学-材料科学与工程（可授工学、理学学位）] 0703[理学-化学] 100602[医学-中西医结合临床] 10[医学] 

基　　金：financially supported by the National Natural Science Foundation of China(Nos.51503013,51390481,and 81472412) the Ministry of Finance and the Ministry of Education of PRC for BUCT 

主　　题：Targeted drug delivery Superficial bladder cancer Intravesical instilled chemotherapy Folic acid Micelles 

摘      要：In this study, a targeting micellar drug delivery system was developed for intravesical instilled chemotherapy of bladder cancer. The amphiphilic diblock copolymer poly（？-caprolactone）-block-poly（ethylene glycol）（PCL-b-PEO） with functional amino group（NH2） at the end of PEO block was synthesized. Then the copolymer was conjugated with folic acid（FA） and fluorescein isothiocyannate（FITC） via the PEO-NH2 terminus, and then assembled into micelles with the target moiety and fluorescence labeling. In addition, drug loaded micelles were also fabricated with anticancer drug doxorubicin（DOX） encapsulated in the hydrophobic core. The micelles were characterized in terms of size, drug loaded efficiency and critical micellization concentration（CMC） by means of DLS, UV and fluorescence spectra. In vitro cellular uptake and cytotoxicity studies showed that FA modified PCL-b-PEO-FA micelles have a greater targeting efficiency to human bladder cancer cell（T-24 cell） compared to PCL-b-PEO-NH2 micelles due to the conjugation of FA on the surface, while no targeting effect to normal tissue originated human embryonic kidney 293（HEK-293） cells was observed, enabling the micelles a promising drug carrier for intravesical instilled chemotherapy of bladder cancer.