title: The synthesis and application of heparin-based smart drug carrier.
abstract: Heparin based polymer drug which could self-assemble into sphere micelle in water was firstly prepared by grafting paclitaxel (PTX) into the hydroxyl of heparin via aconitic bond as pH sensitive spacer. Positive charged drug DOX·HCl and cationic folic acid (CFA) can be further loaded into the polymer drug via electrostatic interaction in aqueous solution so as to prepare smart drug carrier. The drug carrier was able to release more PTX and DOX at pH 4.8 than that at pH 7.4, exhibiting pH sensitivity for two drugs. Furthermore, tumor cell cytotoxicity test proved it possessed significant cytotoxicity against tumor cells MDA-MB-231 as well as its active tumor targeting ability resulting from the loading of CFA. Cellular uptake and intracellular distribution were further revealed by confocal laser scanning microscopy (CLSM). In conclusion, this paper not only provided a simple strategy but also indicated heparin is a versatile platform for the design of smart drug carrier. The as-prepared drug carrier also showed promising potential in chemotherapy.
authors.affiliation: School of Materials Science and Engineering, Beijing Institute of Technology, Beijing 100081, China.
authors.forename: Qingxuan
authors.initials: Q
authors.lastname: Li
authors.affiliation: School of Materials Science and Engineering, Beijing Institute of Technology, Beijing 100081, China.
authors.forename: Lu
authors.initials: L
authors.lastname: Gan
authors.affiliation: School of Chemical Engineering and Environment, Beijing Institute of Technology, Beijing 100081, China.
authors.forename: Hong
authors.initials: H
authors.lastname: Tao
authors.affiliation: School of Materials Science and Engineering, Beijing Institute of Technology, Beijing 100081, China.
authors.forename: Qian
authors.initials: Q
authors.lastname: Wang
authors.affiliation: School of Materials Science and Engineering, Beijing Institute of Technology, Beijing 100081, China. Electronic address: yelin@bit.edu.cn.
authors.forename: Lin
authors.initials: L
authors.lastname: Ye
authors.affiliation: School of Materials Science and Engineering, Beijing Institute of Technology, Beijing 100081, China.
authors.forename: Aiying
authors.initials: A
authors.lastname: Zhang
authors.affiliation: School of Materials Science and Engineering, Beijing Institute of Technology, Beijing 100081, China.
authors.forename: Zengguo
authors.initials: Z
authors.lastname: Feng
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D001692:Biological Transport; D045744:Cell Line, Tumor; D060326:Chemistry Techniques, Synthetic; D004337:Drug Carriers / Q000138:chemical synthesis* / Q000737:chemistry*; D065546:Drug Liberation; D005492:Folic Acid / Q000737:chemistry; D006493:Heparin / Q000138:chemical synthesis* / Q000737:chemistry*; D006801:Humans; D017239:Paclitaxel / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D006493:Heparin; D005492:Folic Acid; D017239:Paclitaxel
keywords: Drug carrier; Heparin; Polymer drug; Tumor targeting ability; pH sensitivity