title: Targeted sustained delivery of antineoplastic agent with multicomponent polylactide stereocomplex micelle.
abstract: A c(RGDfC)-decorated polylactide stereocomplex micelle (cRGD-SCM) was prepared through the stereocomplex and hydrophobic interactions among 4-arm poly(ethylene glycol)-block-poly(D-lactide) (4-arm PEG-b-PDLA), methoxy poly(ethylene glycol)-block-poly(L-lactide) (mPEG-b-PLLA), and c(RGDfC)-poly(ethylene glycol)-block-poly(L-lactide) (cRGD-PEG-b-PLLA) for targeted treatment of αvβ3integrin-positive C26 colon cancer. Doxorubicin (DOX), a model antitumor drug, was loaded into cRGD-SCM with a diameter of approximately 100nm, and the drug loading efficiency was 45.9wt.%. cRGD-SCM/DOX with a sustained release pattern exhibited prolonged circulation time, upregulated accumulation in tumor, enhanced tumor inhibition, and decreased side effects compared with free DOX and non-targeting SCM/DOX in vivo. More interestingly, the targeting ligand in the terminal of PEG can be easily replaced with other targeting groups according to the different types of malignancies. Therefore, the cRGD-decorated platform might be a promising targeted drug delivery system for personal chemotherapy clinically.
authors.affiliation: Jilin University, Changchun, PR China; Key Laboratory of Polymer Ecomaterials, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun, PR China.
authors.forename: Kexin
authors.initials: K
authors.lastname: Shen
authors.affiliation: Key Laboratory of Polymer Ecomaterials, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun, PR China.
authors.forename: Di
authors.initials: D
authors.lastname: Li
authors.affiliation: Jilin University, Changchun, PR China.
authors.forename: Jingjing
authors.initials: J
authors.lastname: Guan
authors.affiliation: Key Laboratory of Polymer Ecomaterials, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun, PR China. Electronic address: jxding@ciac.ac.cn.
authors.forename: Jianxun
authors.initials: J
authors.lastname: Ding
authors.affiliation: Department of Radiation Oncology, Shandong Cancer Hospital Affiliated to Shandong University, Shandong Academy of Medical Sciences, Jinan, PR China. Electronic address: zhongtangw@163.com.
authors.forename: Zhongtang
authors.initials: Z
authors.lastname: Wang
authors.affiliation: Jilin University, Changchun, PR China.
authors.forename: Jingkai
authors.initials: J
authors.lastname: Gu
authors.affiliation: Jilin University, Changchun, PR China. Electronic address: tongjunliu@163.com.
authors.forename: Tongjun
authors.initials: T
authors.lastname: Liu
authors.affiliation: Key Laboratory of Polymer Ecomaterials, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun, PR China.
authors.forename: Xuesi
authors.initials: X
authors.lastname: Chen
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D045744:Cell Line, Tumor; D003106:Colon / Q000187:drug effects* / Q000473:pathology; D003110:Colonic Neoplasms / Q000188:drug therapy* / Q000473:pathology; D003692:Delayed-Action Preparations / Q000737:chemistry*; D004317:Doxorubicin / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D016503:Drug Delivery Systems; D051379:Mice; D008807:Mice, Inbred BALB C; D008823:Micelles; D010456:Peptides, Cyclic / Q000737:chemistry*; D011091:Polyesters / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D003692:Delayed-Action Preparations; D008823:Micelles; D010456:Peptides, Cyclic; D011091:Polyesters; C507169:cyclic arginine-glycine-aspartic acid peptide; C033616:poly(lactide); D004317:Doxorubicin
keywords: Chemotherapy; Multicomponent micelle; Polylactide; Stereocomplex interaction; Targetability