title: Folate-functionalized polymeric micelles based on biodegradable PEG-PDLLA as a hepatic carcinoma-targeting delivery system.
abstract: Targeted delivery of anti-cancer drugs is a highly desirable strategy to improve therapeutic outcome because of the combination of enhanced efficacy and reduced toxicity. In this study, the anti-cancer drug doxorubicin (DOX) was accommodated in the cores of polymeric micelles self-assembled from amphiphilic block copolymers of poly(ethylene glycol)(PEGs) and poly(D,L-lactide) (PDLLA) with a targeting ligand (folate) attached to the distal ends of the PEG (Folate-PEG-PDLLA). In vitro tumor cell targeting efficacy was evaluated upon observing cellular uptake of these micelles by human hepatic carcinoma cells (Bel 7402 cells) overexpressing surface receptors for folate. In control release tests, DOX behavior of controlled release in folate receptor-mediated micellar folate-PEG-PDLLA-DOX-micelles was obvious, with pH sensitivity. Bel 7402 cells showed micelles to have low toxicity and suggested potential therapeustic application as a multifunctional platform for tumor management.
authors.affiliation: Department of Radiology, Fifth Affiliated Hospital, Sun Yat-Sen Memorial Hospital, China.
authors.forename: Chuanqiang
authors.initials: C
authors.lastname: Niu
authors.forename: Qiquan
authors.initials: Q
authors.lastname: Sun
authors.forename: Jingxing
authors.initials: J
authors.lastname: Zhou
authors.forename: Du
authors.initials: D
authors.lastname: Cheng
authors.forename: Guobin
authors.initials: G
authors.lastname: Hong
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry; D006528:Carcinoma, Hepatocellular / Q000188:drug therapy* / Q000378:metabolism; D045744:Cell Line, Tumor; D004317:Doxorubicin / Q000008:administration & dosage / Q000737:chemistry; D004337:Drug Carriers / Q000008:administration & dosage* / Q000737:chemistry; D016503:Drug Delivery Systems / Q000379:methods; D005492:Folic Acid / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism; D006801:Humans; D006863:Hydrogen-Ion Concentration; D008024:Ligands; D008113:Liver Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D008823:Micelles; D011091:Polyesters / Q000008:administration & dosage* / Q000737:chemistry; D011092:Polyethylene Glycols / Q000008:administration & dosage* / Q000737:chemistry; D011956:Receptors, Cell Surface / Q000378:metabolism
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D008024:Ligands; D008823:Micelles; D011091:Polyesters; D011956:Receptors, Cell Surface; D011092:Polyethylene Glycols; C033616:poly(lactide); D004317:Doxorubicin; D005492:Folic Acid