title: Doxorubicin-Loaded Micelles Based on Folic Acid Conjugated pH-Dependent Thermo-Sensitive Copolymer: In Vitro and In Vivo Evaluation.
abstract: In this paper, the doxorubicin (DOX)-loaded micelles were prepared based on a novel folic acid conjugated pH-dependent thermo-sensitive copolymer poly(D,L-lactic acid)-b-poly(N-isopropyl methacrylamide-co-N-isopropylmaelic acid-co-10-undecenoic acid) (PLA-PNNUA-FA) constructed to provide an active targeting drug delivery and triggered drug release system. The micelles were able to target tumors through the interaction between folic acid and its receptors which are overexpressed on the tumor cell membrane, and achieved pH-dependent thermo induced drug release in the intracellular mild acidic media such as endosomes and lysosomes after the micelles enter the cells. The results of cell assays and animal experiments showed that the micelles exhibited obvious tumor penetration efficiency in vivo, also improved DOX cell uptake and cytotoxicity in vitro. It was suggested that copolymer PLA-PNNUA-FA might be a potential targeted drug carrier to deliver chemotherapeutic drugs achieving better efficacy of chemotherapy.
authors.forename: Hongli
authors.initials: H
authors.lastname: Zhao
authors.forename: Liang
authors.initials: L
authors.lastname: Tao
authors.forename: Ronghua
authors.initials: R
authors.lastname: Yu
authors.forename: Huihui
authors.initials: H
authors.lastname: Yuan
authors.forename: Minbo
authors.initials: M
authors.lastname: Lan
mesh_terms: D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000008:administration & dosage / Q000737:chemistry; D002470:Cell Survival / Q000187:drug effects; D003692:Delayed-Action Preparations / Q000008:administration & dosage / Q000138:chemical synthesis*; D004058:Diffusion; D004317:Doxorubicin / Q000008:administration & dosage* / Q000737:chemistry; D058973:Folate Receptors, GPI-Anchored / Q000378:metabolism; D005492:Folic Acid / Q000737:chemistry / Q000493:pharmacokinetics*; D006367:HeLa Cells; D006801:Humans; D006863:Hydrogen-Ion Concentration; D061986:MCF-7 Cells; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D008823:Micelles; D053769:Nanocapsules / Q000008:administration & dosage / Q000737:chemistry* / Q000648:ultrastructure; D058726:Nanoconjugates / Q000008:administration & dosage / Q000737:chemistry / Q000648:ultrastructure; D009369:Neoplasms / Q000188:drug therapy* / Q000378:metabolism* / Q000473:pathology; D010316:Particle Size; D013696:Temperature; D016896:Treatment Outcome
chemical_list: D000903:Antibiotics, Antineoplastic; D003692:Delayed-Action Preparations; D058973:Folate Receptors, GPI-Anchored; D008823:Micelles; D053769:Nanocapsules; D058726:Nanoconjugates; D004317:Doxorubicin; D005492:Folic Acid