title: Enhancing curcumin anticancer efficacy through di-block copolymer micelle encapsulation.
abstract: We report herein the development of a novel aqueous formulation and improved antitumor activity for curcumin by encapsulating it into a biocompatible and biodegradable poly(L-lactic acid) based poly(anhydride-ester)-b-poly(ethylene glycol) (PAE-b-PEG) micelle. The resulting curcumin loaded micelles were completely water-dispersible, overcoming the problem of poor water solubility that limited its efficacy and bioavailability. In vitro cellular studies revealed that the curcumin-loaded micelles were taken up mainly via endocytosis route and exhibited higher cytotoxicities toward model cancer cell lines (HeLa and EMT6) than free curcumin. An in vivo biodistribution study revealed that the curcumin-loaded micelles displayed significantly enhanced accumulation inside the tumor of EMT6 breast tumor-bearing mice. More impressively, the curcumin-loaded micelles showed stronger antitumor activity, higher anti-angiogenesis effects and induced apoptosis on the EMT6 breast tumor model bearing mice than free curcumin. Furthermore, the curcumin-loaded micelles showed no significant toxicity towards hemotological system, major organs or tissues in mice. Combined with a high antitumor activity and low toxic side-effects, the curcumin-loaded micelles developed here thus appear to be a highly attractive nanomedicine for effective, targeted cancer therapy.
authors.forename: Li
authors.initials: L
authors.lastname: Lv
authors.forename: Yuanyuan
authors.initials: Y
authors.lastname: Shen
authors.forename: Jieying
authors.initials: J
authors.lastname: Liu
authors.forename: Feihu
authors.initials: F
authors.lastname: Wang
authors.forename: Min
authors.initials: M
authors.lastname: Li
authors.forename: Min
authors.initials: M
authors.lastname: Li
authors.forename: Aijie
authors.initials: A
authors.lastname: Guo
authors.forename: Yun
authors.initials: Y
authors.lastname: Wang
authors.forename: Dejian
authors.initials: D
authors.lastname: Zhou
authors.forename: Shengrong
authors.initials: S
authors.lastname: Guo
mesh_terms: D020533:Angiogenesis Inhibitors; D000818:Animals; D000970:Antineoplastic Agents / Q000009:adverse effects / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D016923:Cell Death / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D003474:Curcumin / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D004705:Endocytosis / Q000187:drug effects; D005260:Female; D005453:Fluorescence; D006367:HeLa Cells; D006801:Humans; D057446:Hydrodynamics; D020128:Inhibitory Concentration 50; D051379:Mice; D008823:Micelles; D046529:Microscopy, Electron, Transmission; D009369:Neoplasms / Q000188:drug therapy* / Q000473:pathology; D010316:Particle Size; D011091:Polyesters / Q000737:chemistry; D011092:Polyethylene Glycols / Q000737:chemistry; D011108:Polymers / Q000737:chemistry*; D014018:Tissue Distribution; D016896:Treatment Outcome
chemical_list: D020533:Angiogenesis Inhibitors; D000970:Antineoplastic Agents; D008823:Micelles; D011091:Polyesters; D011108:Polymers; D011092:Polyethylene Glycols; D003474:Curcumin