title: Polymeric micelles for targeted tumor therapy of platinum anticancer drugs.
abstract: Platinum anticancer drugs are effective against a wide range of tumors, though their severe adverse effects and resistance remain unresolved. A breakthrough in these drawbacks could be achieved by using polymeric micelles, i.e. nanoassemblies having a drug loaded core and a protective hydrophilic shell, incorporating platinum drugs for tumor-targeted delivery. Areas covered: The development of cisplatin- (NC-6004) and DACHPt-loaded micelles (NC-4016) has been reviewed, particularly, from the viewpoint of the effect of their structural features on the tumor-targeting efficacy. We have also described new approaches for molecular targeting by installing ligand moieties on the surface of micelles. Moreover, small platinum drugs and platinum drug-loaded nanocarriers are introduced to explain the context for developing platinum drug-loaded polymeric micelles. Expert opinion: NC-6004 and NC-4016 micelles meet critical structural and functional requirements for achieving safe and effective tumor targeting, enhancing efficacy even against drug resistant cancer cells, and have been translated into human studies, aiming to be the first-of-their-kind in the clinic. Due to their flexible design, polymeric micelles could readily integrate new features based on the knowledge arising from the human clinical trials toward the development of innovative formulations with superior performance.
authors.affiliation: a Innovation Center of NanoMedicine , Kawasaki Institute of Industrial Promotion , Kawasaki , Japan.
authors.forename: Yuki
authors.initials: Y
authors.lastname: Mochida
authors.affiliation: b Department of Bioengineering , Graduate School of Engineering, The University of Tokyo , Tokyo , Japan.
authors.forename: Horacio
authors.initials: H
authors.lastname: Cabral
authors.affiliation: a Innovation Center of NanoMedicine , Kawasaki Institute of Industrial Promotion , Kawasaki , Japan.|c Policy Alternatives Research Institute, The University of Tokyo , Tokyo , Japan.
authors.forename: Kazunori
authors.initials: K
authors.lastname: Kataoka
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage*; D045744:Cell Line, Tumor; D004337:Drug Carriers / Q000737:chemistry*; D006801:Humans; D008823:Micelles; D009369:Neoplasms / Q000188:drug therapy; D009944:Organoplatinum Compounds / Q000008:administration & dosage* / Q000737:chemistry; D011099:Polyglutamic Acid / Q000008:administration & dosage / Q000031:analogs & derivatives*; D011108:Polymers / Q000737:chemistry
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D008823:Micelles; C000627050:NC-4016; D009944:Organoplatinum Compounds; D011108:Polymers; D011099:Polyglutamic Acid; C557897:demplatin pegraglumer
keywords: Block copolymer; drug delivery; platinum anticancer drug; polymeric micelles; targeted cancer therapy