title: A micellar prodrug of paclitaxel conjugated to cyclotriphosphazene.
abstract: A novel water soluble and biodegradable cyclotriphosphazene-paclitaxel conjugate was prepared by reacting 2'-succinyl paclitaxel with cyclotriphosphazenes bearing equimolar glycyl-L-lysine and methoxy poly(ethylene glycol) as side groups. The macromolecular conjugate was found to self-assemble in aqueous solution to form stable micelles with a mean hydrodynamic diameter of 24.7 nm and a low critical micelle concentration of 10 mg/L. The present conjugate exhibited lower than free paclitaxel but reasonably high in vitro cytotoxicity against selected human tumor cells due to their hydrolytic degradation in PBS solution.
authors.affiliation: Department of Chemistry and Nano Science, Ewha Womans University, 11-1 Daehyun-Dong, Seodaemun-Gu, Seoul 120-750, Republic of Korea.
authors.forename: Yong Joo
authors.initials: YJ
authors.lastname: Jun
authors.forename: Jee Hyon
authors.initials: JH
authors.lastname: Min
authors.forename: Da Eun
authors.initials: da E
authors.lastname: Ji
authors.forename: Jin Hee
authors.initials: JH
authors.lastname: Yoo
authors.forename: Ji Hyeon
authors.initials: JH
authors.lastname: Kim
authors.forename: Hwa Jeong
authors.initials: HJ
authors.lastname: Lee
authors.forename: Byeongmoon
authors.initials: B
authors.lastname: Jeong
authors.forename: Youn Soo
authors.initials: YS
authors.lastname: Sohn
mesh_terms: D001673:Biodegradation, Environmental; D004151:Dipeptides / Q000737:chemistry; D015195:Drug Design; D006801:Humans; D006868:Hydrolysis; D009682:Magnetic Resonance Spectroscopy; D008823:Micelles; D008968:Molecular Conformation; D009943:Organophosphorus Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D017239:Paclitaxel / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology*; D010758:Phosphorus / Q000737:chemistry; D011092:Polyethylene Glycols / Q000737:chemistry; D011355:Prodrugs; D012995:Solubility; D013499:Surface Properties; D014867:Water / Q000737:chemistry*
chemical_list: D004151:Dipeptides; D008823:Micelles; D009943:Organophosphorus Compounds; D011355:Prodrugs; C540148:cyclotriphosphazene-paclitaxel conjugate; D014867:Water; D010758:Phosphorus; D011092:Polyethylene Glycols; C035809:glycyllysine; D017239:Paclitaxel