title: Preclinical evaluation of efficacy and stability of docetaxel micelle-encapsulated by a tripodal cyclotriphosphazene amphiphile.
abstract: Docetaxel formulated by micelle-encapsulation using a tripodal cyclotriphosphazene amphiphile [NP(MPEG750)(GlyPheLeu)2Et]3 (CP750) was named "Phostaxel" and compared in efficacy and stability with Taxotere(®) formulated using the surfactant polysorbate 80, which is currently in clinical use. Phostaxel has always shown better efficacy than Taxotere(®) in various xenograft trials at the same dosage and administration schedule against the tumor cell lines tested. The better efficacy of Phostaxel could be explained based on the difference in pharmacokinetic and biodistribution profiles of Phostaxel and Taxotere(®). Phostaxel exhibited significantly slower clearance rate and larger AUClast value compared with Taxotere(®). Phostaxel has also shown higher DTX distribution in tumor than Taxotere(®). In addition, Phostaxel displayed better solution stability compared with Taxotere(®) both in distilled water and in saline solution at room and refrigerator temperatures.
authors.affiliation: Division of Life and Pharmaceutical Sciences & College of Pharmacy (Global Top 5 Research Program), Ewha Womans University, 52, Ewhayeodae-gil, Seodaemun-gu, Seoul 120-750, Republic of Korea. Electronic address: yuki1226@naver.com.
authors.forename: Song Wha
authors.initials: SW
authors.lastname: Chae
authors.affiliation: C & Pharm, Rm B211, Science Building B, Ewha Womans University, 52, Ewhayeodae-gil, Seodaemun-gu, Seoul 120-750, Republic of Korea. Electronic address: yjjun23@hanmail.net.
authors.forename: Yong Joo
authors.initials: YJ
authors.lastname: Jun
authors.affiliation: C & Pharm, Rm B211, Science Building B, Ewha Womans University, 52, Ewhayeodae-gil, Seodaemun-gu, Seoul 120-750, Republic of Korea. Electronic address: cjxybu04@126.com.
authors.forename: Jin Xin
authors.initials: JX
authors.lastname: Cui
authors.affiliation: Division of Life and Pharmaceutical Sciences & College of Pharmacy (Global Top 5 Research Program), Ewha Womans University, 52, Ewhayeodae-gil, Seodaemun-gu, Seoul 120-750, Republic of Korea. Electronic address: 10239@hanmail.net.
authors.forename: Jung Hyun
authors.initials: JH
authors.lastname: Park
authors.affiliation: Division of Life and Pharmaceutical Sciences & College of Pharmacy (Global Top 5 Research Program), Ewha Womans University, 52, Ewhayeodae-gil, Seodaemun-gu, Seoul 120-750, Republic of Korea. Electronic address: hwalee@ewha.ac.kr.
authors.forename: Hwa Jeong
authors.initials: HJ
authors.lastname: Lee
authors.affiliation: C & Pharm, Rm B211, Science Building B, Ewha Womans University, 52, Ewhayeodae-gil, Seodaemun-gu, Seoul 120-750, Republic of Korea. Electronic address: yssohn@ewha.ac.kr.
authors.forename: Youn Soo
authors.initials: YS
authors.lastname: Sohn
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use; D001835:Body Weight / Q000187:drug effects; D000077143:Docetaxel; D004353:Drug Evaluation, Preclinical; D004355:Drug Stability; D005260:Female; D008297:Male; D008819:Mice, Nude; D008823:Micelles; D009943:Organophosphorus Compounds / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D010455:Peptides / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D011092:Polyethylene Glycols / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D017207:Rats, Sprague-Dawley; D012996:Solutions; D013501:Surface-Active Agents / Q000494:pharmacology / Q000627:therapeutic use*; D043823:Taxoids / Q000494:pharmacology / Q000627:therapeutic use*; D013997:Time Factors; D014018:Tissue Distribution / Q000187:drug effects; D016896:Treatment Outcome; D023041:Xenograft Model Antitumor Assays
chemical_list: C571634:(NP(PEG750)(GlyPheLeu)2Et)3; D000970:Antineoplastic Agents; D008823:Micelles; D009943:Organophosphorus Compounds; D010455:Peptides; D012996:Solutions; D013501:Surface-Active Agents; D043823:Taxoids; D000077143:Docetaxel; D011092:Polyethylene Glycols
keywords: Anticancer drug; Cyclotriphosphazene; Docetaxel; Drug delivery; Polymeric micelle