Stable and efficient delivery of docetaxel by micelle-encapsulation using a tripodal cyclotriphosphazene amphiphile

Yong Joo Jun, Vithal B. Jadhav, Jee Hyon Min, Jin Xin Cui, Song Wha Chae, Jong Min Choi, In Sun Kim, Soo Jin Choi, Hwa Jeong Lee, Youn Soo Sohn

Research output: Contribution to journalArticlepeer-review

32 Scopus citations

Abstract

Docetaxel micelle-encapsulated by a tripodal cyclotriphosphazene amphiphilile [NP(PEG750)(GlyPheLeu) 2Et] 3 (CP750) exhibited outstanding drug-loaded micelle stability in aqueous solution compared with the polymeric micelles assembled from linear block copolymers. Furthermore, docetaxel micelle-encapsulated by CP750 is obtainable in solvent free powder form, which is immediately soluble in any aqueous media including saline and PBS and very stable to photo-degradation even in the room light at room temperature. Although docetaxel micelle-encapsulated by CP750 did not display highly improved pharmacokinetic profile compared with Taxotere® currently in clinical use, its in vivo xenograft trials exhibited excellent antitumor efficacy by showing complete tumor regression against the breast cancer cells (MDA-MB-231) at a lower dose of 5 mg/kg and better efficacy against gastric cancer cells (MKN-28) compared with Taxotere®. Furthermore, according to the comparative acute toxicity study, toxicities associated with Taxotere® may be remarkably reduced by micelle-encapsulation of docetaxel using CP750, which afforded a much higher LD 50 value of 75 mg/kg compared with 28 mg/kg of docetaxel in Taxotere®. Thus docetaxel micelle-encapsulated by CP750 has entered the stage of preclinical studies.

Original languageEnglish
Pages (from-to)374-380
Number of pages7
JournalInternational Journal of Pharmaceutics
Volume422
Issue number1-2
DOIs
StatePublished - 17 Jan 2012

Keywords

  • Anticancer drug
  • Cyclotriphosphazene
  • Docetaxel
  • Micelle
  • Taxane

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