A micellar prodrug of paclitaxel conjugated to cyclotriphosphazene

Yong Joo Jun, Jee Hyon Min, Da Eun Ji, Jin Hee Yoo, Ji Hyeon Kim, Hwa Jeong Lee, Byeongmoon Jeong, Youn Soo Sohn

Research output: Contribution to journalArticlepeer-review

14 Scopus citations

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.

Original languageEnglish
Pages (from-to)6410-6413
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume18
Issue number24
DOIs
StatePublished - 15 Dec 2008

Keywords

  • Antitumor agent
  • Cyclotriphosphazene
  • Paclitaxel
  • Prodrug

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