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

Title
Stable and efficient delivery of docetaxel by micelle-encapsulation using a tripodal cyclotriphosphazene amphiphile
Authors
Jun Y.J.Jadhav V.B.Min J.H.Cui J.X.Chae S.W.Choi J.M.Kim I.-S.Choi S.-J.Lee H.J.Sohn Y.S.
Ewha Authors
손연수이화정
SCOPUS Author ID
손연수scopus; 이화정scopus
Issue Date
2012
Journal Title
International Journal of Pharmaceutics
ISSN
0378-5173JCR Link
Citation
vol. 422, no. 41276, pp. 374 - 380
Indexed
SCI; SCIE; SCOPUS WOS scopus
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. © 2011 Elsevier B.V.
DOI
10.1016/j.ijpharm.2011.10.052
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자연과학대학 > 화학·나노과학전공 > Journal papers
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