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Polymeric micelles as a drug delivery system enhance cytotoxicity of vinorelbine through more intercellular accumulation.

Abstract
Polymeric micelles had been used as an efficacious carrier system for anti-cancer drug delivery. However, it is not clear whether the molecular mechanism of drug encapsulated in micelles is same as free drug. In this study, the mechanism of vinorelbine loaded in glycol-phosphatidylethanolamine (PEG-PE) micelles (M-Vino) on tumor cells was investigated. Compared with free vinorelbine (Free Vino), M-Vino was more effective in inhibiting the growth of tumor cells in vitro, inducing G(2)/M phase arrest and apoptosis of tumor cells. M-Vino showed a faster entry and higher accumulation in 4T1 cells than free vinorelbine. Therefore, M-Vino destabilized microtubules, induced cell death, and enhanced its cytotoxicity through more intercellular accumulation of vinorelbine.
AuthorsXiaoyan Lu, Fayun Zhang, Lei Qin, Fengying Xiao, Wei Liang
JournalDrug delivery (Drug Deliv) Vol. 17 Issue 4 Pg. 255-62 (May 2010) ISSN: 1521-0464 [Electronic] England
PMID20307251 (Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Cytotoxins
  • Micelles
  • Polymers
  • Vinblastine
  • Vinorelbine
Topics
  • Animals
  • Cell Death (drug effects, physiology)
  • Cell Line, Tumor
  • Cytotoxins (administration & dosage, pharmacokinetics, toxicity)
  • Dose-Response Relationship, Drug
  • Drug Delivery Systems (methods)
  • Extracellular Fluid (drug effects, metabolism)
  • Mice
  • Micelles
  • Polymers (administration & dosage, pharmacokinetics, toxicity)
  • Vinblastine (administration & dosage, analogs & derivatives, pharmacokinetics, toxicity)
  • Vinorelbine

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