Document Detail

Novel mixed polymeric micelles for enhancing delivery of anticancer drug and overcoming multidrug resistance in tumor cell lines simultaneously.
MedLine Citation:
PMID:  20411408     Owner:  NLM     Status:  MEDLINE    
PURPOSE: To evaluate novel mixed polymeric micelles based on monomethoxy poly(ethylene glycol)-poly(D,L-lactic acid) (mPEG-PLA) and Pluronic L61 for delivery of paclitaxel (PTX) to circumvent unfavorable effects resulting from Cremophore EL in Cremophore EL-based PTX formulation and overcoming multidrug resistance (MDR) in tumor cells at the same time. METHODS: PTX-loaded plain micelles and mixed micelles were prepared and characterized by determining PTX release in vitro, MDR reversal effect in human breast cancer MDR MCF-7/ADR cell sublines and pharmacokinetics in vivo. RESULTS: Both PTX-loaded plain micelles and mixed micelles had similar in vitro release profile. Mixed micellar PTX significantly reduced IC(50) of PTX in MCF-7/ADR cells compared to free PTX and plain micellar PTX, and mixed micelles substantially enhanced cellular accumulation of R 123 in MCF-7/ADR cells compared to free R123 and plain micelles. PTX-loaded mixed micelles with lower content of L61 exhibited comparable cytotoxicity to that observed with Cremophore EL-based PTX formulation in inhibiting the growth of MCF-7/ADR cells. Moreover, plain micelles and mixed micelles retained the pharmacokinetic characteristics of PTX in rats compared with Cremophore EL-based PTX formulation. CONCLUSION: This study suggested that the mixed micelles could enhance delivery of PTX and cell-killing effect for MDR MCF-7/ADR cells.
Xinru Li; Pingzhu Li; Yanhui Zhang; Yanxia Zhou; Xingwei Chen; Yanqing Huang; Yan Liu
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2010-04-23
Journal Detail:
Title:  Pharmaceutical research     Volume:  27     ISSN:  1573-904X     ISO Abbreviation:  Pharm. Res.     Publication Date:  2010 Aug 
Date Detail:
Created Date:  2010-07-05     Completed Date:  2010-10-13     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  8406521     Medline TA:  Pharm Res     Country:  United States    
Other Details:
Languages:  eng     Pagination:  1498-511     Citation Subset:  IM    
Department of Pharmaceutics, School of Pharmaceutical Sciences Peking University, Beijing, 100191, China.
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MeSH Terms
Antineoplastic Agents, Phytogenic / administration & dosage*
Breast Neoplasms / drug therapy
Cell Line, Tumor
Drug Compounding
Drug Delivery Systems*
Drug Resistance, Neoplasm*
Inhibitory Concentration 50
Paclitaxel / administration & dosage*
Particle Size
Poloxamer / pharmacokinetics*
Polyesters / pharmacokinetics*
Polyethylene Glycols / pharmacokinetics*
Rats, Sprague-Dawley
Reg. No./Substance:
0/Antineoplastic Agents, Phytogenic; 0/Micelles; 0/Polyesters; 0/Polyethylene Glycols; 0/methoxy poly(ethylene glycol)-poly(lactide); 0/pluronic L61; 106392-12-5/Poloxamer; 33069-62-4/Paclitaxel

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