Abstract | PURPOSE: 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.
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Authors | Xinru Li, Pingzhu Li, Yanhui Zhang, Yanxia Zhou, Xingwei Chen, Yanqing Huang, Yan Liu |
Journal | Pharmaceutical research
(Pharm Res)
Vol. 27
Issue 8
Pg. 1498-511
(Aug 2010)
ISSN: 1573-904X [Electronic] United States |
PMID | 20411408
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Antineoplastic Agents, Phytogenic
- Micelles
- Polyesters
- methoxy poly(ethylene glycol)-poly(lactide)
- pluronic L61
- Poloxamer
- Polyethylene Glycols
- Paclitaxel
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Topics |
- Animals
- Antineoplastic Agents, Phytogenic
(administration & dosage)
- Breast Neoplasms
(drug therapy)
- Cell Line, Tumor
- Drug Compounding
- Drug Delivery Systems
- Drug Resistance, Neoplasm
- Female
- Humans
- Inhibitory Concentration 50
- Micelles
- Paclitaxel
(administration & dosage)
- Particle Size
- Poloxamer
(pharmacokinetics)
- Polyesters
(pharmacokinetics)
- Polyethylene Glycols
(pharmacokinetics)
- Rats
- Rats, Sprague-Dawley
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