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Abstract:
Objective To prepare paclitaxel-loaded pH-sensitive block copolymer micelles and evaluate the in vitro anti-cancer effect. Methods A block copolymer, poly(ε-caprolactone)-poly(N,N-diethylamino-ethylmethacrylate)-poly (ethylene glycol)(PDC), was prepared by ATRP and click reactions and polymeric micelles were prepared. The sizes and zeta potentials of micelles were determined under varied pH values. Paclitaxel was encapsulated n the micelles. The encapsulation efficiency and loading efficiency were measured. Drug release was investigated using dialysis method. Human breast cancer MCF-7 cells were used to evaluate the anti-cancer effect of drug-loaded micelles by MTT method. Results The sizes and zeta potentials of micelles decreased with the increase of pH values. The drug encapsulation efficiency was 92. 0% and the loading efficiency was 8. 36%. Under neutral environment, the mean size was 100. 3 nm, and the zeta potential was close to zero. The micelles showed faster drug release, higher accumulation release, and better anti-cancer effect in the low pH (6. 5)media than n the neutral media. Conclusion The pH-sensitive block copolymer micelles have the merits of pH-sensitive drug release and high anti-cancer effect. It is a promising anti-cancer drug carrier.
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Source :
Journal of International Pharmaceutical Research
ISSN: 1674-0440
Year: 2013
Issue: 2
Volume: 40
Page: 233-236,241
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ESI Highly Cited Papers on the List: 0 Unfold All
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30 Days PV: 1