Incorporation and release behavior of amitriptylene in core-shell-corona type triblock copolymer micelles

Incorporation and release behavior of amitriptylene in core-shell-corona type triblock copolymer micelles
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DOI:
10.1016/j.colsurfb.2011.08.009
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发表时间:
2011-12-01
影响因子:
5.8
通讯作者:
Nakashima, Kenichi
Nakashima, Kenichi
中科院分区:
工程技术2区
文献类型:
--
作者:
Bastakoti, Bishnu Prasad;Guragain, Sudhina;Nakashima, Kenichi

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将阳离子抗抑郁药物氨甲三丁烯成功地引入到聚苯乙烯-b-2-(acryiamido)-2-methyl-1-propanesulfonate-b-ethylene氧化钠(PS-b-PAMPS-b-PEO)核壳电晕胶束中。Zeta电位测量表明,静电和疏水相互作用都有助于药物与聚合物的结合。用动态光散射、扫描电子显微镜和透射电子显微镜对AMT/PS-b-PAMPS-b-PEO纳米复合材料进行了表征。随着载药量的增加,载药纳米络合物的流体力学直径从80 nm减小到40 nm。这归因于阳离子药物消除了PAMPS基团的负电荷。AMT/PS-b-PAMPS-b-PEO纳米复合材料在水溶液中稳定,几个月来没有聚集或沉淀。研究了AMT在无盐和0.1M氯化钠溶液中的体外释放。药物在0.1M氯化钠溶液中的释放速度比在无盐溶液中的释放速度快。这是由于盐对静电相互作用的屏蔽作用。然而,在这两种情况下,药物释放主要是通过Fickian扩散机制进行的。(C)2011爱思唯尔B.V.保留所有权利。
A cationic antidepressant drug, amitriptylene (AMT), was successfully incorporated into core-shell-corona micelles of poly[styrene-b-sodium 2-(acryiamido)-2-methyl-1-propanesulfonate-b-ethylene oxide] (PS-b-PAMPS-b-PEO). Zeta-potential measurements revealed that both electrostatic and hydrophobic interactions contributed to the binding of the drug to the polymer. The AMT/PS-b-PAMPS-b-PEO nanocomplexes were characterized by dynamic light scattering, scanning electron microscopy, and transmission electron microscopy. The hydrodynamic diameter of the AMT loaded nanocomplexes decreased from 80 to 40 nm depending on the amount of the drug loaded on the polymer. This is attributed to the cancellation of the negative charge of the PAMPS group by the cationic drug. The AMT/PS-b-PAMPS-b-PEO nanocomplexes were stable in aqueous solution exhibiting no aggregation or no precipitation for several months. Release of the AMT from the nanocomplexes was investigated in vitro in salt-free and 0.1 M NaCl solutions. The drug was released faster in the 0.1 M NaCl solution than in the salt-free solution. This is due to the shielding effect of the salt on the electrostatic interaction. However, in both cases, the drug release mainly occurs by the Fickian diffusion mechanism. (C) 2011 Elsevier B.V. All rights reserved.