Physicochemical aspects of doxorubicin-loaded pH-sensitive polymeric micelle formulations from a mixture of poly(L-histidine)-b-poly(ethylene glycol)/poly(L-lactide)-b-poly(ethylene glycol) [corrected].

Physicochemical aspects of doxorubicin-loaded pH-sensitive polymeric micelle formulations from a mixture of poly(L-histidine)-b-poly(ethylene glycol)/poly(L-lactide)-b-poly(ethylene glycol) [corrected].
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DOI:
10.1016/j.ejpb.2008.08.013
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发表时间:
2009-02
期刊:
European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V
影响因子:
--
通讯作者:
Bae YH
Bae YH
中科院分区:
其他
文献类型:
--
作者:
Yin H;Bae YH

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在这项研究中,多柔比星(DOX)被物理掺入由聚(1-组氨酸)-b-聚(乙二醇)/聚(1-丙交酯)-b-聚(乙二醇)(75/25,重量%)的混合物制成的pH敏感性胶束中。使用透析方法配制DOX负载的混合胶束,并且在0.2(wt./wt.)重量)当适量水相(0.2,v./ v.)的一个例子加入到通用溶剂(DMSO)溶液中,然后在4°C下透析。动态光散射、紫外-可见吸收和荧光实验结果表明,包封的药物主要位于疏水胶束核内,受到良好的保护,不能被外部分子所接近。在体外条件下,虽然胶束的微观结构被改变低于pH 8.0的包封药物,载药胶束仍然表现出期望的能力,控制药物释放响应肿瘤细胞外pH。
In this study, doxorubicin (DOX) was physically incorporated into pH sensitive micelles made from a mixture of poly(l--Histidine)-b-poly(ethylene glycol)/ poly(l--Lactide)-b-poly(ethylene glycol) (75/25, wt.%). The DOX-loaded mixed micelles were formulated using dialysis methods and optimal DOX incorporation was achieved at a drug/polymer feed ratio of 0.2 (wt./wt.) when proper amount of aqueous phase (0.2, v./v.) was added into the common solvent (DMSO) solution, followed by dialysis at 4°C. Based on the results obtained from dynamic light scattering, UV-Vis absorption, and fluorescence experiments, it was demonstrated that the encapsulated drugs were mainly located inside the hydrophobic micelle cores, well protected and inaccessible to exterior molecules. Under in vitro conditions, although the microstructure of the micelles was altered below pH 8.0 by the encapsulated drugs, the drug-loaded micelles still exhibited desirable ability to control the drug release in response to tumor extracellular pH.
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