Biodegradable and thermosensitive micelles of amphiphilic polyaspartamide derivatives containing aromatic groups for drug delivery

Biodegradable and thermosensitive micelles of amphiphilic polyaspartamide derivatives containing aromatic groups for drug delivery
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用于药物递送的含有芳香基团的两亲性聚天冬酰胺衍生物的可生物降解和热敏胶束

DOI:
10.1002/pola.26794
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发表时间:
2013-09
期刊:
Journal of Polymer Science Part A: Polymer Chemistry
影响因子:
--
通讯作者:
Zhuo, Renxi
Zhuo, Renxi
中科院分区:
其他
文献类型:
--
作者:
Ma, Yingying;Jiang, Xulin;Zhuo, Renxi

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研究了生物可降解紫杉醇聚合物胶束制剂的制备、表征、释放和体外细胞毒性。采用快速加热法,在不使用有毒有机溶剂的条件下,制备了具有温敏性和可降解性的两亲性含侧链芳香结构的聚天冬酰胺衍生物(phe-g-PHPA-g-mPEG)胶束。动态光散射结果表明,胶束在生理条件下稀释时是稳定的,并且胶束的去稳定化是pH依赖性的,并且phe-g-PHPA-g-mPEG聚合物是可生物降解的。PTX以> 90%的包封率负载到phe-g- PHPAs-g-mPEG胶束中,导致高药物负载含量(高达29%)。PTX负载的胶束具有约70 nm的平均尺寸,具有窄的尺寸分布(多分散指数,<0.1)。载紫杉醇的胶束具有明显的缓释作用和与紫杉醇相似的抗肿瘤活性,而空白胶束无毒性。结果表明,phe-g-PHPA- g-mPEG温敏性胶束是一种很有前途的疏水药物释放体系。V C 2013 Wiley Periodicals,Inc. J.波利姆科学,A部分:聚合物2013,51,3917-3924
The preparation, characterization, release, and in vitro cytotoxicity of a biodegradable polymeric micellar formu- lation of paclictaxel (PTX) were investigated. The micelles based on thermosensitive and degradable amphiphilic polyas- partamide derivatives containing pendant aromatic structures (phe-g-PHPA-g-mPEG) were prepared by a quick heating method without using toxic organic solvent. Dynamic light- scattering results show that the micelles are stable upon dilu- tion under physiological conditions and the destabilization of the micelles is pH-dependent and the phe-g-PHPA-g-mPEG polymers are biodegradable. PTX was loaded into the phe-g- PHPAs-g-mPEG micelles with encapsulation efficiency of >90%, resulting in a high drug loading content (up to 29%). PTX-loaded micelles had a mean size around 70 nm with narrow size distribution (polydispersity index, <0.1). The PTX- loaded micelles showed sustained drug release and obvious anticancer activity similar to Taxol against HepG2 cells, whereas blank micelles were nontoxic. The present results sug- gest that the thermosensitive and biodegradable phe-g-PHPA- g-mPEG micelles are a promising delivery system for the hydrophobic drugs. V C 2013 Wiley Periodicals, Inc. J. Polym. Sci., Part A: Polym. Chem. 2013, 51, 3917-3924
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