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首页> 外文期刊>Acta biomaterialia >A pH-sensitive charge-conversion system for doxorubicin delivery.
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A pH-sensitive charge-conversion system for doxorubicin delivery.

机译：用于多柔比星输送的pH敏感电荷转换系统。

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A novel pH-sensitive charge-conversion shielding system was designed by the electrostatic binding of polyethylenimine (PEI)-poly(l-lysine)-poly(l-glutamic acid) (PELG), PEI, and cis-aconityl-doxorubicin (CAD). Doxorubicin (DOX) was modified by cis-aconityl linkage to form acid-sensitive CAD, which was then adsorbed by the positively charged PEI. The PEI/CAD complexes were subsequently shielded with the pH-responsive charge-conversion PELG. In normal tissues, the PELG/PEI/CAD complexes were negatively charged; in acidic tumor tissues, the shielding PELG was positively charged and detached from the PELG/PEI/CAD complexes. The resulting positively charged PEI/CAD complexes thus became exposed and were endocytosed. CAD was then cleaved in the acidic intracellular environment of endosomes and lysosomes, and converted back into DOX. The charge reversal of the PELG/PEI/CAD complexes was verified by zeta potential analysis at different pH values. Moreover, DOX release increased with decreasing pH. Cell uptake and confocal laser scanning microscopy analyses showed that, at pH 6.8, PELG/PEI/CAD had the highest endocytosis rate and more DOX entered cell nuclei. More importantly, the system showed remarkable cytotoxicity against cancer cells. These results revealed that the combination of pH-sensitive charge-conversion shielding with pH-sensitive drug release is a potential drug delivery system for tumor treatment.
机译：一种新颖的pH敏感的电荷转换屏蔽系统是由静电聚乙烯亚胺（PEI） - 聚（L-赖氨酸） - 聚（L-谷氨酸）的结合（PELG），PEI，和顺式 - 乌头 - 阿霉素（CAD设计）。多柔比星（DOX）通过顺式 - 乌头联动修饰以形成酸敏感CAD，然后将其通过带正电的PEI吸附。的PEI / CAD复合物随后与pH-响应电荷转换PELG屏蔽。在正常组织中，PELG / PEI / CAD复合物带负电荷;在酸性肿瘤组织，遮蔽PELG是带正电，并从PELG / PEI / CAD络合物分离。将得到的带正电的PEI / CAD络合物因此成为暴露并内吞。 CAD然后在核内体和溶酶体的酸性细胞内环境切割，并且转换回DOX。所述PELG / PEI / CAD络合物的电荷反转，通过在不同pH值的ζ电位分析证实。此外，DOX释放随pH升高。细胞摄取和共聚焦激光扫描显微镜分析表明，在pH 6.8，PELG / PEI / CAD具有最高的细胞内吞作用速率和更DOX进入细胞核。更重要的是，系统显示了对癌细胞的细胞毒作用显着。这些结果表明，pH敏感的电荷转换屏蔽的具有pH敏感的药物释放的组合对于肿瘤治疗的潜在药物递送系统。

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