Division of Biotechnology, The Catholic University of Korea, Wonmi-gu, Bucheon-si, Gyeonggi-do, Republic of Korea.
Colloids Surf B Biointerfaces. 2010 Jun 15;78(1):120-6. doi: 10.1016/j.colsurfb.2010.02.023. Epub 2010 Feb 26.
In this study, a novel pH-responsive nanogel composed of glycol chitosan (GCS) grafted with functional 3-diethylaminopropyl (DEAP) groups (denoted as GCS-g-DEAP hereafter) was fabricated. The GCS-g-DEAP was designed to have a self-assembled arrangement consisting of hydrophilic block (GCS) and hydrophobic block (DEAP) at physiological pH. As the pH decreased to tumor extracellular pH (pH(e)), the nanogel was destabilized due to the protonation of DEAP. The pH-responsive property of the nanogel at tumor extracellular pH (pH(e)) was characterized in drug-release kinetic studies. The release of doxorubicin (DOX) from DOX-loaded nanogels was significantly accelerated at lower pH values, which allowed for increased DOX uptake by non-small lung carcinoma A546 cells under a slightly acidic pH condition, as in tumor pH(e).
在这项研究中，制备了一种由接枝了功能性 3-二乙氨基丙基（DEAP）基团的乙二醇壳聚糖（GCS）组成的新型 pH 响应性纳米凝胶（以下简称 GCS-g-DEAP）。GCS-g-DEAP 的设计具有在生理 pH 下由亲水嵌段（GCS）和疏水嵌段（DEAP）组成的自组装排列。当 pH 降低至肿瘤细胞外 pH 值（pH(e)）时，由于 DEAP 的质子化，纳米凝胶不稳定。在药物释放动力学研究中，对纳米凝胶在肿瘤细胞外 pH 值（pH(e)）下的 pH 响应特性进行了表征。在较低的 pH 值下，负载 DOX 的纳米凝胶中 DOX 的释放明显加快，这使得在略酸性 pH 条件下，非小细胞肺癌 A546 细胞对 DOX 的摄取增加，如在肿瘤 pH(e)下。
