Dextran-<em>g</em>-lauric acid as IKK complex inhibitor carrier

Chao-Ming Su; Ching Lin; Chen-Yu Huang; Jih-Chao Yeh; Tien-Yao Tsai; Tzong Rong Ger; Ming-Chen Wang; Shyh-Liang Lou

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Dextran-g-lauric acid as IKK complex inhibitor carrier

机译：葡聚糖- g -月桂酸作为IKK复合抑制剂载体

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Copolymeric micelles made from dextran-g-lauric acid were optimized to carry IκB kinase-β inhibitor, IMD-0354, to form a drug delivery system and to verify the effects on drug loading and encapsulation efficiency. Dextran with different molecular weights was modified by lauric acid via an esterification process between the hydroxyl group of dextran and the carboxyl group of lauric acid. The hydrophilic dextran acts as a framework and lauric acid was grafted to its branches, forming an amphiphilic polymer. Fourier transform infrared spectrometry and 1H nuclear magnetic resonance (NMR) were used to confirm and calculate the grafting percentage of dextran-g-lauric acid. The critical micelle concentration (CMC) values were obtained using ultraviolet-visible spectrophotometry, and particle size was measured using dynamic light scattering and transmission electron microscopy (TEM). The effect of drug-loaded micelles was verified using cell viability and immunofluorescence staining. TEM images indicated that the self-assembled micelles are spherical in shape. The drug loading percentage of micelles was 0.76–4.67%, and the encapsulation efficiency was 15.4–93.75%. Regulating the hydrophilic and hydrophobic fragments of dextran-g-lauric acid changed the particle size, grafting rate, CMC, drug loading, and encapsulation efficiency of the polymer. IMD-0354-loaded micelles showed higher apoptosis expression in melanoma than free IMD-0354. This shows that controlled interactions of hydrophilic and hydrophobic regions on dextran-g-lauric acid may have profound effects on drug delivery for cancer treatment. 展开▼

机译：优化了由葡聚糖- g -月桂酸制得的共聚胶束，可携带IκB激酶-β抑制剂IMD-0354，形成药物递送系统，并验证其对载药量和包封效率的影响。月桂酸通过在葡聚糖的羟基和月桂酸的羧基之间的酯化过程来修饰不同分子量的葡聚糖。亲水性葡聚糖充当骨架，月桂酸接枝到其分支上，形成两亲聚合物。用傅里叶变换红外光谱法和 1 H核磁共振（NMR）确定并计算右旋糖酐- g -月桂酸的接枝率。使用紫外可见分光光度法获得临界胶束浓度（CMC）值，并使用动态光散射和透射电子显微镜（TEM）测量粒径。使用细胞活力和免疫荧光染色验证了载药胶束的作用。 TEM图像表明，自组装胶束为球形。胶束的载药率为0.76-4.67％，包封效率为15.4-93.75％。调节葡聚糖- g -月桂酸的亲水性和疏水性片段会改变聚合物的粒径，接枝率，CMC，载药量和包封效率。载有IMD-0354的胶束在黑色素瘤中的凋亡表达高于游离IMD-0354。这表明右旋糖酐- g -月桂酸上亲水性和疏水性区域的受控相互作用可能对癌症治疗的药物输送产生深远影响。 展开▼

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《RSC Advances》 |2017年第89期|共9页

作者
Chao-Ming Su; Ching Lin; Chen-Yu Huang; Jih-Chao Yeh; Tien-Yao Tsai; Tzong Rong Ger; Ming-Chen Wang; Shyh-Liang Lou;
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1. Dextran-g-lauric acid as IKK complex inhibitor carrier [J] . Su Chao-Ming, Lin Ching, Huang Chen-Yu, RSC Advances . 2017,第89期

机译：葡聚糖-G-月桂酸作为IKK复合物抑制剂载体

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Dextran-g-lauric acid as IKK complex inhibitor carrier

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