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Optimizacija svojstava samoorganiziranja graft kopolimera metoksi poli(etilen glikola) i masnih kiselina pri pripravi nanonosača s uklopljenim etopozidom

机译:在制备结合了依托泊苷的纳米载体中,对甲氧基聚乙二醇和脂肪酸的接枝共聚物的自组织性能进行优化

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摘要

The objective of this work was to study the effect of fatty acid chain length grafted to methoxy poly(ethylene glycol) (mPEG) on self assembling properties of micelles for etoposide delivery. Three amphiphilic copolymers were synthesized using mPEG, myristic acid, stearic acid and behenic acid through an esteric linkage. The particle size and zeta potential of the micelles were determined by the dynamic light scattering method. Etoposide was loaded into micelles by film casting using various drug/polymer ratios. Drug release was studied by the dialysis method. The structure of copolymers was confirmed by 1H NMR and FTIR. Critical micellar concentration (CMC) measurements showed that the longer hydrophobic chains formed more thermodynamically stable micelles. Among the prepared copolymers, etoposide showed the highest solubility in the mPEG-behenic copolymer. Drug loading efficiency depended on the hydrophobic chain length and drug/polymer ratio. The highest drug loading efficiency was found in mPEG-myristic micelles with 1:20 drug/polymer ratio. Micelles released 80 % of loaded drug within about 5 h.
机译:这项工作的目的是研究嫁接到甲氧基聚乙二醇(mPEG)的脂肪酸链长对依托泊苷传递的胶束自组装性能的影响。使用mPEG,肉豆蔻酸,硬脂酸和山hen酸通过酯键合成了三种两亲共聚物。通过动态光散射法测定胶束的粒径和ζ电势。通过使用各种药物/聚合物比率的薄膜流延将依托泊苷装载到胶束中。通过透析方法研究药物释放。共聚物的结构通过1 H NMR和FTIR确认。临界胶束浓度(CMC)测量表明,较长的疏水链形成了更热力学稳定的胶束。在制备的共聚物中,依托泊苷在mPEG-山hen酸共聚物中显示出最高的溶解度。载药效率取决于疏水链长度和药物/聚合物比。在药物/聚合物比率为1:20的mPEG-myristic胶束中发现了最高的药物加载效率。胶束在约5小时内释放了80%的载药量。

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