Polymeric micelle-based drug delivery systems have been extensively studied by researchers due to their nanoscopic size and low toxicity. In this study, we have designed and synthesized an amphiphilic ursolic acid-polyethylene glycol conjugate, which on self-assembly results in micellar nanostructures. We conjugated ursolic acid (UA) with polyethylene glycol monomethyl ether in a single step in the presence of a condensing reagent, DCC/DMAP, and their self-assembly was monitored by DLS and TEM. Further an anticancer drug, doxorubicin (DOX), was encapsulated into the hydrophobic core of the self-assembled nanostructures. Due to strong interactions between DOX and UA, high encapsulation efficiency (85.3%) was obtained. The release pattern of DOX from the loaded nanostructures showed a sustained release of drug over a period of time. The projected system showed responsiveness towards lipase and hence, biodegradability aspect of the nanostructure (UA-PEG) was also investigated by lipase-mediated degradation studies. MTT experiments were also carried out on both normal HEK293 cells and MG-63 cancer cells and showed the non-toxic nature of the projected conjugate. These results ensure the promising potential of the projected system as an efficient drug delivery vehicle specifically to cancers cells in vivo and in vitro.

基于聚合物胶束的药物递送系统由于其纳米级的尺寸和低毒性已被研究人员广泛研究。在这项研究中，我们设计并合成了一种两亲性熊果酸-聚乙二醇共轭物，其自组装后形成胶束纳米结构。我们在缩合剂DCC / DMAP存在的情况下，一步将熊果酸（UA）与聚乙二醇单甲醚共轭，并通过DLS和TEM监测了它们的自组装。此外，将抗癌药阿霉素（DOX）封装到自组装纳米结构的疏水核中。由于DOX和UA之间的强相互作用，因此获得了很高的封装效率（85.3％）。从负载的纳米结构释放DOX的模式显示了一段时间内药物的持续释放。预计的系统显示出对脂肪酶的响应性，因此，还通过脂肪酶介导的降解研究对纳米结构（UA-PEG）的生物降解性进行了研究。还对正常的HEK293细胞和MG-63癌细胞都进行了MTT实验，结果表明，该偶联物具有无毒性质。这些结果确保了该计划的系统作为一种专门针对癌细胞的有效药物输送工具的有前途的潜力体内和体外。