Abstract
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.
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