Citation: Qingqing Zhou, Wengui Duan, Luzhi Liu, Yan Huang. Construction and Antitumor Activity of Supramolecular Nano Drug Delivery System Based on Amphiphilic Pillar[5]arene[J]. Chemistry, ;2021, 84(5): 460-466. shu

Construction and Antitumor Activity of Supramolecular Nano Drug Delivery System Based on Amphiphilic Pillar[5]arene

Figures(7)

  • A novel alanine substituted water-soluble pillar[5]arene DAP5 was synthesized, which could be used as building block to construct a supramolecular nano drug loading carrier SDBS⊂DAP5 through host-guest interaction with sodium dodecylbenzene sulfonate (SDBS). This carrier can efficiently encapsulate DOX with an entrapment efficiency of 62.6%. And its nano drug delivery system DOX⊂SDBS⊂DAP5 not only had good pH response performance and could continuously release the drug in a simulated weak acid tumor microenvironment, but also had low toxicity to normal liver cells (LO2) (IC50 >10μmol/L). More importantly, DOX⊂SDBS⊂DAP5 exhibited stronger proliferation inhibition activity and shorter medication time over free drug for four tested cancer cells (Hela, HepG2, MGC-803 and T24). Especially for HepG2, after 24 hours of incubation with drug, IC50 of DOX⊂SDBS⊂DAP5 was 0.77 μmol/L, about 22% of that of DOX (3.43 μmol/L). These results provide important reference information for improving the efficacy and reducing the side effects of supramolecular drug delivery system in the future cancer treatment.
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