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        Synthesis of acid-activated reversible conversion supramolecular nanoplatform: application in drug delivery and anti-tumor activity

        Yang Cuiting,Xiangyu Chen,Jinkui Teng,Shuai Chen,Jianmei Yang,Xiaoqing Liu,Junnan He,Jin Zhang,Yan Zhao 한국고분자학회 2024 Macromolecular Research Vol.32 No.1

        Supramolecular nanoplatforms with stimuli-responsive behavior feature sensitive performance and effective drug delivery, which are desirable as intelligent drug delivery systems. Generally, tumor cells are characterized by excessive acid production, resulting in a lower pH in the tumor microenvironment (pH < 6.5) than in normal tissues (pH ≈7.4) and providing the possibility for the drug delivery system to exploit this decrease in pH as a trigger for drug release. Here, an acid-sensitive supramolecular nanoplatform (CM-β-CD/FC12 +Br− NPs) with assembly/disassembly properties was designed and constructed, which was exploited to capture, deliver, and release anti-tumor compound CSL. 2D NOESY was utilized to examine the host–guest interaction and the potential mechanism for CM-β-CD/FC12 +Br− NPs loading CSL. CM-β-CD/FC12 +Br− NPs present good blood compatibility. Cytotoxicity assay revealed that CSL-loaded NPs display minimal toxicity against normal cells BEAS-2B and good anticancer ability against five human cancer cell lines, especially for Human hepatoma cell line SMMC-7721. In addition, cell apoptosis and cycle assay further verified that CSL-loaded NPs-induced apoptosis in SMMC- 7721 cells up to ~ 93%, as well as blocking the cells in G0/G1 phase and inhibiting the proliferation of SMMC-7721 cells in a dose-dependent manner. We expect that CM-β-CD/FC12 +Br− NPs will be potential acid-answered drug delivery candidates.

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