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• W3005982878 abstract "Carrier-free nanodrug via small-molecule assembly is a promising alternative strategy for tumor therapy. Thus, developing a self-recognizing carrier-free nanodrug without introduction of foreign ligand is very attractive to meet both targeting and therapeutic requirements while reducing structural complexity. Here we fabricated a tumor microenvironment-activated self-targeting nanodrug, via co-assembly of hydroxycamptothecin (HCPT) and bi-functional methotrexate (MTX, not only has antitumor effect but also shows innate affinity towards folate receptors) followed by surface covering through acidity-responsive polyethylene glycol (PEG). Notably, the morphology and size of MTX-HCPT nanodrug could be tuned by varying the drug-to-drug ratio and assembly time. The PEG shell of our nanodrug could be detached in response to acidic tumor microenvironment, and then MTX could be exposed for self-targeting to enhance tumor cell uptake. Subsequently, the shell-detached nanodrug could be dissociated in relatively stronger acidic lysosomal environment, resulting in burst release of both drugs. Further in vitro and in vivo studies demonstrated that our nanodrug showed a ~2.98-fold increase in cancer cell uptake, a ~1.25-fold increase in drug accumulation at tumor site, a significantly lower CI50 value of ~0.3, a ~27.3% improvement in tumor inhibition comparing with the corresponding non-responsive nanodrug. Taken together, the here reported tumor microenvironment-activated self-recognizing nanodrug might be an extremely promising strategy for synergistically enhancing chemotherapy efficiency with minimized side effects." @default.
• W3005982878 created "2020-02-24" @default.
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• W3005982878 date "2020-05-01" @default.
• W3005982878 modified "2023-10-14" @default.
• W3005982878 title "Tumor microenvironment-activated self-recognizing nanodrug through directly tailored assembly of small-molecules for targeted synergistic chemotherapy" @default.
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• W3005982878 doi "https://doi.org/10.1016/j.jconrel.2020.02.025" @default.
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