4.7 Article

Negatively charged polymer-shielded supramolecular nano-micelles with stimuli-responsive property for anticancer drug delivery

期刊

出版社

ELSEVIER
DOI: 10.1016/j.ijpharm.2022.122211

关键词

Charge -conversional; Dual responsive; Supramolecular; Antitumor; Drug delivery

资金

  1. National Natural Science Foundation of China [21YF5FA104]
  2. Key Research and Development Program of Gansu Province [20JR10RA439]
  3. Natural Science Foundation of Gansu Province [2021-ZJ-711]
  4. Natural Science Foundation of Qinghai Province [SSCJG-SP-201919]
  5. Science and Technology Program of Gansu Administration for Market Regulation
  6. [21772080]

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A new kind of polymer-shielded supramolecular nano-micelles with dual-responsive property was designed for tumor treatment, showing excellent antitumor activity.
A new kind of negatively charged polymer-shielded supramolecular nano-micelles with dual-responsive property was designed for tumor treatment, which was prepared on the basis of adamantane terminated linear PAsp(DIP) and disulfide-beta-cyclodextrin-terminated PAsp(EDA). The supramolecular nano-micelles comprised a 2,3-dime-thylmaleic anhydride (DA) protective layer to stabilize the micelles, a pH-responsive core to package hydro-phobic model drugs, and a disulfide-crosslinked interlayer to shackle the core against drug leakage under normal physiological conditions. After arriving at the tumor tissue via EPR, the targeting function could be turned on by dislodging DA groups on the surface of micelles, which allowed the drug-loaded nano-micelles to be easily phagocytized by the tumor cells, and then release the drug inside the cells induced by the increased glutathione level and acidic pH. The results indicated that the charge-conversional dual-responsive supramolecular nano -micelles showed excellent antitumor activity.

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