4.8 Article

Cross-Linked Small-Molecule Micelle-Based Drug Delivery System: Concept, Synthesis, and Biological Evaluation

Journal

CHEMISTRY OF MATERIALS
Volume 28, Issue 21, Pages 7757-7764

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.chemmater.6b02965

Keywords

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Funding

  1. National Natural Science Foundation of China [21372170, 51673130]
  2. Recruitment Program of Global Young Experts of China
  3. Excellent Young Foundation of Sichuan Province [2014JQ0032, 2016JQ0028]
  4. Applied Basic Research Project of Sichuan Province [2015JY0279]
  5. Setup Foundation of Sichuan University [YJ201317]

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Lessons from the covalent capture of small-molecule self-assemblies (monomer molecular weight of <500.0) are applied to grow a generic cross-linked small-molecule micelle-based drug delivery system (CSM-DDS), which has significant advantages over the popular polymeric micelle-based drug delivery systems in terms of drug loading, stability, monomer purity, and cost of preparation. A proof-of-concept CSM-DDS constructed by one-step synthesized amphiphile 1 with anticancer drug gemcitabine confirms the feasibility of the new strategy via its high drug loading content (up to 58%), robust stability, superior predictable biosafety, facile functionalization, and remarkable anticancer activity both in vitro and in vivo.

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