Advanced Search

    FENG Huiru, LIU Yanqin, DONG Ying, YU Xiangxiang, GONG Kai. Preparation of Reduction-Responsive Liver-Targeted Polymeric Micelles and Their Drug-Loading Properties[J]. Journal of Functional Polymers, 2022, 35(6): 566-574. doi: 10.14133/j.cnki.1008-9357.20220329001
    Citation: FENG Huiru, LIU Yanqin, DONG Ying, YU Xiangxiang, GONG Kai. Preparation of Reduction-Responsive Liver-Targeted Polymeric Micelles and Their Drug-Loading Properties[J]. Journal of Functional Polymers, 2022, 35(6): 566-574. doi: 10.14133/j.cnki.1008-9357.20220329001

    Preparation of Reduction-Responsive Liver-Targeted Polymeric Micelles and Their Drug-Loading Properties

    • Firstly, using hepta(6-azido-6-deoxy)-β-cyclodextrin and butyl-3-ynyl-β-d-galactoside as the raw material, galactose-β-cyclodextrin (Gal7-CD) with liver-targeting function was synthesized by Click reaction. Secondly, using cystamine dihydrochloride and octadecanoic acid as the raw material, cystamine octadecyl amide (NH2-SS-SA) was obtained through amino protection, acylation reaction and deprotection reaction. Next, adamantyl polyethylene glycol amine (Ad-PEG1000-NH2) was synthesized by using the acylation reaction of adamantanecarboxylic acid and amino polyethylene glycol, and then, which reacted with succinic anhydride to obtain adamantyl polyethylene glycol succinic acid (Ad-PEG1000-COOH). Then NH2-SS-SA reacted with Ad-PEG1000-COOH to obtain adamantyl polyethylene glycol amine octadecanamide (Ad-PEG1000-SS-C18). Finally, using dialysis method, Gal7-CD and Ad-PEG1000-SS-C18 self-assembled to form amphiphilic polymer through host-guest self-assembly, and then form polymer micelle (Gal7-SS-C18). Doxorubicin (DOX) was then used as a model drug to incorporate into Gal7-SS-C18 micelles. The particle size of polymer micelles and drug-loaded polymer micelles were determined by dynamic light scattering (DLS) to be (169.2±1.3) nm and (177.9±3.0) nm, respectively. The drug-loading capacity of the drug-loaded polymer micelles was measured by UV-Vis spectrophotometer to be (21.2±0.7)% and the encapsulation efficiency was (71.1±0.5)%. In the in vitro release experiment, the cumulative release of drug-loaded polymer micelles was lower in the simulated normal physiological environment of PBS, while the cumulative DOX release reached 82.38% within 48 h in the simulated tumor reduction microenvironment of PBS. The cytotoxicity and antitumor activity of polymer micelles were evaluated by using liver cancer cells (HepG2) and normal tissue cells (HEK-293) as cell models. The research results show that the polymer micelles have good biocompatibility. The drug-loaded polymer micelles show good targeting and controllable release properties, which have better tumor inhibition ability than free DOX.
    • loading

    Catalog

      /

      DownLoad:  Full-Size Img  PowerPoint
      Return
      Return