A dendritic polymer drug delivery system with high tumor recognition and environment-responsive drug release capabilities and its construction method
A technology of dendrimers and environmental response, applied in the direction of antineoplastic drugs, nano-drugs, drug combinations, etc., can solve problems such as lack of selectivity, defects in physical and chemical properties, and influence on drug efficacy, so as to optimize in vivo behavior and reduce toxic and side effects , the effect of prolonging the circulation time in the body
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Embodiment 1
[0047] Embodiment 1: Provide a specific compound (folic acid-polyethylene glycol-polyamide-amine-hydrazone bond-doxorubicin) of a dendrimer drug delivery system with high tumor recognition and environmental response drug delivery capabilities / FA-PEG-PAMAM-hyd-DOX, abbreviated as FPP-hyd-DOX)
[0048] For the structure of this particular complex see Figure 10 As shown, it is centered on the dendrimer 1, and the hydrophilic block 2 of the unmodified ligand and the targeting ligand chain are connected to its surface, and the targeting ligand chain is a hydrophilic block-targeting ligand chain. Ligand 3 chimera; antitumor drug 4 is linked to the surface of dendrimer 1 through acid-sensitive chemical bond 5 . The dendritic polymer in this example is polyamide-amine 4th generation PAMAM, the hydrophilic block is polyethylene glycol PEG, the targeting ligand X is folic acid FA, and the chimerism between polyethylene glycol PEG and folic acid FA The targeting ligand chain PEG-FA i...
Embodiment 2
[0064] With the method of embodiment 1, change the feed molar ratio of FA-PEG-NHS and PP-hyd-DOX to be 32:1, and CH 3 The molar ratio of O-PEG-NHS and PP-hyd-DOX was 32:0.5, and the nano drug loading system with similar number of specific folic acid ligands, PEGylation degree and drug loading capacity was prepared.
Embodiment 3
[0066] With the method of embodiment 1, the molecular weight of PEG in FA-PEG-NHS is between 2000-5000, CH 3 The molecular weight of PEG in O-PEG-NHS is between 2000-5000, and the PEG chain in FA-PEG-NHS is equal to or longer than CH 3 PEG chains in O-PEG-NHS.
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