Nanometer carrier system for tumor in-situ assembly, medicine carrying system and application
A nanoparticle and polyethylene glycol technology, applied in the direction of anti-tumor drugs, nano-drugs, nano-technology, etc., can solve the problems of unsatisfactory drug delivery, the inability of drugs to reach extracellular target sites, and the inability to exert anti-tumor effects. Good biocompatibility and degradability, enhanced enrichment and retention, effects of avoiding uptake
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Embodiment 1
[0053] Example 1: Synthesis and characterization of polyethylene glycol-polylactic acid modified with bioorthogonal groups
[0054] 1. Synthesis of polyethylene glycol-polylactic acid modified by bioorthogonal groups
[0055] DA Cys-PEG-b-PLA is a tert-butoxycarbonyl-protected cysteine (Boc-Cys) and aminated polyethylene glycol-polylactic acid through an amidation reaction, further deprotected by Boc and treated with 2,3-diol Methylmaleic anhydride shielded cysteine residues obtained.
[0056] DA The synthetic route of Cys-PEG-b-PLA polymer material is as follows figure 1 shown.
[0057] Preparation and pretreatment of the required components include:
[0058] (1) Synthesis of tert-butoxycarbonyl-protected cysteine:
[0059] To a 100 mL clean round-bottomed flask, add cysteine (5 g, 0.029 mol) and 50 mL of ultrapure water, and add magnetic stirring to dissolve cysteine. Weigh NaHCO again 3 (2.436 g, 0.029 mol) was added to the above cysteine aqueous solution, c...
Embodiment 2
[0073] Example 2: Nanoparticles and applications of polyethylene glycol-polylactic acid modified at the end of bioorthogonal groups
[0074] 1. Preparation of D-NP and C-NP nanoparticles
[0075] Two kinds of bioorthogonal group surface-modified nanoparticles and their drug-loaded nanoparticles were prepared by nanoprecipitation method or single emulsification method. The specific methods are as follows:
[0076] Weigh 10mg DA Cys-PEG-b-PLA or 10 mg CBT-PEG-b-PLA were dissolved in 1 mL of DMSO, respectively. After vortexing to dissolve completely, the material solution was dropped into the aqueous phase (10 mL, 1×PBS, pH 7.4) and stirred for 2 h. Two types of nanoparticles were obtained. The particle solution was put into a dialysis bag with MWCO=14000Da and put into 1×PBS (pH 7.4, 2L) for dialysis overnight. Then use YM-30 ultrafiltration centrifuge tube (Millipore, MWCO5000Da) for ultrafiltration concentration to prepare D-NP and C-NP nanoparticles.
[0077] 2. Character...
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