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Block copolymer, block copolymer drug-loaded micelle as well as preparation method and application of block copolymer drug-loaded micelle

A technology of block copolymer and drug-loaded micelle, applied in the field of biomedicine

Active Publication Date: 2022-03-11
SOUTHERN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, it is still a challenge to develop nano-drug carriers that can respond sensitively to the characteristics of the tumor microenvironment and produce rapid and controlled release.

Method used

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  • Block copolymer, block copolymer drug-loaded micelle as well as preparation method and application of block copolymer drug-loaded micelle
  • Block copolymer, block copolymer drug-loaded micelle as well as preparation method and application of block copolymer drug-loaded micelle
  • Block copolymer, block copolymer drug-loaded micelle as well as preparation method and application of block copolymer drug-loaded micelle

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] Embodiment 1 provides a kind of block copolymer, the structural formula of described block copolymer is as follows, and preparation method comprises the following steps:

[0061]

[0062] 1) The preparation of TAMA, the synthetic route is as follows:

[0063]

[0064] S1. Dissolve 1.8g of N,N-dimethylethanolamine (20.0mmol) in 40mL of anhydrous tetrahydrofuran, then add a catalytic amount of dibutyltin dilaurate (40μL), stir for 15 minutes, and slowly add 3.8g of methyl Isocyanoethyl acrylate (24.0 mmol). After stirring at room temperature for 4 h, the reaction mixture was concentrated under reduced pressure, separated and purified through a basic alumina column to obtain 4.2 g of a colorless oily product (yield: 85%).

[0065] S2. Dissolve the product of step S1 (4.2g, 17.2mmol) in anhydrous tetrahydrofuran (30mL), slowly add 2.7g methyl iodide (18.9mmol) dropwise after ice bath for 15 minutes, stir for 30 minutes, and continue to stir at room temperature for 2h...

Embodiment 2

[0072] This embodiment 2 provides a new block copolymer, the difference from embodiment 1 is that the monomers are different, the structural formula is as follows, and the preparation method is as follows:

[0073]

[0074] 83mg benzylacrylamide (0.51mmol), 200mg TAMA (0.51mmol), 238mg polyethylene glycol methyl ether acrylate (Mw: 300) (0.68mmol) and 1.5mg azobisisobutyronitrile (0.009mmol), 3.757 mg of 2-cyanopropyl-2-ylbenzodisulfide (0.017 mmol) was dissolved in 600 μL of N,N-dimethylformamide, then transferred to a polymerization tube, degassed by three freeze-thaw cycles, and finally in vacuo Lower seal. The polymerization tube was then immersed in a preheated 65°C oil bath. After stirring for 10 h, the polymerization tube was placed in liquid nitrogen for a while, and the lid was opened to terminate the polymerization. The reaction mixture was precipitated in 100 mL of ether, then the precipitate was dissolved in a small amount of dimethylformamide and precipitated...

Embodiment 3

[0076] Example 3 provides a block copolymer drug-loaded micelle, which includes the block copolymer prepared in Example 1 and an active pharmaceutical ingredient, where the active pharmaceutical ingredient is camptothecin. The preparation method of described block copolymer drug-loaded micelle comprises the steps:

[0077] The 5mg PEG prepared by embodiment 1 45 -b-P(QPBA 0.78 -co-TAMA 0.22 ) 109 Co-dissolve with camptothecin in 1 mL of a suitable organic solvent (dioxane), quickly add to vigorously stirred PBS (9 mL, 10 mM, pH 7.4), continue stirring for 7 minutes, transfer the sample to a dialysis bag, and Water dialysis to remove organic solvents and unloaded drug.

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Abstract

The invention provides a block copolymer, a block copolymer drug-loaded micelle and a preparation method of the block copolymer drug-loaded micelle. The block copolymer comprises a hydrophilic block and a copolymerization block which are covalently connected, wherein the copolymerization block is prepared from a cationic monomer and a pi structure monomer. The cationic monomer and the monomer with the pi structure are introduced into the block copolymer, so that the block copolymer has high stability and drug loading universality. A plurality of cation-pi interaction regions can be formed in the block copolymer, so that the whole copolymer has higher stability, and meanwhile, a cation-drug compound formed by a cation unit and a drug molecule enables the drug-loading micelle to have good drug-loading stability, so that the drug-loading micelle has good drug-loading stability. The medicine leakage in the storage process and the early release of the medicine in blood circulation are greatly reduced, and the toxic and side effects of the medicine are reduced.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to a block copolymer, a block copolymer drug-loaded micelle and a preparation method thereof. Background technique [0002] Despite the rapid development of modern medicine and related basic research, tumors are still an important medical and health problem that threatens human survival. At present, surgery and chemotherapy, as the two most important treatment methods, are still difficult to solve the problems of tumor metastasis, recurrence and drug resistance. Although traditional small molecule drug chemotherapy can also achieve certain curative effect in tumor treatment, its poor selectivity and low efficiency have brought great toxic and side effects to traditional chemotherapy methods and greatly reduced the quality of life of chemotherapy patients. . Secondly, the problem of low drug delivery efficiency will lead to the generation of tumor drug resistance, wh...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08F293/00A61K9/107A61K45/00A61K47/34A61P31/04A61P31/10A61P31/12A61P35/00
CPCC08F293/00A61K47/34A61K9/1075A61K45/00A61P35/00A61P31/12A61P31/04A61P31/10Y02A50/30
Inventor 汪枭睿谭国柱王钰
Owner SOUTHERN MEDICAL UNIVERSITY
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