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Environmental response type anti-tumor nanometer medicine with high medicine loading capacity, carrier and preparation method thereof

An environment-responsive, nano-medicine technology, applied in the fields of medicine and chemistry, can solve the problem of low content of terminal functional groups

Inactive Publication Date: 2018-05-25
北京思如诺科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although TPGS has many advantages as a drug carrier material, its content of terminal functional groups is too low, and it still has many shortcomings in terms of particle size adjustment of nanoparticles and controlled drug release.

Method used

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  • Environmental response type anti-tumor nanometer medicine with high medicine loading capacity, carrier and preparation method thereof
  • Environmental response type anti-tumor nanometer medicine with high medicine loading capacity, carrier and preparation method thereof
  • Environmental response type anti-tumor nanometer medicine with high medicine loading capacity, carrier and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0082] PEG 5k -b-PMASSVE 5K synthesis method

[0083]

[0084] (1) 10 g of hydroxyl and methoxy terminated PEG with a number average molecular weight of 5000 were dissolved in 40 mL of toluene, and after azeotropic water removal twice with toluene, 4-dodecyl trithiocarbonate group- 3.23g of 4-cyanovaleric acid, 0.1g of 4-dimethylaminopyridine (DMAP) and 70ml of toluene, after complete dissolution, add 1.98g of N,N-dicyclohexylurea (DCC), and react in the dark for 96 hours at room temperature . After the reaction, dicyclohexyl urea (DCU) was removed by suction filtration, and then the filtrate was poured into excess ether, and the precipitate was collected. The resulting precipitate was dissolved in a small amount of toluene, and then precipitated with ether. Repeat this 3-5 times until the ether was colorless. The precipitate was vacuum-dried at 40° C. for 24 hours, and the obtained product was a macromolecular chain transfer agent of PEG.

[0085] (2) Under ice-water b...

Embodiment 2

[0088] Example 2 PEG 5K -b-PMACCVE 6K Synthesis

[0089]

[0090] (1) The synthetic method of PEG macromolecular chain transfer agent is the same as that of Example 1 (1).

[0091] (2) 0.5g of hydroxyethyl methacrylate (HEMA), 3.06g of VES, 0.95g of DCC, 0.094g of DMAP and 20ml of DCM were added to a 100ml round bottom flask, and stirred at room temperature overnight. DCU was removed by suction filtration, and purified by silica gel column chromatography using dichloromethane as the mobile phase to obtain the product MACCVE with a yield of 66.9%.

[0092] (3) Take 0.23g of PEG macromolecular chain transfer agent, 0.5g of MACCVE, 2mg of 4,4'-azobis(4-cyanovaleric acid) (V501), and 1ml of DMSO in a vacuum reaction tube, under liquid nitrogen freezing Vacuumize, then return to room temperature, fill with argon, repeat this process of freezing-thawing-filling with argon three times, and finally place the reaction tube in a 70°C oil bath for 48 hours under the protection of a...

Embodiment 3

[0093] Example 3 PHPMA 10K -b-PMASSVE 6K Synthesis

[0094]

[0095] (1) Take 20 mg of dodecyl trithiocarbonate, 0.6 g of N-2-hydroxypropyl methacrylamide (HPMA), and 2 mg of V501 dissolved in 2 ml of DMSO, freeze and pump three times, and react at 70 degrees Celsius for 24 hours. After the reaction is completed, pure PHPMA is obtained by acetone precipitation 10k . The reaction yield was 80%.

[0096] (2) Remove 0.3g PHPMA 10k , 1mg V501, 0.2gMASSVE were dissolved in 1ml DMSO, frozen and pumped three times and reacted at 70 degrees Celsius for 24 hours. After the reaction is completed, acetone precipitates to obtain pure PHPMA 10k -b-PMASSVE 5k . The reaction yield was 78%.

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Abstract

The invention relates to an environmental response type anti-tumor nanometer medicine with high medicine loading capacity, a carrier and a preparation method thereof. The nanometer medicine comprisesan amphiphilic polymer carrier and a medicine prodrug; the amphiphilic polymer carrier comprises a hydrophilic segment and a hydrophobic segment which are connected mutually; the hydrophilic segment comprises polyethylene glycol or poly(N-(2-hydroxypropyl)methacrylamide); the hydrophobic segment comprises D-alpha-tocopherol succinate; the medicine prodrug comprises a medicine for treating tumor aswell as a hydrophobic chain segment which is connected with the medicine through a chemical bond; and the hydrophobic chain segment comprises D-alpha-tocopherol succinate. The nanometer medicine hasthe characteristics of high medicine loading capacity, environmental responsiveness and adjustable and controllable grain size, and can achieve the properties that the tumor penetration ability is high, the tumor cell multidrug resistance is achieved, drug-resistant cells are killed in advance, tumor related fibroblast is not killed and tumor stem cells can be killed effectively according to composition of different polymers and the loaded prodrug molecule types.

Description

technical field [0001] The invention relates to the technical fields of chemistry, medicine, etc., and specifically relates to a high-drug-loading environment-responsive anti-tumor nano-medicine, a carrier and a preparation method capable of selectively regulating the tumor microenvironment, which are applied to targeted imaging and treatment of tumors. Background technique [0002] Microenvironmental factors in tumor tissue (such as abnormal blood vessels, hypoxia, low pH, high fluid pressure, changes in the expression of tumor suppressor genes and oncogenes, etc.) will cause tumor cells deep in tumor tissue to develop multidrug resistance Sex (MDR) (Lara M., J. Control Release, 2011, 155, 237-247). From the perspective of cells and genes, the multidrug resistance of tumor cells can be divided into the following three mechanisms: multidrug resistance protein 1 (common P-gp protein) encoded by MDR1 gene; Breast cancer drug resistance protein encoded by protein 1 and BCRP ge...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/60A61K47/58A61K31/704C08F293/00B82Y5/00A61P35/00
CPCA61K31/704B82Y5/00C08F293/00C08F2438/01
Inventor 喻青松甘志华张佳婧徐铭枝
Owner 北京思如诺科技有限公司
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