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A dual cell microenvironment sensitive anti-tumor drug-loaded nanocapsule and its preparation method

A cell microenvironment, drug-loaded nanotechnology, applied in the field of biomedical materials, can solve the problems of poor anti-tumor effect and safety, complicated operation, slow drug release rate from drug-loaded nanoparticles, etc. Effective, good biosafety effect

Active Publication Date: 2018-06-15
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Aiming at the above-mentioned problems existing in the prior art, the present invention provides an anti-tumor drug-loaded nanocapsule sensitive to the dual cell microenvironment and its preparation method, which can effectively solve the complex operation in the anti-tumor process and the slow drug release speed of drug-loaded nanoparticles. , the problem of poor antitumor effect and safety

Method used

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  • A dual cell microenvironment sensitive anti-tumor drug-loaded nanocapsule and its preparation method
  • A dual cell microenvironment sensitive anti-tumor drug-loaded nanocapsule and its preparation method
  • A dual cell microenvironment sensitive anti-tumor drug-loaded nanocapsule and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Example 1 Preparation of mercaptolated hyaluronic acid

[0043] Dissolve hyaluronic acid (HA) in a phosphate buffer solution with a concentration of 0.01mol / L and pH=7.4, then add 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide and 1 -Hydroxybenzotriazole, activate for 2 hours, then add cystamine dihydrochloride dropwise, stir for 12 hours, dialyze the resultant in deionized water with a 3.5kD dialysis bag for 72 hours, remove small molecular substances such as condensing agents, and finally Dithiothreitol was added to break the formed disulfide bond, purified by deionized water dialysis again, and freeze-dried to obtain thiolated hyaluronic acid; among them, hyaluronic acid, 1-(3-dimethylaminopropyl) The molar ratios of -3-ethylcarbodiimide, 1-hydroxybenzotriazole, cystamine dihydrochloride and dithiothreitol are 1:3:3:3:5;

[0044] Separately dissolve hyaluronic acid and the resulting thiolated hyaluronic acid in D 2 O, do 400 MHz 1 H-NMR scan, see the results figu...

Embodiment 2

[0045] Example 2 Preparation of vinyl-functionalized second-generation isopropylidene-protected galactopyranose

[0046] Dissolve 3-chloro-2-chloromethylpropene and NaH in anhydrous tetrahydrofuran, then add isopropylidene-protected galactopyranose, and add a small amount of KI, 18-crown-6 (18-Crown- 6) and 15-crown-5 (15-Crown-5) as a catalyst, heated to reflux at 65-70°C for 24 hours, added water to terminate the reaction, then extracted the product with ethyl acetate, and removed the organic solvent by rotary evaporation, and then used ethyl acetate Esters: n-hexane = 1:3 (volume ratio) as the eluent, purified with silica gel chromatography, and removed the organic solvent to obtain vinyl-functionalized second-generation isopropylidene protected galactopyranose; where 3-chloro- The molar ratio of 2-chloromethylpropene, NaH, isopropylidene-protected galactopyranose and catalyst is 3:3.13:1:0.0075; wherein the catalyst is KI, 18-crown ether-6 and 15-crown ether- 5 Mix the re...

Embodiment 3

[0048] Example 3 Grafting of second-generation isopropylidene protected galactopyranose on mercaptolated hyaluronic acid

[0049] The mercaptolated hyaluronic acid and vinyl-functionalized second-generation isopropylidene protected galactopyranose were dissolved in a mixture of dimethylformamide and phosphate buffer at a volume ratio of 1:3, and then Add the photoinitiator 2,2-dimethoxy-2-phenylacetophenone (DAPA), and irradiate it with ultraviolet light with a wavelength of 365nm and a power of 6W for 2h. After the reaction is completed, dialyze with deionized water to remove The unreacted small molecular substances are finally freeze-dried to obtain products; among them, mercaptolated hyaluronic acid, vinyl-functionalized second-generation isopropylidene protected galactopyranose and 2,2-dimethoxy-2-phenyl The molar ratio of acetophenone is 1:0.5:0.05.

[0050] make the resulting product 1 H-NMR scanning, nuclear magnetic spectrum such as figure 2 As shown in d, after th...

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Abstract

The invention provides a preparation method of a double-cell and microenvironment-sensitive anti-tumor drug-loaded nanocapsule. The method comprises the following steps: (1) preparing a thiol hyaluronic acid; (2) preparing vinyl-functional second-generation isopropylidene-protected galactopyranose; (3) grafting the second-generation isopropylidene-protected galactopyranose on the thiol hyaluronic acid; and (4) preparing the drug-loaded nanocapsule. The drug-loaded nanocapsule prepared by the method is high in compatibility with a tumor cell, has dual high-sensitive responsiveness on high-concentration glutathione and acid environment, achieves high-selectivity rapid release in the tumor cell, and is high in anti-tumor efficiency and good in safety.

Description

technical field [0001] The invention belongs to the technical field of biomedical materials, and in particular relates to an anti-tumor drug-loaded nanocapsule sensitive to dual cell microenvironments and a preparation method thereof. Background technique [0002] Tumor has become one of the important diseases that threaten human health. In recent years, nanomedicine preparations have shown great application potential in tumor treatment. Nanotechnology has made great progress in solving the problems of poor water solubility, low selectivity, and large toxic and side effects of traditional anticancer drugs, such as polymer nanoparticles, micelles, liposomes, and assembled dendrimers loaded with anticancer drugs. Particles, etc. These nanocarriers are composed of specific chemical structures, which can carry and protect drugs very well; at the same time, various functional modifications of nanocarriers can realize the selective degradation of particles under specific environme...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K47/36A61K31/704A61P35/00A61K31/337
CPCA61K9/19A61K9/5161A61K31/337A61K31/704A61K2300/00
Inventor 易强英马瑾顾忠伟康珂
Owner SICHUAN UNIV
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