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Nanoparticles for promoting tumor coagulation and enzyme/ATP dual responsive drug release, and preparation method and application of nanoparticles

A nanoparticle, drug-loaded nanotechnology, applied in the direction of anti-tumor drugs, pharmaceutical formulations, medical preparations of non-active ingredients, etc.

Active Publication Date: 2021-02-05
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, how to quickly kill cancer cells by inducing blood coagulation in tumor blood vessels through more precise, effective and convenient ideas and methods still needs research and breakthroughs

Method used

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  • Nanoparticles for promoting tumor coagulation and enzyme/ATP dual responsive drug release, and preparation method and application of nanoparticles
  • Nanoparticles for promoting tumor coagulation and enzyme/ATP dual responsive drug release, and preparation method and application of nanoparticles
  • Nanoparticles for promoting tumor coagulation and enzyme/ATP dual responsive drug release, and preparation method and application of nanoparticles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0084] (1) Preparation of core layer PLL-FPBA drug-loaded nanoparticles

[0085] 100mgε-polylysine hydrochloride (PLL·HCl, weight average molecular weight 5×10 3 g / mol) was dissolved in 20mL deionized water, 44mg FPBA (3-fluoro-4-carboxyphenylboronic acid) was dissolved in 8.8mL deionized water, after the two solutions were mixed (the molar ratio of PLL and FPBA was 1:10), Add 560 mg of activator 4-(4,6 dimethoxytriazin-2-yl)-4-methylmorpholine hydrochloride (DMTMM, molar ratio DMTMM:PLL·HCl=3:1), stir at room temperature After 24 hours of reaction, the solution was transferred to a dialysis bag (MWCO: 2kDa) and dialyzed with deionized water for 7 days, and the amphiphilic polymer PLL-FPBA was obtained after freeze-drying. PLL-FPBA 1 HNMR spectrum as figure 2 As shown, the substitution degree of FPBA is 36.7%. The critical micelle concentration CMC value of PLL-FPBA measured by fluorescence spectroscopy was 5.9 μg / mL, as image 3 shown.

[0086] Dissolve 20mg of PLL-FPB...

Embodiment 2

[0100] (1) Preparation of core layer PLL-FPBA drug-loaded nanoparticles

[0101] 100mgε-polylysine hydrochloride (PLL·HCl, weight average molecular weight 1×10 4 g / mol) was dissolved in 20mL deionized water, 22mg FPBA was dissolved in 4.4mL deionized water, and the two solutions were mixed (the molar ratio of PLL and FPBA was 1:5). Add 560 mg of activator 4-(4,6 dimethoxytriazin-2-yl)-4-methylmorpholine hydrochloride (DMTMM, molar ratio DMTMM:PLL·HCl=3:1), stir at room temperature After 24 hours of reaction, the solution was transferred to a dialysis bag (MWCO: 2kDa) and dialyzed with deionized water for 7 days, and the amphiphilic polymer PLL-FPBA was obtained after freeze-drying. 1 H NMR test showed that the substitution degree of FPBA was 10%. The critical micelle concentration CMC value of PLL-FPBA measured by fluorescence spectroscopy was 8.0μg / mL.

[0102] Dissolve 20mg of PLL-FPBA in 20mL DMSO / HCl (volume ratio, 0.1M HCl / DMSO=1:4), stir to dissolve and add 5mg of ant...

Embodiment 3

[0110] (1) Preparation of core layer PLL-FPBA drug-loaded nanoparticles

[0111] 100mgε-polylysine hydrochloride (PLL·HCl, weight average molecular weight 3×10 3 g / mol) was dissolved in 20 mL of deionized water, 88 mg of FPBA was dissolved in 17.6 mL of deionized water, after the two solutions were mixed (the molar ratio of PLL and FPBA was 1:20), 560 mg of activator 4-(4,6 di Methoxytriazin-2-yl)-4-methylmorpholine hydrochloride (DMTMM, molar ratio DMTMM:PLL·HCl=3:1), stirred and reacted at room temperature for 24h, after the reaction was completed, the solution was transferred to dialysis The bag (MWCO: 2kDa) was dialyzed with deionized water for 7 days, and the amphiphilic polymer PLL-FPBA was obtained after freeze-drying. 1 H NMR test showed that the substitution degree of FPBA was 50%. The critical micelle concentration CMC value of PLL-FPBA measured by fluorescence spectroscopy was 3.3μg / mL.

[0112] Dissolve 20mg of PLL-FPBA in 20mL DMSO / HCl (volume ratio, 0.1M HCl / D...

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Abstract

The invention provides nanoparticles for promoting tumor coagulation and enzyme / ATP dual responsive drug release as well as a preparation method and application of the nanoparticles. According to thenanoparticles, cross-linked hyaluronic acid modified by methacrylic anhydride is used as a shell layer, drug-loaded nanoparticles formed by self-assembly after polylysine is modified by 3-fluorine-4-carboxyphenylboronic acid are used as a core layer, and CaCO3 nanoparticles are generated in situ; after targeting tumor tissues through administration, Ca <2+> is rapidly released in a tumor acidic environment, tumor blood vessel coagulation is induced, sugar supply of cancer cells is blocked, and residual lactic acid of tumors is neutralized and decomposed, and the resistance of lactation to cancer cell apoptosis due to sugar deficiency is eliminated; then, a nano-carrier entering the cancer cells escapes from endosome / lysosome to cytoplasm under the proton sponge effect of PLL, and acts withadenosine triphosphate (ATP) to quickly release drugs, so that the cancer cells are quickly killed by cooperation of tumor coagulation, deacidification and ATP response drug release, and important significance for tumor treatment is achieved.

Description

technical field [0001] The invention belongs to the field of biomedical materials and drug controlled release, and in particular relates to a nanoparticle capable of promoting tumor coagulation and enzyme / ATP dual-responsive drug release, as well as its preparation method and application. Background technique [0002] With the rising morbidity and mortality of cancer, cancer has become the main killer threatening human health. At present, the clinical methods of treating cancer mainly include surgery, radiotherapy, chemotherapy and immunotherapy. Surgical treatment is the first choice for early cancer, but chemotherapy is mainly used for advanced metastatic tumors, and drugs interfere with cancer cell division to inhibit cancer cell growth. Since small molecule chemotherapeutic drugs will be distributed throughout the body after entering the body, they lack specificity, so they will kill normal tissue cells while killing cancer cells, and the side effects are extremely seve...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/34A61K47/24A61K47/69A61K31/416A61K31/337A61K31/704A61K33/10A61P35/00
CPCA61K9/5146A61K9/5123A61K47/6939A61K31/416A61K31/337A61K31/704A61K33/10A61P35/00A61K2300/00
Inventor 赵剑豪吴琰黎华强容建华
Owner JINAN UNIVERSITY
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