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Drug-loaded nanoparticles capable of efficiently delivering siRNA as well as preparation method and application of drug-loaded nanoparticles

A drug-loaded nano-delivery technology, applied in the fields of nanomaterials and nano-biomedicine, can solve the problems that nano-delivery systems are difficult to break through cell defense properties, nano-delivery systems have no tumor targeting function, and cannot achieve tumor cell targeting. , to achieve the effect of enhancing delivery efficiency, improving stability and enhancing activity

Active Publication Date: 2022-03-25
HUNAN PROVINCIAL PEOPLES HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Patent CN112353950A discloses a "drug-loaded" siRNA nano-delivery system, which uses quercetin and siRNA to self-assemble through π-π bonds, hydrophilic-hydrophobic interactions, and hydrogen-bond interactions to form nano-drugs, in order to realize the delivery of quercetin and siRNA Synergistic effect on tumor cells, but the siRNA nano-delivery system has obvious defects: 1) the stability of siRNA loaded only by quercetin is not high, it is easy to be cleaved during human transportation, and the delivery efficiency is not high; 2) quercetin After the nanosystem formed by the protein and siRNA is ingested by the cell, the lysosome in the cell can remove exogenous macromolecular substances, and the nuclease rich in the lysosome can efficiently digest and decompose the siRNA entering the cell , it will make it difficult for the nano-delivery system to break through the defense properties of the cells themselves, and it will be difficult to further inhibit tumor cells; 3) The nano-delivery system does not have tumor targeting function and cannot achieve the targeting effect on tumor cells

Method used

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  • Drug-loaded nanoparticles capable of efficiently delivering siRNA as well as preparation method and application of drug-loaded nanoparticles
  • Drug-loaded nanoparticles capable of efficiently delivering siRNA as well as preparation method and application of drug-loaded nanoparticles
  • Drug-loaded nanoparticles capable of efficiently delivering siRNA as well as preparation method and application of drug-loaded nanoparticles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Quercetin and Zn 2+ Preparation of Complex (ZnQ)

[0041] Add 0.3mmol quercetin and 2.5mL absolute ethanol to a 100mL three-necked flask equipped with a stirrer and a condenser, heat and stir to dissolve to obtain a yellow clear solution, add 0.6mmol anhydrous Na2CO3 to the solution and continue stirring for 1h, Then add 0.6mmol anhydrous Zn(Ac) 2 Reflux and stir for 4 h, filter with suction to obtain a light brown solid, wash the solid with hot absolute ethanol and dry it to obtain ZnQ.

Embodiment 2

[0043] Preparation of phenylboronic acid-hyaluronic acid conjugate (BHA)

[0044] Add 0.5mmol of hyaluronic acid with a molecular weight of 48kDa to a 100mL eggplant-shaped bottle, add 20mL of deionized water to dissolve, put in 0.75mmol of EDC and 0.75mmol of NHS, after completely dissolving, adjust the pH to 4-5 and activate for 0.5h; weigh 4 -Aminomethylphenylboronic acid 0.5mmol and added to the above mixture, sealed at room temperature for 24h (pH maintained at 4-5), dialyzed for 4 days to remove unreacted 4-aminomethylphenylboronic acid and other impurities, etc., using a freeze dryer After lyophilization, about 4 mg of the obtained sample was weighed and dissolved in 0.5 mL of heavy water to obtain a BHA solution.

Embodiment 3

[0046] Preparation of drug-loaded nanoparticles (siRNA / ZnQ-BHA) for efficient delivery of siRNA

[0047] Take 10 μL of ZnQ (500 mM) prepared in Example 1 and 10 μL of siRNA (4.8 μM) and mix well, and incubate at 37°C for 1 h; then add 20 μL of BHA prepared in Example 2 dropwise and mix well, and incubate at 37°C for 1 h; finally, gradually 20 μL of HEPES buffer was added dropwise and mixed evenly, and incubated at 37° C. for 1 hour to obtain siRNA / ZnQ-BHA nanoparticles (final pH=7.4), which were stored at 4° C. for future use.

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Abstract

The invention provides a drug-loaded nanoparticle capable of efficiently delivering siRNA and a preparation method and application thereof.The siRNA drug-loaded nanoparticle is formed by self-assembly of Zn < 2 + >, quercetin, siRNA and phenylboronic acid-hyaluronic acid conjugates, after Zn < 2 + > and quercetin are complexed, siRNA is entrapped to form a drug-loaded inner core, and the drug-loaded inner core is coated with the quercetin; and then the phenylboronic acid-hyaluronic acid conjugate wraps the drug-loading core to assemble the drug-loading nanoparticles capable of efficiently delivering siRNA. According to the drug-loaded nanoparticles, a novel'drug-loaded 'inner core is formed through the coordination and complexation of Zn < 2 + >, quercetin and siRNA, HA modified by phenylboronic acid groups is used as a shell, the dual-acid-sensitive combined drug-loaded nanoparticles are constructed, and co-delivery and synergistic treatment of SIRT1-targeted gene drugs and small molecular drugs can be achieved; meanwhile, the drug-loaded nanoparticles contain double acid-sensitive functional groups of zinc phosphate coordinate bonds and phenylboronic acid ester bonds, and are rapidly broken in an intracellular lysosome acid environment, so that the carrier is effectively disintegrated, and osmotic pressure in the lysosome is induced to rise to promote efficient delivery and release of drugs.

Description

technical field [0001] The invention relates to the fields of nanomaterials and nanobiomedicine, in particular to a drug-loaded nanoparticle for efficiently delivering siRNA and its preparation method and application. Background technique [0002] Bladder cancer is a common malignancy. According to the statistics of cancer in the United States in 2018, there are about 77,000 new cases in the United States alone, and the incidence rate is on the rise. The high cost of treatment and high mortality rate of bladder cancer has become a serious social problem worldwide. Adjuvant chemotherapy can reduce the recurrence rate of cancer and prevent or delay the progression of cancer. However, conventional chemotherapy methods lack targeting, and the severe side effects produced greatly reduce patient compliance and quality of life; in comparison, Combination medication can significantly reduce the dosage of a single drug and reduce the occurrence of toxic and side effects, which has ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/36A61K47/12A61K47/02A61K31/352A61K48/00A61P35/00B82Y5/00B82Y40/00
CPCA61K9/5192A61K9/5161A61K9/5123A61K9/5115A61K31/352A61K48/005A61P35/00B82Y5/00B82Y40/00A61K2300/00Y02A50/30
Inventor 陈佳李龙吴志颖张跃玟
Owner HUNAN PROVINCIAL PEOPLES HOSPITAL
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