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Dual-targeting delivery method of pectin nanoparticles modified by folic acid

A nanoparticle, dual-targeting technology, applied in the fields of advanced nanotechnology, biopharmaceuticals, and polymer materials, can solve problems such as indigestibility, avoid sudden release, improve stability and yield, and improve biocompatibility sexual effect

Inactive Publication Date: 2018-05-01
BEIJING FORESTRY UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Pectin has become a new darling of drug carriers due to its good biological activity and biocompatibility. In recent years, researchers have found that the galectin-3 (Gal-3) ligand of pectin can recognize and interfere with tumor growth The gastrointestinal tract cannot be digested, and the pectinase secreted by the colon can degrade pectin, achieving colon targeting. At the same time, studies have found that pectin can target liver cancer, induce cell apoptosis, and inhibit cell metastasis. There are few reports on pectin as a drug carrier, especially the report based on targeted pectin drug loading. Therefore, it is particularly important to establish a new pectin drug loading system, and provide a new way

Method used

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  • Dual-targeting delivery method of pectin nanoparticles modified by folic acid
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  • Dual-targeting delivery method of pectin nanoparticles modified by folic acid

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] (1) Dissolve 1.0 g of folic acid in dimethyl sulfoxide, add 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDC) to activate the terminal carboxyl group of folic acid, and react After 30 minutes, add ethylenediamine and pyridine, stir evenly, and react in the dark for 24 hours to obtain aminofolate (FA-NH 2 ), transfer the reaction solution to the dialysis membrane, use phosphate buffer solution (pH=7.4) as the outer fluid for dialysis, dialyze overnight, change the outer fluid for dialysis every 4 hours, collect the solution in the dialysis membrane, and freeze-dry to obtain a yellow powder;

[0035] (2) Dissolve 1.0g pectin in deionized water, stir well, add EDC to react for 30 minutes, activate the carboxyl group of pectin, then add 0.1g FA-NH 2 React with 4-dimethylaminopyridine (DMAP) in the dark for 24 hours, transfer the reaction solution to the dialysis membrane, use phosphate buffer solution (pH=7.4) as the external fluid for dialysis, dialyze over...

Embodiment 2

[0041] (1) Dissolve 1.0 g of folic acid in dimethyl sulfoxide, add 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDC) to activate the terminal carboxyl group of folic acid, and react After 30 minutes, add ethylenediamine and pyridine, stir well, and react in the dark for 24 hours to obtain aminated folic acid (FA-NH2), transfer the reaction solution to the dialysis membrane, and use phosphate buffer solution (pH=7.4) as the external fluid for dialysis , dialyze overnight, change the outer dialyzed fluid every 4 hours, collect the inner solution of the dialyzed membrane, freeze-dry to obtain a yellow powder;

[0042] (2) Dissolve 1.0g of pectin in deionized water, stir well, add EDC to react for 30 minutes, activate the carboxyl group of pectin, then add 0.2g of FA-NH2 and 4-dimethylaminopyridine (DMAP) to avoid light reaction After 24 hours, the reaction solution was transferred to the dialysis membrane, and the phosphate buffer solution (pH=7.4) was used as the...

Embodiment 3

[0048] (1) Dissolve 1.0 g of folic acid in dimethyl sulfoxide, add 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDC) to activate the terminal carboxyl group of folic acid, and react After 30 minutes, add ethylenediamine and pyridine, stir well, and react in the dark for 24 hours to obtain aminated folic acid (FA-NH2), transfer the reaction solution to the dialysis membrane, and use phosphate buffer solution (pH=7.4) as the external fluid for dialysis , dialyze overnight, change the outer dialyzed fluid every 4 hours, collect the inner solution of the dialyzed membrane, freeze-dry to obtain a yellow powder;

[0049] (2) Dissolve 1.0g of pectin in deionized water, stir well, add EDC to react for 30 minutes, activate the carboxyl group of pectin, then add 0.1g of FA-NH2 and 4-dimethylaminopyridine (DMAP) to avoid light reaction After 24 hours, the reaction solution was transferred to the dialysis membrane, and the phosphate buffer solution (pH=7.4) was used as the...

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Abstract

The invention discloses a dual-targeting delivery method of pectin nanoparticles modified by folic acid. The pectin nanoparticles are prepared by the following steps: performing conjugated combinationof pectin and eight-arm polyethylene glycol, connecting the pectin with the folic acid through an amido bond, combining the eight-arm polyethylene glycol with an anti-cancer drug ursolic acid throughan ester bond to obtain a folic acid-(pectin-multi-arm polyethylene glycol)-ursolic acid prodrug, and mixing the folic acid-(pectin-multi-arm polyethylene glycol)-ursolic acid prodrug with an anti-cancer drug hydroxycamptothecine in a certain proportion so as to prepare dual-targeting nanoparticles with a core-shell structure through a self-assembly method. The dual-targeting pectin nanoparticlesprepared by the method have good biocompatibility, the pectin can be degraded by pectinase of the colon, the eight-arm polyethylene glycol is a nontoxic carrier, a burst release phenomenon does not occur in an in vivo transport process of drugs, and an in vitro release test shows good pH value responsivity. A prepared nano drug is high in drug loading rate, controllable in embedding rate and highin yield; and as a novel drug carrier, the pectin has good clinical application prospect.

Description

technical field [0001] The invention relates to a method for preparing a new type of anticancer agent with natural pectin as a drug carrier, specifically a dual-target delivery method of folic acid-modified pectin nanoparticles, which belongs to the fields of polymer material application, advanced nanotechnology and biopharmaceuticals. Background technique [0002] Pectin widely exists in the fruits, roots, stems, and leaves of plants. It is a component of the cell wall and forms a bond between adjacent cells, which makes the plant tissue cells tightly bonded together. Pectin is a linear polysaccharide polymer, mainly composed of galacturonic acid, containing hundreds to about 1,000 anhydrogalacturonic acid residues, and its corresponding average relative molecular mass is 50,000-150,000. It is mainly used in the food processing industry , such as gelling agents, emulsifiers and thickeners. Pectin has become a new darling of drug carriers due to its good biological activity...

Claims

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Application Information

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IPC IPC(8): A61K47/61A61K47/60A61K47/54A61K31/56A61K31/4745A61K9/19A61K47/36A61P35/00
CPCA61K9/19A61K31/4745A61K31/56A61K47/36A61K2300/00
Inventor 雷建都刘彦雪曹永丽郑督罗敏孔天娇杨子萱肖萌
Owner BEIJING FORESTRY UNIVERSITY
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