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Preparation method of novel water-soluble nanoparticles

A nanoparticle, water-soluble technology, applied in the field of biopharmaceuticals and nanometers, can solve the problems of high drug loading, water solubility difference, low bioavailability, etc., and achieves strong targeting, low toxicity and good biocompatibility. Effect

Inactive Publication Date: 2016-08-31
BEIJING FORESTRY UNIVERSITY
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  • Abstract
  • Description
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AI Technical Summary

Problems solved by technology

[0004] The purpose of the present invention is to address the deficiencies in the prior art and provide a new method for preparing water-soluble nanoparticles. PET-UA can self-assemble into nanoparticles in an aqueous medium to solve the problem of UA's water-soluble phase difference and low bioavailability. The problem is that the self-assembly process encapsulates DHA or HCPT at the same time to form PET-UA(DHA)•NPs and PET-UA(HCPT)•NPs, which increases the drug loading capacity of the system, and the encapsulated drugs have a wide choice, a large number of hydrophobic Drugs are self-assembled and packaged at the same time. The particle size of the nanoparticles is not affected much before and after the packaged drugs. Pectin is used as the drug carrier, which has good targeting and high drug loading, and avoids incomplete release of drugs and Toxic and side effects of sudden release on patients

Method used

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  • Preparation method of novel water-soluble nanoparticles
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  • Preparation method of novel water-soluble nanoparticles

Examples

Experimental program
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Embodiment 1

[0023] Embodiment 1, a kind of preparation method of novel water-soluble nanoparticles:

[0024] (1) Acetylation of PET

[0025] Take 1g of PET (esterification degree 50%~80%), slowly add 25ml of glacial acetic acid, 15ml of acetic anhydride and 0.6ml of sulfuric acid, react in ice bath for a period of time, then raise the temperature to 50°C, stir until the solution is clear, and the mixture is rotary evaporated , washed with ethanol until neutral, freeze-dried to obtain acetylated pectin powder A.

[0026] (2) Synthesis of PET-UA

[0027] Take 0.1g of PET in (1), slowly add it into a 25ml round bottom flask containing 4ml of pyridine, and sonicate for 10min, stir and dissolve for 20min, then add 0.1g of activator 1-(3-dimethylaminopropyl)- 3-Ethylcarbodiimide hydrochloride (EDC), 0.02g catalyst 4-dimethylaminopyridine (DMAP), stirred for 30min, added 0.1g of UA, and reacted in water bath for 48h to obtain PET-DHA polymer mixture.

[0028] (3) Purification of PET-UA

[00...

Embodiment 2

[0032] Embodiment 2, a kind of preparation method of novel water-soluble nanoparticles:

[0033] In this example, through the same synthesis method and steps as in Example 1, PET 0.1g, UA 0.5g, the measured particle size is 20-80nm.

Embodiment 3

[0034] Embodiment 3, a kind of preparation method of novel water-soluble nanoparticles:

[0035] In this example, through the same synthesis method and steps as in Example 1, PET 0.1g, UA 0.05g, the measured particle size is 30-130nm.

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Abstract

The invention discloses a preparation method of novel water-soluble nanoparticles. The method comprises the following steps: pectin (PET) is used as a carrier; esterification is carried out between carboxyl of pectin and hydroxy of ursolic acid (UA) in order to form macromolecule micelle; self assembly is carried out in order to form nanoparticles PET-UA.NPs, a dihydroartemisinin hydrophobic medicament or 10-hydroxycamptothecin is enveloped during the process of self assembly, in order to form PET-UA(DHA).NPs or PET-UA(HCPT).NPs, and the nanoparticles with core-shell structures are formed. The water-soluble nanoparticles are used as a nanometer medicament with a slow release function, and the nanoparticles have the advantages of adjustable drug loading, good targeting ability, good stability, good biocompatibility, and low toxicity. The nanoparticles belong to the fields of biological pharmacy and nanometer technology, and the method has the advantages of simple preparation technology, operation convenience, and short period.

Description

technical field [0001] The invention belongs to the fields of biopharmaceuticals and nanotechnology, relates to a drug delivery system, and in particular to a preparation method of novel water-soluble nanoparticles. Background technique [0002] Ursolic acid (UA for short) and Dihydroartemisinin (DHA for short) are insoluble in water, and direct oral administration has a certain degree of toxic and side effects on the body. They cannot treat a single cancer and have no effect on cancer cells. Recognition ability, killing cancer cells and normal cells at the same time, and poor bioavailability, these limit the wide application of UA in the field of pharmacy, therefore, to solve the problem of its water solubility, increase drug stability, improve the The slow-release killing ability of a single cancer cell is the key to the clinical application of UA. [0003] Pectin is a polysaccharide macromolecular substance present in plant cell walls. Widely present in apples, citrus a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K31/366A61K31/4745A61K47/36A61K47/28A61P35/00
CPCA61K9/5161A61K31/366A61K31/4745A61K31/56A61K2300/00
Inventor 雷建都刘彦雪刘静何静王璐莹晋禄禄
Owner BEIJING FORESTRY UNIVERSITY
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