Nanogel, preparation method of nanogel and anti-tumor nanogel drug loading system and preparation method of anti-tumor nanogel drug loading system

A technology of nanogel and summation, which is applied in antitumor drugs, liquid delivery, drug combination, etc., can solve the problems of poor water solubility and stability, and large drug side effects, and achieve good biocompatibility, tumor inhibition, and promotion of Effects of tumor targeting and endocytosis

Active Publication Date: 2015-07-08
CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, clinically used antineoplastic drugs have many defects in applicati

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  • Nanogel, preparation method of nanogel and anti-tumor nanogel drug loading system and preparation method of anti-tumor nanogel drug loading system
  • Nanogel, preparation method of nanogel and anti-tumor nanogel drug loading system and preparation method of anti-tumor nanogel drug loading system
  • Nanogel, preparation method of nanogel and anti-tumor nanogel drug loading system and preparation method of anti-tumor nanogel drug loading system

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preparation example Construction

[0080] The invention provides a kind of preparation method of nanogel, comprising the following steps:

[0081] In the presence of a phenylboronic acid initiator and a morpholine initiator, reacting L-glutamic acid oligoethylene glycol monomethyl ether ester-N-cyclic acid anhydride in an organic solvent to obtain a reaction solution;

[0082] Mixing the reaction solution with L-cystine-N-cyclic anhydride and L-phenylalanine-N-cyclic anhydride to react to obtain a nanogel;

[0083] The nanogel includes phenylboronic acid group, morpholine group, glutamic acid oligoethylene glycol monomethyl ether ester chain link, phenylalanine chain link and cystine link;

[0084] The nano gel forms a cross-linked network structure through disulfide bonds; the nano gel is a polyamino acid material.

[0085] The present invention aims to solve the problem of intelligent delivery of anti-tumor drugs. In order to overcome the shortcomings of low utilization rate and large side effects of anti-tu...

Embodiment 1

[0119] Weigh 10 g of L-glutamic acid and 20 mL of ethylene glycol monomethyl ether and mix them under stirring conditions, add 5 mL of concentrated sulfuric acid dropwise, and react under stirring conditions to obtain a reaction solution. Adjusting the pH value of the reaction solution to neutral, performing centrifugation, and then dissolving the centrifuged solid with methanol to obtain a mixed solution. Pour the mixed solution into isopropanol for centrifugation, and vacuum-dry the solid obtained by centrifugation to obtain L-glutamic acid oligoethylene glycol monomethyl ether ester.

Embodiment 2～5

[0121] According to the method of Example 1, L-glutamic acid oligoethylene glycol monomethyl ether esters were prepared respectively; the difference is that the raw materials for reacting with 10g of L-glutamic acid were: Methyl ether, 60mL triethylene glycol monomethyl ether, 80mL tetraethylene glycol monomethyl ether and 100mL pentaethylene glycol monomethyl ether.

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Abstract

The invention provides a nanogel and a preparation method thereof. The method comprises the following steps: in the presence of a phenylboronic acid initiator and a morpholine initiator, carrying out reaction on L-glutamic acid oligo-polyethylene glycol monomethyl ether ester-N-anhydride in an organic solvent to obtain reaction liquid; and mixing the reaction liquid with L-cystine-anhydride and L-phenylalanine-N-anhydride and reacting to obtain the nanogel which comprises phenylboronic acid groups, morpholine groups, glutamic acid oligo-polyethylene glycol monomethyl ether ester chain links, phenylalanine chain links and cystine chain links and form a crosslinked network structure through disulfide bonds. The invention provides an anti-tumor nanogel drug loading system and a preparation method thereof. The drug loading particles have phenylboronic acid and morpholine groups on the surfaces to promote tumor targeting and endocytosis. A nanogel structure is formed through the disulfide bonds. After targeted enrichment and endocytosis in the tumor parts, the drug loading particles can quickly release the drug to achieve the effect of inhibiting tumors.

Description

technical field [0001] The invention relates to the technical field of polymer drug carriers, in particular to a nanogel, a preparation method thereof, an anti-tumor nanogel drug-loading system and a preparation method thereof. Background technique [0002] At present, tumor has become one of the most serious diseases threatening human health. The commonly used clinical methods for treating malignant tumors include chemotherapy, radiotherapy and surgical treatment. Among them, chemotherapy is the use of chemical drugs to treat cancer, and it is the most commonly used and important treatment approach. However, the clinically used antineoplastic drugs have many defects in their application, such as poor water solubility and stability, and high toxicity and side effects. [0003] In order to solve these problems, anti-tumor drugs can be combined with drug carriers to improve the water solubility and stability of drugs; and intelligent drug carriers can be designed to control t...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K47/34A61K45/00A61P35/00C08J3/24C08J9/28C08G69/40
Inventor 丁建勋陈进进庄秀丽陈学思
Owner CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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