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Polymer nanosphere with function of target recognition of cancer cells and preparation method of polymer nanosphere

A technology for targeting and identifying cancer cells, which can be used in medical preparations, drug combinations, and pharmaceutical formulations that are not active ingredients.

Active Publication Date: 2017-07-07
TSINGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the above methods all have defects such as complex material synthesis process, high cost, poor versatility, and inability to achieve large-scale production.

Method used

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  • Polymer nanosphere with function of target recognition of cancer cells and preparation method of polymer nanosphere
  • Polymer nanosphere with function of target recognition of cancer cells and preparation method of polymer nanosphere
  • Polymer nanosphere with function of target recognition of cancer cells and preparation method of polymer nanosphere

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Embodiment 1, the preparation of the polymer nanosphere of biotin surface modification

[0060] according to figure 1 The schematic diagram for the preparation of biotin-surface-modified polymer nanospheres is shown:

[0061] 1) According to figure 1 Step (a) prepares the polymer nanosphere that surface contains amine group, concrete steps are as follows:

[0062] Dissolve emulsifier 0.2g sodium dodecyl sulfate (SDS) and 0.1g nonylphenol polyoxyethylene ether (OP-10) in water 90mL to obtain emulsifier aqueous solution; initiator azobisisobutyronitrile ( AIBN) is dissolved in a mixed solvent of other copolymerized monomer styrene (styrene), amine-containing monomer dimethylaminoethyl methacrylate (DMAEMA) and cross-linking monomer divinylbenzene (AIBN, styrene The mass ratio of DMAEMA and divinylbenzene is 0.2:6.7:3.3:0.03) to obtain a monomer solution. Pour the emulsifier aqueous solution into a three-neck flask equipped with a spherical condenser and a stirring pad...

Embodiment 2

[0068] Embodiment 2, the preparation of the polymer nanosphere of biotin surface modification

[0069] 1) Preparation of polymer nanospheres containing amine groups on the surface:

[0070] Dissolve 0.2g of cetyltrimethylammonium bromide, 0.1g of nonylphenol polyoxyethylene ether (OP-10) and 0.2g of initiator azobisisobutylamidine hydrochloride in 90mL of water to obtain Aqueous solution containing an emulsifier; other copolymerizable monomers butyl acrylate, methyl methacrylate, amine-containing monomer diethylaminoethyl methacrylate and cross-linking monomer N,N-methylenebis Acrylamide was mixed in a mass ratio of 4:2.5:3.5:0.03 to obtain a monomer solution. Pour the aqueous solution containing the emulsifier into a three-neck flask equipped with a spherical condenser and a stirring paddle, and then drop the monomer solution into the water phase (the mass ratio of the emulsifier aqueous solution to the monomer solution is 9:1). The mixed solution was pre-emulsified using h...

Embodiment 3

[0075] The preparation of the polymer nanosphere of embodiment 3, folic acid surface modification

[0076] 1) Preparation of polymer nanospheres containing amine groups on the surface: the same as in Example 1.

[0077] 2) Synthesis of aminated folic acid: Dissolve folic acid in the organic solvent DMF (10 mg folic acid dissolved in 1 mL DMF), and add N,N'-disuccinimide carbonate equivalent to four times the molar amount of folic acid in an ice-water bath (DSC), under the catalysis of triethylamine (the molar ratio of triethylamine and folic acid is 2:1), react at room temperature (25°C) for 12 hours. The product precipitate was washed three times with diethyl ether, isopropanol and diethyl ether, respectively. Re-dissolve the obtained product in DMF (dissolve 10 mg of product in 1 mL of DMF), then back-drop the solution into excess ethylenediamine (equivalent to 2 times the molar amount of folic acid), and react at room temperature (25°C) for 24 hours . Precipitate and was...

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Abstract

The invention discloses a polymer nanosphere with a function of target recognition of cancer cells and a preparation method of the polymer nanosphere. The polymer nanosphere comprises polymer nanospheres with surfaces containing amino groups and aminated cancer cell target-mediated molecules, wherein the aminated cancer cell target-mediated molecules are fixedly arranged on the surfaces of the polymer nanospheres containing the amino groups through hydrogen bonds formed by the amino groups in the aminated cancer cell target-mediated molecules and the amino groups in the polymer nanospheres containing the amino groups. The polymer nanosphere prepared by virtue of the preparation method can be used as a drug carrier for coating anti-cancer drugs, and the nanosphere carriers have no cytotoxicity; and the aminated cancer cell target-mediated molecules are fixedly arranged on the surfaces of the nanospheres through the hydrogen bonds, and after the nanospheres are sent into a body in an intravenous injection or oral manner, the nanosphere carriers can be aggregated in a targeted manner adjacent to cancer cells so as to release drugs, so that the drug concentrations of local regions of the cancer cells are increased, and the targeted killing of the cancer cells is realized.

Description

technical field [0001] The invention belongs to the technical field of polymer materials and targeted drug delivery, and in particular relates to a polymer nanosphere with a cancer cell target recognition function and a preparation method thereof. Background technique [0002] The effect of tumor chemotherapy is largely limited by the small distribution of chemotherapy drugs in tumor sites (often less than 1%), the significant multidrug resistance of tumor cells, and the toxicity of chemotherapy drugs to normal cells. As a delivery carrier for chemotherapy drugs, polymer nanospheres have the advantages of various types, biodegradability, excellent surface properties, and responsiveness to the pH environment and enzyme molecules in the human body, and have received extensive attention. Through the mediation of targeting molecules, the recognition and uptake of nanospheres by tumor cells can be effectively promoted, so as to achieve targeted drug delivery to tumor cells, incre...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K47/54A61K47/64C08F212/08C08F220/34C08F212/36C08F220/18C08F220/14C08F222/38C08F8/32C08G81/00A61P35/00
CPCC08F8/32C08F212/08C08F220/18C08G81/00C08F220/1804C08F220/34C08F212/36C08F220/14C08F222/385
Inventor 蒋国强胡杨阚成友于常军
Owner TSINGHUA UNIV
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