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Preparation method and application of acid-responsive polymer drug based on dextran

A technology of dextran and polymers, which is applied in the fields of chemical drugs and biological applications, and can solve the problems of poor selective and controllable release of drugs, low drug loading, and poor stability of micelles.

Inactive Publication Date: 2018-11-09
SOUTHWEST UNIVERSITY
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] Aiming at the shortcomings of the current drug delivery system, such as poor stability of micelles, low drug loading capacity, and poor selective and controllable release of drugs during delivery, the present invention aims to design and provide a class of drugs with good micelle stability and drug loading. A high-quantity, controlled-release preparation method of dextran-based acid-responsive polymer drugs, and by synthesizing two acid-responsive polymer drugs with different chain lengths to study and compare their drug release in vitro, cytotoxicity, etc. difference

Method used

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  • Preparation method and application of acid-responsive polymer drug based on dextran
  • Preparation method and application of acid-responsive polymer drug based on dextran
  • Preparation method and application of acid-responsive polymer drug based on dextran

Examples

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Embodiment 1

[0048] Example 1 Preparation of dextran-based acid-responsive polymer drug Dextran-P(OEGMA)-b-P(MGMA-DOX)

[0049] (1) Preparation of dextran-based initiator Dextran-Br:

[0050] Under the condition of argon atmosphere, dextran (Dextran, 5g) dissolved in ionic liquid (25.0g) was cooled to 0°C, and N-methylpyrrolidone (NMP, 20mL) and N,N-dimethyl 2-bromoisobutyryl bromide (BIBB, 168.54mmol, 21mL) was slowly added dropwise, and the ice bath was continued for 0.5-2h, then warmed to room temperature (25°C), protected from light Reaction for 12-72h; b) after the reaction, the resulting mixed solution was added dropwise to deionized water to stir and precipitate, and the obtained precipitate was dissolved with acetone and reprecipitated. This was repeated three times to obtain a light yellow intermediate product, which was dried in a vacuum oven (25 -30°C); c) Dissolve the above light yellow intermediate product (500mg) in NMP (5mL), cool in an ice bath to 0°C, slowly add BIBB (5g,...

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Abstract

The invention particularly relates to an acid-responsive polymer drug based on dextran and application of the acid-responsive polymer drug. In a molecular formula of the polymer drug, the value rangeof x is 3 to 30, and m and n separately indicate polymerization degrees of a hydrophobic block and a hydrophilic block. A method comprises the following synthetic steps: (1) using dextran to synthesize an ATRP initiator (Dextran-Br); (2) introducing the hydrophilic and hydrophobic blocks by utilizing ATRP polymerization reaction; (3) using N2H4-H2O to substitute an ester group on MGMA, thus obtaining an acid-responsive precursor; and (5) using amino and carbonyl on doxorubicin to react to form hydrazone bonds to synthesize an acid-responsive polymerization prodrug. In a cancer cell weak acid environment, the polymerization prodrug can be selectively released and has the advantages of higher micelle stability, high drug loading amount and the like, and can effectively overcome the defects in a drug delivery system of the nano technology that hydrophobic drug molecules are poor in solubility, high in toxicity and side effects and the like.

Description

technical field [0001] The invention relates to the field of chemical medicine and biological application, in particular to a preparation method and application of a class of dextran-based acid-responsive polymer medicine. Background technique [0002] In the nanotechnology drug delivery system, Doxorubicin (DOX), as a common anticancer drug, is commonly used to treat a variety of diseases. Its CAS number: 23214-92-8, chemical structure: C 27 h 29 NO 11 , relative molecular weight: 543.52. Doxorubicin inhibits the synthesis of RNA and DNA, and the inhibitory effect on RNA is the strongest. Its mechanism of action is mainly that the drug intercalates into DNA and inhibits the synthesis of nucleic acid, thereby killing cancer cells. Doxorubicin is a cycle non-specific drug, which has a killing effect on a variety of tumor cells with different growth cycles. Adriamycin has a certain therapeutic effect on acute leukemia, acute lymphoblastic leukemia and myelocytic leukemia a...

Claims

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Application Information

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IPC IPC(8): C08F293/00C08F8/30C08F8/32C08J3/03A61K9/107A61K47/36A61K31/704A61P35/00
CPCA61K9/1075A61K31/704A61K47/36A61P35/00C08F8/30C08F8/32C08F293/005C08F2438/01C08J3/03C08J2353/00
Inventor 许志刚张天刘峰王亚君白霜马晓倩
Owner SOUTHWEST UNIVERSITY
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