Novel antitumor doxorubicin-containing macromolecular drug

A doxorubicin, anti-tumor technology, applied in the directions of anti-tumor drugs, nano-drugs, drug combinations, etc., can solve the problems of low water solubility of drug molecules, high synthesis cost, poor biocompatibility, etc., and reduce toxic and side effects. , good biocompatibility, large loading effect

Inactive Publication Date: 2014-08-27
CHENGDU LVKE HUATONG TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, due to the complex structure of the polymer in the star polymer, the prepared drug carrier has problems such as poor biocompatibility, decreased drug loading capacity, and reduced water so...

Method used

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  • Novel antitumor doxorubicin-containing macromolecular drug
  • Novel antitumor doxorubicin-containing macromolecular drug
  • Novel antitumor doxorubicin-containing macromolecular drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] ① Prepare azide small molecule initiator

[0043] Step 1: Dissolve 5 mL of 2-chloroethoxyethanol in 25 mL of butanone, and add 4.5 g of NaN to the solution 3 , 2.5gBu 4NI, 10 mg of dicyclohexane-18-crown-6, the mixture was heated to boiling and stirred for 24 hours. The mixture was filtered and the precipitate was rinsed thoroughly with acetone. The resulting mixed solution is the crude product of the product, after the mixed solution was concentrated, at 90 o C was distilled to obtain the pure product. The resulting 2-azidoethoxyethanol 1 H NMR (CDCl 3 ): δ 3.70 (t, 2 H, C H 2 OH), 3.65 (t, 2 H, HOCH 2 C H 2 O), 3.56 (t, 2H, N 3 CH 2 C H 2 O), 3.37 (t, 2H, C H 2 N 3 ), and 2.56 (s, 1H, OH).

[0044] Step 2: Dissolve 2g of 2-azidoethoxyethanol and 5.09g of α-chloroacyl chloride in 30mL of dichloromethane prepared in step 1, transfer the reaction system to ice, and dissolve 6.8g of dicyclohexyl The carbodiimide was slowly added to the reaction vesse...

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Abstract

The invention discloses a novel antitumor doxorubicin-containing macromolecular drug. A preparation method includes the steps: polymerizing acrylic acid by an atomic transfer radical polymerization method to obtain polyacrylic acid; polymerizing lysine benzyl ester carboxylic acid anhydride by a ring opening polymerization method, to obtain poly(lysine benzyl ester); grafting poly(lysine benzyl ester) with adriamycin through a hydrazone bond; carrying out bond connection of polyacrylic acid and poly(lysine benzyl ester) by a click chemistry method, to obtain a block copolymer; dissolving the block polymer in tetrahydrofuran, transferring into a dialysis bag, dialyzing with pure water, and filtering the dialyzed liquid with a filter membrane; and freeze-drying the filtered solution, and thus obtaining drug-loaded micelles. The drug carrier micelles have a core-shell double-layer structure, an outer layer is hydrophilic polyacrylic acid, and an inner layer is a drug molecular wrapping layer. The material has the following advantages that the material belongs to nanoparticles, can realize targeted delivery of drugs on cancer cells and pH sensitive release in the cancer cells, and has large drug loading capacity and good stability; and the targeted function can effectively reduce toxic and side effects of the drugs to normal tissues and organs.

Description

Technical field [0001] The present invention involves a new type of antitumor containing Dorno -Star Polymer drugs, especially the preparation method of a polymer material carrier beam with a targeted carcinogenic cells.It belongs to the field of polymer chemistry and polymer technology. Background technique [0002] Cancer has become the most important disease that endangers human health. One of the important means of treating cancer is drug treatment. However, many anti -cancer drugs have defects such as difficulty in water and poor stability.For example, the citrine, paclitaxel, dodorbixing, and 5-fluoropicidine are difficult to use by the organism due to poor solubility. It is difficult to solve its water-soluble problems. It is the clinical application of this type of drug preparation.In addition, the role of tumor treatment and diagnosis of drugs is mostly non -selective. Some normal tissue organs are often distributed, and the treatment dosage has great side effects on nor...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K9/51A61K31/704B82Y5/00C08G81/02C08F120/06C08G69/48C08G69/40A61P35/00
Inventor 不公告发明人
Owner CHENGDU LVKE HUATONG TECH
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