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Novel anti-cancer polymer drug

A technology of polymers and polymer materials, applied in the direction of nano-medicines, anti-tumor drugs, drug combinations, etc., can solve the problems of reduced water solubility of drug molecules, high synthesis costs, poor biocompatibility, etc., to reduce toxic side effects, Good biocompatibility and large loading effect

Inactive Publication Date: 2015-03-18
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 solubility of drug molecules on the surface of dendrimer.
In addition, dendrimer has a complex structure and high synthesis cost
These problems limit the application of star-shaped polymer nano-drug delivery system

Method used

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  • Novel anti-cancer polymer drug
  • Novel anti-cancer polymer drug
  • Novel anti-cancer polymer drug

Examples

Experimental program
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Effect test

Embodiment 1

[0044] ① Preparation of azide small molecule initiator

[0045] Step 1: Dissolve 5mL 2-chloroethoxyethanol in 25mL methyl ethyl ketone, add 4.5g NaN to the solution 3 , 2.5gBu 4 NI, 10 mg of dicyclohexane-18-crown-6, heat the mixture to boiling and stir for 24 hours. The mixture was filtered and the precipitate was thoroughly rinsed with acetone. The resulting mixed solution is the crude product. After concentrating the mixed solution, o C is distilled to obtain a pure product. The resulting 2-azidoethoxyethanol 1 H NMR (CDCl 3 ): 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).

[0046] Step 2: Dissolve 2 g of 2-azidoethoxyethanol and 5.09 g of α-chloro acid chloride prepared in step 1 in 30 mL of dichloromethane, transfer the reaction system to the ice field, and transfer 6.8 g of dicyclohexyl The carbodiimide was slowly added to the reaction vessel and stirred. 0.4 g of dimethylaminopyrid...

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Abstract

The invention discloses a novel anti-cancer polymer drug. A preparation method of the drug comprises the following steps: polymerizing pyrrolidone by utilizing an atom transfer radical polymerization method, thus obtaining polypyrrolidone; modifying polypyrrolidone by utilizing folic acid molecules; polymerizing lysine benzyl ester carboxylic acid anhydride by utilizing a ring opening polymerization method, thus obtaining polylysine benzyl ester; grafting adriamycin onto polylysine benzyl ester via hydrazone bonds; connecting polypyrrolidone with polylysine benzyl ester with bonds through click chemistry, thus obtaining block copolymers; after dissolving the block copolymers in tetrahydrofuran respectively, transferring the solutions into a dialysis bag, dialyzing the solutions with pure water, and filtering the dialysate with a filter membrane; freeze-drying the solutions after filtration, thus obtaining a drug-loading micelle. The drug carrier micelle has a core / shell double-layer structure, wherein the outer layer is formed by hydrophilic polypyrrolidone, and the inner layer is a drug molecule coated layer. The material has the advantages that the material belongs to nanoparticles; the drug can achieve targeting delivery to cancer cells and pH-sensitive release in the cancer cells; the material has high drug loading capacity and good stability; the toxic and side effects of the drug on normal tissues and organs can be effectively reduced via the targeting function of the drug.

Description

Technical field [0001] The invention relates to a new type of anti-cancer polymer drug, in particular to a method for preparing a block polymer material drug carrier micelle with cancer cell targeting. 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 methods for treating cancer is drug therapy. However, many anti-cancer drugs have defects such as insoluble in water and poor stability. For example, camptothecin, paclitaxel, doxorubicin, 5-fluorouracil, etc. are difficult to be used by organisms due to poor solubility. Solving the problem of water solubility is the key to the clinical application of such pharmaceutical preparations. In addition, the effects of tumor treatment and diagnostic drugs are mostly non-selective, and some normal tissues and organs are often distributed, and the therapeutic doses have large toxic side effects on n...

Claims

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Application Information

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