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Preparation method of adriamycin polymer drug

A doxorubicin and polymer technology, applied in the field of polymer chemistry and polymers, can solve the problems of reduced water solubility of drug molecules, high synthesis cost, poor biocompatibility, etc., to reduce toxic side effects and improve biocompatibility Good, heavy load effect

Inactive Publication Date: 2015-12-23
成都市龙华新科技有限公司
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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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  • Preparation method of adriamycin polymer drug
  • Preparation method of adriamycin polymer drug
  • Preparation method of adriamycin polymer drug

Examples

Experimental program
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Embodiment 1

[0044] ①Prepare azide small molecule initiator

[0045] Step 1: Dissolve 5mL of 2-chloroethoxyethanol in 25mL of methyl ethyl ketone, add 4.5g of 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 HNMR(CDCl 3 ): δ 3.70(t,2H,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 ), and2.56(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 dimethylaminopyridine was dissolv...

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Abstract

The invention discloses a preparation method of an adriamycin polymer drug. The method comprises the following steps: polymerizing acrylamide by utilizing an atom transfer radical polymerization method to obtain polyacrylamide; modifying the polyacrylamide by utilizing folic acid molecules; polymerizing glutamic acid-benzyl ester-carboxylic acid anhydride by utilizing a ring opening polymerization method to obtain poly (benzyl glutamate); grafting the poly (benzyl glutamate) with adriamycin by hydrazone bond; carrying out bond connection between the polyacrylamide and the poly (benzyl glutamate) by a click chemical method to obtain a block copolymer; dissolving the block copolymer respectively in tetrahydrofuran, and then moving into a dialysis bag to dialyze by using pure water, and filtering dialysate by using a filter membrane; performing freeze drying to a filtered solution to obtain micelle loading medicine. The micelle loading the medicine has a core-shell bilayer structure, wherein the outer layer is hydrophilic polyacrylamide, and the inner layer is a wrapper of pharmaceutical molecules. The adriamycin polymer drug has the following advantages of belonging to nanoparticles; being capable of realizing targeted delivery of the medicine for cancerous cells and pH sensitivity releasing in the cancerous cells; large drug loading capacity; good stability; effectively reducing toxic and side effects of the medicine on normal tissues and organs by virtue of the targeted delivery function.

Description

Technical field [0001] The invention relates to a method for preparing doxorubicin polymer drugs, in particular to a method for preparing block polymer material drug carrier micelles 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 eff...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/704A61K9/107A61P35/00C08G81/02
Inventor 不公告发明人
Owner 成都市龙华新科技有限公司
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