Preparation method of doxorubicin-containing anti-tumor micelles

A doxorubicin and anti-tumor technology, which is applied in the direction of anti-tumor drugs, medical preparations containing active ingredients, medical preparations with non-active ingredients, etc. Poor compatibility and other problems, to achieve the effect of reducing toxic and side effects, large drug load, and good biocompatibility

Inactive Publication Date: 2014-08-13
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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  • Preparation method of doxorubicin-containing anti-tumor micelles
  • Preparation method of doxorubicin-containing anti-tumor micelles
  • Preparation method of doxorubicin-containing anti-tumor micelles

Examples

Experimental program
Comparison scheme
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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 preparation method of doxorubicin-containing anti-tumor micelles. The preparation method includes the steps: polymerizing acrylic acid by an atomic transfer radical polymerization method to obtain polyacrylic acid; polymerizing glutamic acid benzyl ester carboxylic acid anhydride by a ring opening polymerization method, to obtain poly(glutamic acid benzyl ester); grafting poly(glutamic acid benzyl ester) with adriamycin through a hydrazone bond; carrying out bond connection of polyacrylic acid and poly(glutamic acid 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 invention relates to a preparation method of an anti-tumor micelle containing doxorubicin, in particular to a preparation method of a block polymer material drug carrier micelle with cancer cell targeting. The invention 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 to treat cancer is drug therapy. However, many anticancer drugs have defects such as insoluble in water and poor stability. For example, camptothecin, paclitaxel, doxorubicin, and 5-fluorouracil are difficult to be well utilized by organisms due to their poor solubility. Solving the problem of their water solubility is the key to the clinical application of such pharmaceutical preparations. In addition, most of the tumor treatment and diagnostic drugs have non-selective effects, and are often distributed in some normal tissues and organ...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K9/107A61K31/704A61P35/00C08G81/02A61K47/59
Inventor 不公告发明人
Owner CHENGDU LVKE HUATONG TECH
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