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Preparation method of antitumor micelle containing adriamycin

A doxorubicin and anti-tumor technology, which is applied in the field of preparation of block polymer material drug carrier micelles, can solve the problems of reduced water solubility of drug molecules, high synthesis cost, poor biocompatibility and the like, and achieves biocompatibility. Good, reduce toxic side effects, the effect of large load

Inactive Publication Date: 2015-03-18
CHENGDU LVKE HUATONG TECH
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  • Abstract
  • Description
  • Claims
  • Application Information

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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 antitumor micelle containing adriamycin
  • Preparation method of antitumor micelle containing adriamycin
  • Preparation method of antitumor micelle containing adriamycin

Examples

Experimental program
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Embodiment 1

[0044] ① Preparation of azide small molecule initiator

[0045] Step 1: Dissolve 5 mL of 2-chloroethoxyethanol in 25 mL of butanone, and add 4.5 g of NaN to the solution3 , 2.5gBu 4 NI, 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 ): 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 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 v...

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Abstract

The invention discloses a preparation method of an antitumor micelle containing adriamycin. The preparation method comprises the following steps: polymerizing acrylic acid by utilizing an atom transfer radical polymerization method, thus obtaining polyacrylic acid; modifying polyacrylic acid by utilizing folic acid molecules; polymerizing glutamic acid benzyl ester carboxylic acid anhydride by utilizing a ring opening polymerization method, thus obtaining polyglutamic acid benzyl ester; grafting adriamycin onto polyglutamic acid benzyl ester via hydrazone bonds; connecting polyacrylic acid with polyglutamic acid 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 polyacrylic acid, 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 of 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 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): A61K9/51A61K47/48A61K31/704B82Y5/00C08G81/02A61P35/00
Inventor 不公告发明人
Owner CHENGDU LVKE HUATONG TECH
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