Polymethacrylic acid-containing self-assembled drug carrier microcapsule system

A technology of polymethacrylic acid and self-assembly, which is applied in the direction of microcapsules, capsule delivery, and drug combination, which can solve the problems of high synthesis cost, reduced water solubility of drug molecules, and poor biocompatibility, and achieve large drug loads, Good biocompatibility, reducing toxic and side effects

Inactive Publication Date: 2015-03-25
CHENGDU LVKE HUATONG TECH
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  • Summary
  • 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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  • Polymethacrylic acid-containing self-assembled drug carrier microcapsule system
  • Polymethacrylic acid-containing self-assembled drug carrier microcapsule system
  • Polymethacrylic acid-containing self-assembled drug carrier microcapsule system

Examples

Experimental program
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Effect test

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 solution 3 , 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 present invention discloses a polymethacrylic acid-containing self-assembled drug carrier microcapsule system. The preparation method comprises: adopting an atom transfer radical polymerization method to polymerize methacrylic acid to obtain polymethacrylic acid; modifying the polymethacrylic acid with folic acid molecules; adopting a ring-opening polymerization method to polymerize O-benzyl-L-tyrosine carboxylic anhydride to obtain poly O-benzyl-L-tyrosine; grafting adriamycin on the poly O-benzyl-L-tyrosine; bonding the polymethacrylic acid and the poly O-benzyl-L-tyrosine through a click chemistry method to obtain a block copolymer; respectively dissolving the block polymer in tetrahydrofuran, transferring into a dialysis bag, carrying out dialysis with purified water, and filtering the dialyzed solution with a filtration membrane; and carrying out freeze-drying on the filtered solution to obtain the drug-loaded micelles, wherein the drug carrier micelles have a core-shell double-layer structure, the outer layer is the hydrophilic polymethacrylic acid, and the inner layer is the drug molecule wrapping layer. According to the present invention, the material has the following advantages that: the material belongs to the nanoparticles; the targeted drug delivery on the cancer cells and the pH-sensitive drug release in the cancer cells can be achieved; the drug loading is high; the stability is good; and with the targeting function, the toxic-side effect of the drug on the normal tissues and organs can be effectively reduced.

Description

technical field [0001] The invention relates to a self-assembled drug carrier microcapsule system containing polymethacrylic acid, in particular to a preparation method of a block polymer material drug carrier microcapsule 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...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K31/704A61K47/48C08G81/02A61P35/00
Inventor 不公告发明人
Owner CHENGDU LVKE HUATONG TECH
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