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Preparation of high-molecular-based pH-sensitive medicament micelle

A high-molecular-based and high-molecular material technology, which is applied in the preparation of block polymer material drug carrier micelles and the preparation of high-molecular-based pH-sensitive drug micelles, can solve the problem of low water solubility of drug molecules, high synthesis cost, Poor biocompatibility and other problems, to achieve the effect of reducing toxic and side effects, good biocompatibility, and large load capacity

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 of high-molecular-based pH-sensitive medicament micelle
  • Preparation of high-molecular-based pH-sensitive medicament micelle
  • Preparation of high-molecular-based pH-sensitive medicament micelle

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] ① Preparation of 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 ): 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...

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Abstract

The invention discloses a preparation method of a high-molecular-based pH-sensitive medicament micelle. Phosphatidylcholine is subjected to an atom transfer radical polymerization reaction to obtain poly phosphatidylcholine. Benzyl glutamate carboxylic acid anhydride is subjected to a ring-opening polymerization reaction to obtain poly(benzyl glutamate) ester. The poly(benzyl glutamate) ester is grafted to doxorubicin through a hydrazone bond. The poly phosphatidylcholine is bonded to the poly(benzyl glutamate) ester in a manner of click chemistry to obtain a block copolymer. The block copolymer is respectively dissolved in tetrahydrofuran to obtain a solution. The solution is transferred to a dialysis bag for carrying out a dialysis process through pure water to obtain a dialysate which is filtered through a filter membrane. A freeze drying process is carried out to the filtered solution to obtain a medicant carrier micelle. The drug carrier micelle has a core-shell double-layer structure with an external layer being hydrophilic poly phosphatidylcholine and an internal layer being medicament molecule wrapping layer. The drug carrier micelle has advantages of belonging to nano particles and enabling a targeting transmission of a drug to cancer cells and a pH-sensitive releasing process in the cancer cells to be achieved. The drug carrier micelle is large in drug carrying capacity and good in stability. A targeting function of the drug carrier micelle can effectively reduce toxic and side effects of drugs on normal tissues and organs.

Description

Technical field [0001] The invention relates to a preparation method of a polymer-based pH-sensitive drug micelle, 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 organs, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K9/107A61K31/704A61P35/00C08G81/00
Inventor 不公告发明人
Owner CHENGDU LVKE HUATONG TECH
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