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Glucan polymer, polymer micelle and medicine carrier system

A polymer glue and carrier system technology, applied in the field of polymer micelles and drug carrier systems, dextran polymers, can solve the problems of poor targeting, insufficient stability, limited application of polymer micelles, etc., to reduce damage , Good hydrogen peroxide responsiveness, good responsiveness

Inactive Publication Date: 2018-06-01
THE SECOND HOSPITAL AFFILIATED TO WENZHOU MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, the existing polymeric micelles have defects such as poor targeting and insufficient stability when preparing tumor drug carriers, which limits the application of polymeric micelles in tumor drugs.

Method used

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  • Glucan polymer, polymer micelle and medicine carrier system
  • Glucan polymer, polymer micelle and medicine carrier system
  • Glucan polymer, polymer micelle and medicine carrier system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] A kind of preparation method of dextran polymer and micelle with hydrogen peroxide responsiveness, its synthetic route is such as figure 1 shown, the specific steps are as follows:

[0060] 1) First carry out the reaction of boron ester and dodecanoic acid, under nitrogen protection, put boron ester raw material A (1 eq) and dodecanoic acid (1.5 eq) into a 25 mL round bottom flask and dissolve with DCM. DMAP (0.2 eq) EDCI (1.5 eq) and Et3N (0.5 eq) were respectively dissolved in DCM and injected into the system using a syringe. The reaction solution was reacted at room temperature for 18h, followed by TLC spot plate. After the reaction was completed, water was added to quench. The aqueous layer was extracted 4 times with DCM, the organic phases were combined and MgSO was used 4 Dry, filter with suction, spin dry to obtain the crude product, and then purify it by column chromatography. The product was a yellow oil. reaction process such as figure 2 shown.

[0061...

Embodiment 2

[0066] The critical micelle concentration (CMC) of the micelles described in Example 1 was measured using fluorescent probe technology, and the specific steps were as follows:

[0067] 1) Preparation of fluorescent probe pyrene in methanol solution

[0068] Dissolve 0.0051 g of pyrene in 25 ml of methanol to obtain a pyrene solution with a concentration of 1.01×10-3 mol / L, and then dilute with methanol to obtain a pyrene solution of 1.616×10-6 mol / L.

[0069] 2) Preparation of DA-B-DEX aqueous solutions of different concentrations

[0070] The preparation concentration is 1 × 10 -4 , 1×10 -3 , 1×10 -2 , 1×10 -1 , 1, 10, 100, 1000 mg / ml of DA-B-DEX solution.

[0071] 3) Preparation of pyrene-containing micelles

[0072] Take 150 μl of the prepared pyrene solution, put it into several 10 ml volumetric flasks, and evaporate the methanol to dryness. Then, 10 ml of each concentration of DA-B-DEX solution was added to a 10 ml volumetric flask containing a trace amount of pyre...

Embodiment 3

[0076] A method for preparing a polymer micelle drug carrier with hydrogen peroxide response, the steps are as follows:

[0077] 1) Dissolve DA-B-DEX (100 mg) in DMSO (10 ml), add dropwise to PBS buffer (100 ml, pH 7.4) under stirring, and keep stirring for 30 min. Spontaneous formation of micelles was confirmed by observation of a clear opalescent solution.

[0078] 2) At the same time, prepare DA-B-DEX micelles that physically encapsulate doxorubicin. DA-B-DEX (91.5 mg) and DOX (8.5 mg) are dissolved in 10 mL of dimethyl sulfoxide (DMSO) together under stirring. It was added dropwise to 100 mL of PBS buffer and stirred for 30 min. Dialysis was carried out through a dialysis bag (molecular weight cut-off = 3.5KD) for 24 hours to remove organic solvents and free drugs, and finally freeze-dried for storage.

[0079] 3) The particle size distribution was measured using a Malvern laser particle sizer (Zetasized Nano, ZS, Malvern, United Kingdom). The morphology and size of mic...

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Abstract

The invention relates to a glucan polymer, a polymer micelle and a medicine carrier system. The glucan polymer is prepared from glucan, 4-(hydroxymethyl)benzeneboronic acid pinacol ester and polyol fatty acid through reaction, wherein the glucan and the polyol fatty acid provide hydrophilic and hydrophobic units, so that the polymer can automatically form the micelle; the polymer formed by the glucan, the 4-(hydroxymethyl)benzeneboronic acid pinacol ester and the polyol fatty acid through chemical reaction is sensitive to hydrogen peroxide; the response can be fast generated on hydrogen peroxide in an environment of ROS high expression diseases (such as myocardial ischemial injury, atherosclerosis, intestinal inflammation and tumor); the micelle disassembly is caused, so that the medicinemolecules are fast released.

Description

technical field [0001] The present invention relates to the field of drug carriers, in particular to a dextran polymer, polymer micelle and drug carrier system. Background technique [0002] According to a recent research report released by the World Health Organization's International Center for Research on Cancer, according to the current trend of cancer incidence, the incidence of cancer worldwide will increase by 50% in 2020, and the number of new cancer patients will reach 15 million each year. It seems that cancer has become one of the common causes of morbidity and mortality today, but there is a lack of safe and effective treatments. [0003] At present, the main methods of treating cancer include surgery, chemotherapy, radiotherapy, targeted therapy, and immunotherapy. Chemotherapy is the abbreviation of chemical drug treatment. The purpose of treatment is achieved by using chemotherapy drugs to kill cancer cells. However, the selectivity of chemotherapy is low, t...

Claims

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Application Information

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IPC IPC(8): C08B37/02A61K9/107A61K47/36A61K47/61A61K45/00A61P35/00A61P9/00A61P29/00
CPCA61K9/1075A61K45/00A61K47/36C08B37/0009C08B37/0024
Inventor 褚茂平孙昌正徐逸曾静静金其可卢孔场荣星林振坤李磊
Owner THE SECOND HOSPITAL AFFILIATED TO WENZHOU MEDICAL COLLEGE
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