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Application of polymer based on beta-cyclodextrin

A polymer and cyclodextrin technology, which is applied in the directions of inactive medical preparations, inactive polymer compounds, and medical preparations containing active ingredients, etc. problems, to achieve good biocompatibility, inhibition of P-gp effect, and the effect of reversing drug resistance

Active Publication Date: 2010-07-07
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] β-CD is a widely used drug carrier and drug excipient approved by the FDA. Although there are a large number of documents reporting the successful application of β-CD in drug and gene carriers, due to the limited size of the hydrophobic space of β-CD properties limit its application to certain

Method used

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  • Application of polymer based on beta-cyclodextrin
  • Application of polymer based on beta-cyclodextrin
  • Application of polymer based on beta-cyclodextrin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1: Application of β-CD-PLA1000-mPEG2000 (Y: PLA, molecular weight 1000; Z: mPEG, molecular weight 2000) polymer micelles in inhibition of P-gp

[0026] 1. Preparation of β-CD-PLA1000-mPEG2000 polymer micelles and determination of their physical and chemical properties

[0027] Amino activation reaction:

[0028] Dissolve 11.3g (10mmol) of β-CD in 75ml of pyridine, slowly add 25ml of pyridine solution containing 13.3g (70mmol) of p-toluenesulfonyl chloride (TsCl) dropwise, and magnetically stir the reaction for 4 hours in an ice-water bath, then continue at room temperature Stir for 20h. After stopping the reaction, distill off most of the pyridine under reduced pressure at 40°C, soak in ether for 2 days, then form a fine powder, wash with water, filter, soak in acetone for 1 day, and dry in vacuum after filtering.

[0029] Add 5.0 g of sulfonylated β-CD into 20 ml of ethylenediamine, and react at 40° C. for 48 h. Concentrate the reaction solution under redu...

Embodiment 2

[0052] Example 2: Application of β-CD-PLA2000-mPEG2000 (Y: PLA, molecular weight 2000; Z: mPEG, molecular weight 2000) polymer micelles in inhibition of P-gp

[0053] 1. Preparation of β-CD-PLA2000-mPEG2000 polymer micelles and determination of their physical and chemical properties

[0054] Amino activation reaction: the method is the same as 1(1) of Example 1.

[0055] (2) Synthesis of hydroxyl-terminated Y-Z polymer:

[0056] Method is the same as 1(2) of Example 1. The dosage of mPEG2000 is 2g, the dosage of lactide is 2g, and the dosage of stannous octoate is 0.01g.

[0057] (3) Y-Z polymer terminal hydroxyl activation:

[0058] Method is the same as 1(3) of embodiment 1. mPEG2000-PLA2000:DMAP:TEA:succinic anhydride=1:1.2:1.2:1.2 (mol / mol).

[0059] (4) Cyclodextrin polymer synthesis:

[0060] Method is the same as 1(4) of Example 1. mPEG2000-PLA2000-COOH:DCC:DMAP:β-CDen7=1:7.2:7.2:7.2 (mol / mol). The NMR spectrum of the polymer is attached Figure 4 (B).

[00...

Embodiment 3

[0071] Example 3: Application of β-CD-PLA2000-mPEG5000 (Y: PLA, molecular weight 2000; Z: mPEG, molecular weight 5000) polymer micelles in inhibition of P-gp

[0072] 1. Preparation of β-CD-PLA2000-mPEG5000 polymer micelles and determination of their physical and chemical properties

[0073] Amino activation reaction: the method is the same as 1(1) of Example 1.

[0074] (2) Synthesis of hydroxyl-terminated Y-Z polymer:

[0075] Method is the same as 1(2) of Example 1. The dosage of mPEG5000 is 5g, the dosage of lactide is 2g, and the dosage of stannous octoate is 0.01g.

[0076] (3) Y-Z polymer terminal hydroxyl activation:

[0077] Method is the same as 1(3) of embodiment 1. mPEG5000-PLA2000:DMAP:TEA:succinic anhydride=1:1.2:1.2:1.2 (mol / mol).

[0078] (4) Cyclodextrin polymer synthesis:

[0079] Method is the same as 1(4) of Example 1. mPEG5000-PLA2000-COOH:DCC:DMAP:β-CDen7=1:7.2:7.2:7.2 (mol / mol). The NMR spectrum of the polymer is attached Figure 4 (C).

[00...

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Abstract

The invention provides the application of a polymer system based on beta-cyclodextrin in P-glycoprotein of suppressive tumour cells. The polymer consists of the beta-cyclodextrin and grafted amphipathy polymer. The star-shaped amphipathy polymer based on beta-CD and provided by the invention has remarkable effect of restraining P-gp protein, and the restraining effect thereof is obviously superior to the inhibitor CsA of the P-gp protein. The polymer of the invention has the characteristics of low cytotoxicity, good biocompatibility, biodegradability, long intracorporeal circulation time and the like, and provides an ideal dose carrier material for hydrophobic antineoplastic agents.

Description

technical field [0001] The invention belongs to the pharmaceutical use of polymers, and relates to the application of a polymer micelle drug delivery system in inhibiting drug-resistant tumor cells, in particular to the polymer micelle drug delivery system reversing drug resistance of tumor cells through P-gp inhibition Applications. Background technique [0002] Tumor is a major disease that threatens human health. About 60% of cancer patients die every year due to ineffective treatment. Tumor chemotherapy is currently a widely used tumor treatment method, but it still has its own limitations, such as low cure rate, high toxicity and side effects, multidrug resistance and other major problems. Among them, multidrug resistance is one of the main reasons for the failure of clinical chemotherapy of tumors. The cause of death of 90% of metastatic cancer patients is directly or indirectly related to the resistance of tumor cells to anti-tumor cell drugs. Therefore, finding a ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/40A61K47/34A61K31/704A61K9/00A61P35/00
Inventor 邱利焱王蓉娟
Owner ZHEJIANG UNIV
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