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Glucosamine-modified polyethyleneglycol-polylactic acid, preparation method therefor and application thereof

A technology of glucosamine and polyethylene glycol, applied in the field of glucosamine-modified polyethylene glycol-polylactic acid and its preparation, can solve the problems of high toxicity and side effects, lack of targeting, low curative effect, etc., and achieve high safety , improve the effect of tumor treatment

Inactive Publication Date: 2015-09-09
GUANGZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, PLA-b-PEG as a drug carrier brings low curative effect and high side effects due to the lack of specific targeting in the process of drug delivery

Method used

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  • Glucosamine-modified polyethyleneglycol-polylactic acid, preparation method therefor and application thereof
  • Glucosamine-modified polyethyleneglycol-polylactic acid, preparation method therefor and application thereof
  • Glucosamine-modified polyethyleneglycol-polylactic acid, preparation method therefor and application thereof

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Embodiment 1

[0031] A preparation method of glucosamine-modified polyethylene glycol-polylactic acid, comprising the following steps:

[0032] (1) Under the protection of nitrogen, 10g M-COOH-PEG 400 (Carboxy-modified polyethylene glycol, Beijing Jiankai Technology Co., Ltd.) was added to 80g of lactic acid (LA) solution, stirred at room temperature for 6hrs, vacuumed nitrogen replacement 3 times, heated and melted under vacuum (-0.1MPa) and Stir to mix the raw materials evenly, return to normal pressure under nitrogen protection, add the catalyst stannous octoate (2g) and react in a vacuum state for 25hrs; dissolve the product in dichloromethane, precipitate and purify with ether, and dry in vacuum under reduced pressure to obtain M-COOH- PEG 400 -PLA 720 polymer;

[0033] (2) Dissolve 5g of glucosamine (AG) in 10mL DMF at room temperature to form an AG solution; take 10g of M-COOH-PEG prepared in step (1) 400 -PLA 720 The polymer was dissolved in 20 mL of dimethylformamide (DMF) at ...

Embodiment 2

[0040] A preparation method of glucosamine-modified polyethylene glycol-polylactic acid, comprising the following steps:

[0041] (1) Under the protection of nitrogen, 50g M-COOH-PEG 2000(Carboxy-modified polyethylene glycol, Beijing Jiankai Technology Co., Ltd.) was added to 400g lactic acid (LA) solution, stirred at room temperature for 6hrs, vacuumed nitrogen replacement 3 times, heated and melted under vacuum (-0.1MPa) and Stir to mix the raw materials evenly, return to normal pressure under nitrogen protection, add the catalyst stannous octoate (10g) and react in a vacuum state for 30hrs; dissolve the product in dichloromethane, precipitate and purify with ether, and dry in vacuum under reduced pressure to obtain M-COOH- PEG 2000 -PLA 6600 polymer;

[0042] (2) Dissolve 20g of glucosamine (AG) in 40mL DMF at room temperature to form an AG solution; take 40g of M-COOH-PEG prepared in step (1) 2000 -PLA 6600 Dissolve the polymer in 80mL dimethylformamide (DMF) at room ...

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Abstract

The invention discloses glucosamine-modified polyethyleneglycol-polylactic acid, a preparation method therefor and an application thereof A chemical structure of glucosamine-modified polyethyleneglycol-polylactic acid is shown in the specification, wherein x and y are integers larger than 0. AG is grafted on PEG-PLA, and a novel target polymer is obtained, so that the curative effect of tumors can be improved and the polymer can be used as a medicine carrier. The PEG-PLA is approved by FDA of the United States and is widely applied to the field of biological medicines, so that the AG-PEG-PLA is high in safety and can be greatly applied to clinical medicines.

Description

technical field [0001] The invention belongs to the field of pharmaceutical polymer materials, and in particular relates to a glucosamine-modified polyethylene glycol-polylactic acid and a preparation method and application thereof. Background technique [0002] Malignant tumors are the number one killer of human health. Targeted drugs have attracted much attention in the treatment of cancer patients to prolong the survival period and improve the quality of life. Most malignant tumor cells have high metabolic characteristics, aerobic and anaerobic metabolism coexist, and tumor cells overexpress glucose transporter to absorb enough glucose, so glucose can be used as a target molecule to identify tumor cells. [0003] Currently, D-glucosamine etc. are labeled with radionuclides 18 F, There have been a lot of reports as a sharp tool for tumor diagnosis and analysis, but there is no report on modifying biodegradable materials (such as PLA-PEG) to form polymers as drug carriers...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G63/91C08G63/664A61K47/34A61K9/14A61K9/06A61K9/16A61P35/00
Inventor 周毅王赫杜玲然彭维
Owner GUANGZHOU MEDICAL UNIV