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Injectable polypeptide hydrogel for local tumor radiotherapy and preparation method thereof

A hydrogel and topical technology, applied in the field of injectable polypeptide hydrogel and its preparation, can solve the pain of tumor treatment and postoperative healing of patients, the troubles and troubles of radiotherapy plan formulation and implementation, and achieve good cell growth inhibition effect, good degradability, and highly specific tumor-killing effect

Active Publication Date: 2019-01-22
INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, when long-term radiotherapy or short-half-life radiotherapy is required, frequent multiple operations to create radioactive seed sources and create and remove seed sources after treatment will bring great pain and trouble to the patient's tumor treatment and postoperative healing. It has brought troubles to the formulation and implementation of radiotherapy plans

Method used

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  • Injectable polypeptide hydrogel for local tumor radiotherapy and preparation method thereof
  • Injectable polypeptide hydrogel for local tumor radiotherapy and preparation method thereof
  • Injectable polypeptide hydrogel for local tumor radiotherapy and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0030] Example 1: mPEG-p(Tyr) 4 Preparation and Characterization of Copolymers

[0031] Polyethylene glycol (mPEG-NH) with a molecular weight of 2000 g / moL and methoxyl and amino 2 , 2.0 g) and tyrosine-N-carboxy-cyclic anhydride (Tyr-NCA, 0.873 g) were dissolved in 5 mL of anhydrous dimethylformamide, and reacted in a water bath at 30 °C for 48 hours. Then, the reaction solution was added dropwise to glacial ether, filtered, the precipitate was taken, and vacuum-dried to obtain the copolymer mPEG-p(Tyr) of polyethylene glycol and polytyrosine. x , by H NMR spectroscopy 1 The degree of polymerization of the tyrosine monomer in the product identified by H NMR analysis was 4. The polymerization reaction equation and the chemical structure of the product are as follows figure 1 shown.

Embodiment 2

[0032] Example 2: mPEG-p(Tyr) 8 Preparation and Characterization of Copolymers

[0033] Polyethylene glycol (mPEG-NH) with a molecular weight of 2000 g / moL and methoxyl and amino 2 , 1.0 g) and tyrosine-N-carboxy-cyclic anhydride (Tyr-NCA, 0.873 g) were dissolved in 5 mL of anhydrous dimethylformamide, and reacted in a water bath at 30 °C for 48 hours. Then, the reaction solution was added dropwise to glacial ether, filtered, the precipitate was taken, and vacuum-dried to obtain the copolymer mPEG-p(Tyr) of polyethylene glycol and polytyrosine. x, by H NMR spectroscopy 1 The degree of polymerization of the tyrosine unit in the H NMR analysis product is 8, the result is as follows figure 2 As shown, the polymer is labeled as mPEG-p(Tyr) 8 .

Embodiment 3

[0034] Example 3: mPEG-p(Tyr) 10 Preparation and Characterization of Copolymers

[0035] Polyethylene glycol (mPEG-NH) with a molecular weight of 2000 g / moL and methoxyl and amino 2 , 1.0 g) and tyrosine-N-carboxy-cyclic anhydride (Tyr-NCA, 1.09 g) were dissolved in 20 mL of anhydrous dimethylformamide, and reacted in a water bath at 30 °C for 48 hours. Then, the reaction solution was added dropwise to glacial ether, filtered, the precipitate was taken, and vacuum-dried to obtain the copolymer mPEG-p(Tyr) of polyethylene glycol and polytyrosine. x , by H NMR spectroscopy 1 H NMR analysis showed that the degree of polymerization of tyrosine units in the product was 10.

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Abstract

The invention relates to injectable polypeptide hydrogel for local radiotherapy on tumor and a preparation method of the injectable polypeptide hydrogel. The injectable polypeptide hydrogel consists of polyethylene glycol and hydrophobic polytyrosine macromolecule block polymers in a self-assembled manner; a radiotherapy agent 131I is marked on a polytyrosine chain segment of hydrogel by using a chloramine T method, then loading of the radiotherapy agent can be completed, and the injectable polypeptide hydrogel for local radiotherapy can be prepared. The injectable polypeptide hydrogel provided by the invention has the characteristics of being high in radiotherapy agent loading rate, free of toxin, good in stability and degradability, easy to inject and the like. Specificity long-term local radiotherapy of gel on tumor is innovated, and compared with other radiotherapy preparations, the injectable polypeptide hydrogel has the advantages that injection treatment can be easily achieved, operation invasive implantation and seed source removal are avoided, radiation injury of non-tumor tissue can be avoided, and the pharmacological function lasts for a long time.

Description

technical field [0001] The invention relates to an injectable polypeptide hydrogel for local tumor radiotherapy and a preparation method thereof. Based on polyethylene glycol and hydrophobic polytyrosine copolymer, an injectable and degradable polypeptide hydrogel capable of efficiently loading radiotherapeutic agents was developed and disclosed for specific local radiotherapy of tumors. Background technique [0002] At present, the number of morbidity and death of cancer in my country is still increasing, and radiotherapy is still one of the main means of clinical treatment of tumors. However, due to the large radiation area, large radiation dose and penetration through the human body, conventional radiotherapy has great damage to the normal tissue structure of the human body. At present, the "radioactive seed source implantation therapy" based on iodine-125 is widely used clinically, that is, the radioactive seed source is implanted into tumor tissue or its surroundings t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K51/12A61K51/08A61K9/06A61K31/337A61K31/704A61K47/34A61K101/02
CPCA61K9/0019A61K9/06A61K31/337A61K31/704A61K47/10A61K47/183A61K47/42A61K51/08A61K51/1213
Inventor 王伟伟黄平升孔德领
Owner INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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