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ROS-sensitive polyethylene glycol-polyester copolymer nano-drug delivery system and application thereof

A polyethylene glycol and copolymer technology, applied in the field of biomedicine, can solve the problems of short effective time, poor effect, and can only be used by injection, so as to achieve the effect of oral administration

Active Publication Date: 2021-10-22
INST OF RADIATION MEDICINE CHINESE ACADEMY OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Amifostine is the only chemical drug with radiation protection effect approved by the FDA, but its effective time is short, it cannot be taken orally and can only be used by injection
Poor effect when taken orally (N.P.Praetorius, T.K.Mandal, J.Pharm.Pharmacol.60(2008) 809-815)

Method used

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  • ROS-sensitive polyethylene glycol-polyester copolymer nano-drug delivery system and application thereof
  • ROS-sensitive polyethylene glycol-polyester copolymer nano-drug delivery system and application thereof
  • ROS-sensitive polyethylene glycol-polyester copolymer nano-drug delivery system and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Embodiment 1 ROS sensitive polymer preparation

[0033] Add thioketal TK (1.0 g) into the reaction flask, and add 3 mL of acetic anhydride to dissolve it, and react at room temperature for 2 hours under nitrogen protection. Then 20 mL of toluene was added to the system, and dried under reduced pressure for 3 times. Add 10 mL of dichloromethane into the reaction bottle, and add polyethylene glycol (3.0 g) with a relative molecular weight of 2000, and react overnight. The product solution was washed 3 times with water, the oil phase was concentrated, and the product was dried. TK-PEG-TK is obtained. In a dry reaction flask, add TK-PEG-TK (1.4g), EDCI (0.55g) and HoBt (0.38g) dissolved in 20mL of dichloromethane, and react for half an hour. Then 1.4 g of polycaprolactone (PCL2000) were added. React at room temperature for 24 hours. The reaction solution was concentrated, dialyzed in distilled water for 24 hours, and the product was freeze-dried for 24 hours to obtain ...

Embodiment 2

[0038] Example 2 (II-1) Preparation of disulfide bond-linked ROS sensitive compounds

[0039] In a dry reaction flask, add cystine (1.0 g), EDCI (0.55 g) and HoBt (0.38 g) dissolved in 20 mL of dichloromethane, and react for half an hour. Add polyethylene glycol (1.0 g) with a relative molecular weight of 2000 into the reaction flask, and add 3 mL of acetic anhydride to dissolve it, and react at room temperature for 2 hours under nitrogen protection. Then 20 mL of toluene was added to the system, and dried under reduced pressure for 3 times. Add 10 mL of dichloromethane into the reaction flask, and add methyl-terminated polyethylene glycol (3.0 g) with a relative molecular weight of 2000, and react overnight. The product solution was washed 3 times with water, the oil phase was concentrated, and the product was dried. Obtain mPEG-TK. In a dry reaction vial, add mPEG-TK (1.4g),

[0040] EDCI (0.55g) and HoBt (0.38g) were dissolved in 20mL of dichloromethane and reacted for ...

Embodiment 3

[0045] The preparation of embodiment 3 drug-loaded nanoparticles

[0046] The polymers prepared in Examples 1-2 above can be combined with various bioactive molecules to form drug-loaded nanoparticles for radiation protection. In the following, only amifostine (Am) and its metabolite WR-1065 are used as examples for illustration.

[0047] The ROS-sensitive polymer self-assembly was prepared by double emulsion (W / O / W) method.

[0048] Drug-loaded nanoparticles 1: Preparation of I-1 / WR-1065 nanoparticles

[0049] Dissolve 50mg of WR-1065 in 200mL of distilled water to form an internal water phase (W1), and dissolve 100mg of I-1 polymer in 2mL of dichloromethane to form an oil phase (O). Add W1 to O and ultrasonicate for 3 minutes in an ice-water bath , forming the first emulsion (W1 / O). Add colostrum into 10 mL of distilled water (W2), and sonicate for 3 minutes in an ice-water bath to form a W1 / O / W2 double emulsion. The dichloromethane was removed by rotary evaporation, and...

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PUM

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Abstract

The invention provides an ROS-sensitive polyethylene glycol-polyester nano-drug delivery system which is characterized by comprising an ROS-sensitive polyethylene glycol hydrophilic segment A and a polyester hydrophobic segment B, and the hydrophilic and hydrophobic segments are linked by ROS-sensitive bonds to form A-B and B-A-B copolymers. The ROS sensitive material provided by the invention at least has one of the following advantages: the polymer material provided by the invention can be used for preparing a nano drug carrying material, drug wrapping is carried out through polymer self-assembly, drug molecules can be stabilized, ROS response sensitive release can be realized, and oral administration and the like can be realized.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to the protection of ionizing radiation damage, in particular to an amphiphilic polymer material, a nanometer drug-carrying system and applications thereof. Background technique [0002] Radiation damage is tissue damage caused by ionizing radiation (IR), which usually occurs in nuclear leak accidents, radioactive source loss accidents, and radiotherapy for tumor patients. Instantaneous exposure to high-dose rays or prolonged exposure to low-dose rays can cause tissue damage. Ionizing radiation can generate reactive oxygen species (ROS) free radicals in tissues and cells, interfere with DNA, protein and other macromolecules, induce cell damage and abnormal cell function, and eventually lead to functional disorders and pathological changes in various organs of the body Even cause the body to mutate or die. [0003] So far, most medical efforts aimed at mitigating radiation damage have re...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K45/00A61K47/34A61P7/00A61P39/00B82Y5/00B82Y40/00C08G81/00
CPCA61K9/5146A61K45/00A61P7/00A61P39/00B82Y5/00B82Y40/00C08G81/00
Inventor 蔺晓娜田红旗
Owner INST OF RADIATION MEDICINE CHINESE ACADEMY OF MEDICAL SCI
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