Degradable acid-sensitive polyaspartamide copolymer and its preparation method and use

A polyasparagine and copolymer technology, applied in the field of copolymers, can solve problems such as slow drug release, and achieve the effects of maintaining curative effect, excellent biocompatibility, and improving bioavailability

Inactive Publication Date: 2015-05-06
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this new type of drug and gene delivery system is quite complex and challenging. The release of the drug is very slow. Only less than 20% of the drug is released in 120 hours in vitro, and the time of

Method used

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  • Degradable acid-sensitive polyaspartamide copolymer and its preparation method and use
  • Degradable acid-sensitive polyaspartamide copolymer and its preparation method and use
  • Degradable acid-sensitive polyaspartamide copolymer and its preparation method and use

Examples

Experimental program
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Effect test

Embodiment 1

[0049] Example 1: Preparation of biodegradable acid-sensitive amphiphilic block copolymer

[0050] 1.1 Preparation of N-carboxylic acid anhydride of L-benzyl aspartate:

[0051] Benzyl L-aspartate (5.7 g) was vacuum-dried for at least 2 hours, then added 200 mL of ethyl acetate, and heated to reflux at 90 °C for 0.5 h. Another weighed triphosgene solid (2.93 g) was dissolved in 60 mL of ethyl acetate, and then the solution was slowly added dropwise to the solution of L-aspartic acid benyl ester, and stirred thoroughly until clear. All operations were performed under the protection of dry argon. Stop heating, wash with saturated sodium bicarbonate solution 2 to 3 times in a 500 mL separatory funnel to remove excess triphosgene, add saturated sodium chloride to break the emulsion, and make the solution clear. Pour the reaction solution into a 500 mL Erlenmeyer flask filled with anhydrous magnesium sulfate, and dry for more than half an hour to remove water. After drying, f...

Embodiment 2

[0062] Preparation of Polymer Nanocarriers Loading Hydrophobic Drugs and Basic Performance Test

[0063] 2.1 Preparation of polymer nanocarriers loaded with hydrophobic drugs:

[0064] Dissolve AC-DEX-PAsp(DET)-CD polymer (2.5 mg) and doxorubicin hydrochloride (0.45 mg) in 1 mL of dichloromethane and 100 L of chloroform, respectively, and add doxorubicin hydrochloride in chloroform Add 4 L of triethylamine to adjust to hydrophobic doxorubicin, and mix the two evenly. Take 41 L of pure water as the internal water phase, and add it dropwise to the mixed solvent under ultrasonic conditions in a water bath to form a milky red water / oil (W / O) colostrum solution. Then, the colostrum system was added dropwise to 6 mL of the external aqueous phase under ultrasonic conditions of the probe to form a water / oil / water (W / O / W) composite system. Finally, transfer it to a constant temperature magnetic stirrer, stir at 30°C for 3 h to remove the organic phase to obtain a blue-purple ...

Embodiment 3

[0068] Preparation and Basic Performance Test of Polymer AC-DEX-PAsp(DET)-CD Nanoparticles Simultaneously Loading Hydrophobic Drugs and Plasmid DNA

[0069] 3.1 Preparation of polymer nanoparticles loaded with hydrophobic drugs and plasmid DNA

[0070] The polymer AC-DEX-PAsp(DET)-CD (2.5 mg) and doxorubicin hydrochloride (0.45 g) were dissolved in 1 mL of dichloromethane and 100 L of chloroform, respectively, and then added to the chloroform solution of doxorubicin hydrochloride Add 4 L of triethylamine to make it hydrophobic doxorubicin, and finally mix the two evenly. Take a certain amount of DNA aqueous solution as the inner water phase (determined according to different N / P=1; N / P=12; N / P=24; N / P=42; N / P=60; N / P=72 The amount of DNA added) was added dropwise to this mixed solvent under ultrasonic conditions in a water bath to form a milky red water / oil (W / O) colostrum solution. Then this solution was slowly added to 6 mL of pure water under the ultrasonic condit...

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Abstract

The invention discloses a preparation method of a degradable acid-sensitive polyaspartamide copolymer and a use of the degradable acid-sensitive polyaspartamide copolymer as a drug and a gene co-transmission nanoparticle. Hydrophilic and hydrophobic sections of the degradable acid-sensitive polyaspartamide copolymer respectively comprise aziridine-grafted polyaspartic acid and acetalated dextran, and a molecular weight ratio of the aziridine-grafted polyaspartic acid to acetalated dextran is 1: 1-10. The preparation method comprises that dextran undergoes an acetalation reaction, the reaction product is bonded to nitrine-terminated poly(b-benzyl-L-aspartate), through a benzyl ester aminolysis reaction, and the combined product is bonded to polyaziridine so that an acetalated dextran-polyaziridine-grafted polyaspartic acid derivative with acid sensitivity and degradability is prepared. The copolymer can form nanoparticles with uniform particle sizes and stability by a double emulsification method, and can be combined with a carrying drug and a gene and realizes targeting conveying to tumor cells so that tumor chemotherapy and gene treatment synergism is obtained. The copolymer has a wide application prospect in the field of tumor treatment.

Description

technical field [0001] The invention relates to a copolymer, more specifically, to a degradable acid-sensitive polyasparagine copolymer and its preparation method and application. Background technique [0002] The occurrence of tumors is the result of long-term effects of various reasons, rather than instantaneous outbreaks, and the most promising gene therapy for clinical use is to a large extent only effective for a mutated gene, which is far from meeting the current needs for tumor treatment. Therefore, through the synergistic effect of multiple treatment methods, it is expected to significantly improve the therapeutic effect of tumors by improving the deficiency of single treatment and exerting the synergistic effect of multiple treatments. At present, the combination therapy of multiple drugs is mainly used clinically. Although this method reduces the dosage to a certain extent and increases the curative effect, if the body produces a physiological reaction, it is diffi...

Claims

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Application Information

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IPC IPC(8): C08G81/00C08B37/02C08G69/14A61K47/36A61P35/00
Inventor 戴箭李倩倩陈维聪
Owner SUN YAT SEN UNIV
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