A kind of degradable acid-sensitive polyasparagine copolymer and its preparation method and application

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, improving bioavailability and excellent biocompatibility

Inactive Publication Date: 2018-02-06
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. Therefore, it is urgent to introduce new materials into the joint delivery system of genes and drugs in order to obtain better synergistic therapeutic effects of drugs and genes

Method used

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  • A kind of degradable acid-sensitive polyasparagine copolymer and its preparation method and application
  • A kind of degradable acid-sensitive polyasparagine copolymer and its preparation method and application
  • A kind of degradable acid-sensitive polyasparagine copolymer and its preparation method and application

Examples

Experimental program
Comparison scheme
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-type benzyl aspartate:

[0051] After vacuum-drying benzyl L-aspartate (5.7 g) for at least 2 hours, 200 mL of ethyl acetate was added, and heated to reflux at 90° C. for 0.5 h. Another weighed triphosgene solid (2.93g) was dissolved in 60mL of ethyl acetate, and then the solution was slowly added dropwise to the solution of L-aspartic acid benyl ester, and fully stirred 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 500mL separatory funnel to remove excess triphosgene, add saturated sodium chloride to break the emulsion, and make the solution clear. The reaction solution was poured into a 500 mL Erlenmeyer flask filled with anhydrous magnesium sulfate, dried for more than half an hour to remove water, after drying wa...

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 then add to the chloroform solution of doxorubicin hydrochloride 4L of triethylamine was adjusted to hydrophobic doxorubicin, and the two were mixed evenly. Take 41L 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 the ultrasonic condition 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 hours to remove the organic phase ...

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]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 4 L was added to the chloroform solution of doxorubicin hydrochloride Triethylamine to adjust it into hydrophobic doxorubicin, and finally mix the two evenly. Get 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 the 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 6mL of pure water under the ultrasonic condition of the p...

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Abstract

The invention discloses a method for synthesizing a degradable acid-sensitive polyasparagine copolymer and as a drug and gene co-transporting nanoparticle. The hydrophilic and hydrophobic segments of the present invention are respectively composed of polyaspartic acid grafted with polyethyleneimine and acetalized dextran, and the corresponding molecular weight ratio is 1:1-10. In the preparation method of the present invention, dextran is subjected to an acetalization reaction, and then combined with azide-terminated polyaspartic acid benzyl ester, and polyethylenimine is bonded through the aminolysis reaction of the benzyl ester to prepare a Acetalized Dextran-Polyethyleneimine Grafted Polyaspartic Acid Derivatives with Acid Sensitivity and Degradability. The polymer of the present invention can form nanoparticles with uniform particle size and stability by means of double emulsification, which can be combined with drugs and genes and delivered to tumor cells at the same time, achieving the synergistic effect of tumor chemotherapy and gene therapy. The therapeutic field has broad application prospects.

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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Patent Type & Authority Patents(China)
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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