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Potential of hydrogen (pH) response random copolymer based on poly-beta amino ester and preparation method and application thereof

A technology of random copolymers and amino esters, which is applied in the direction of medical preparations of non-active ingredients, drug combinations, antineoplastic drugs, etc., can solve the problems of drug side effects, slow process, and aggravated burst release, and achieve high load The effect of the dose

Inactive Publication Date: 2012-08-08
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are two major problems: one is the toxic and side effects of drugs; the other is the drug resistance of tumors (cancer cells)
In the usual micellar drug-loading system, there is a certain spatial distance between the drug-loaded layer and the pH-responsive layer, which makes the process of pH response-micelle swelling-drug release of the micelles slow, and the response to environmental pH changes is not accurate and sensitive enough. However, if too many pH-responsive groups are added, the drug-loading capacity will be reduced, and the burst release phenomenon will also be aggravated.

Method used

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  • Potential of hydrogen (pH) response random copolymer based on poly-beta amino ester and preparation method and application thereof
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  • Potential of hydrogen (pH) response random copolymer based on poly-beta amino ester and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0092] (1) Synthesis of HO-PLA-OH (A:B:C=100:5:1, A represents the monomer lactide, B represents the initiator 1,4-butanediol, C represents the catalyst Sn(Oct) 2 , the ratio is mass percentage, the same below). Add a stirring bar and monomeric lactide (20 g, 93.9 parts) into a 100 mL reaction bottle with a stirring bar, seal it and pump-ventilate three times, under the protection of argon, add the solvent toluene (40 mL ) and catalyst Sn(Oct) 2 (0.3 mg, 1.41 parts) and the initiator 1,4-butanediol (1 g, 4.69 parts). After freezing with liquid nitrogen, vacuumize-heat-inflate three times, and react in an oil bath at 100 °C for 24 h under the protection of argon. After the reaction was completed, the obtained solution was evaporated under reduced pressure to remove toluene, and then the polymer was dissolved in chloroform to obtain a solution, which was slowly added to 300 mL (equivalent to 10 times the volume of the solution) of refrigerated methanol / water (1:1, v / v), wash...

Embodiment 2

[0098] (1) Synthesis of HO-PLA-OH (A:B:C=100:15:3, A represents the monomer lactide, B represents the initiator 1,4-butanediol, C represents the catalyst Sn(Oct) 2 , the ratio is mass percentage, the same below). Add a stirrer and monomeric lactide (10 g, 91.32 parts) into a 100 mL reaction bottle with a stirrer, seal it and pump-ventilate three times, under the protection of argon, add the solvent toluene (40 mL ) and catalyst Sn(Oct) 2 (0.15 mg, 1.37 parts) and the initiator 1,4-butanediol (0.8 g, 7.31 parts). After freezing with liquid nitrogen, vacuumize-heat-inflate three times, and react in an oil bath at 95 °C for 30 h under the protection of argon. After the reaction was completed, the obtained solution was evaporated under reduced pressure to remove toluene, and then the polymer was dissolved in chloroform to obtain a solution, which was slowly added to 300 mL (equivalent to 10 times the volume of the solution) of refrigerated methanol / water (1:1, v / v), washed twi...

Embodiment 3

[0103] (1) Synthesis of HO-PLA-OH (A:B:C=300:5:1, A represents the monomer lactide, B represents the initiator 1,4-butanediol, C represents the catalyst Sn(Oct) 2 , the ratio is mass percentage, the same below). Add a stirrer and monomeric lactide (30 g, 98.04 parts) into a 100 mL reaction bottle with a stirrer, seal it and pump-ventilate three times, under the protection of argon, add the solvent toluene (40 mL ) and catalyst Sn(Oct) 2 (0.1 mg, 0.33 parts) and the initiator 1,4-butanediol (0.5 g, 1.63 parts). After freezing with liquid nitrogen, vacuumize-heat-inflate three times, and react in an oil bath at 105 °C for 20 h under the protection of argon. After the reaction was completed, the obtained solution was evaporated under reduced pressure to remove toluene, and then the polymer was dissolved in chloroform to obtain a solution, which was slowly added to 300 mL (equivalent to 10 times the volume of the solution) of refrigerated methanol / water (1:1, v / v), washed twic...

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Abstract

The invention discloses a potential of hydrogen (pH) response random copolymer based on poly-beta amino ester and a preparation method and application thereof. Firstly, polylactic acid with two ends sealed with hydroxide radicals is synthesized through a solution polymerization method, propylene serves as a macro-monomer after acidification, and a pH response amphiphilic copolymer is prepared through the Michael gradual addition reaction. The proportion of functional groups in the polymer molecule can be regulated. The synthetic process is simple, and the production rate is high. By means of a polymeric micelle obtained through a dialysis method and with a hydrophobic group (polylactic acid) and a pH response group (poly-beta amino ester) forming a kernel and a hydrophilic group forming acasing, water slight-solubility anti-cancer drugs can be coated into the kernel of the micelle, and the drugs can be slowly released in low quantity under neutral or weak alkaline conditions and can be quickly and controllably released under weakly acidic conditions.

Description

technical field [0001] The invention relates to the field of high molecular polymer materials for biomedicine, in particular to a poly-based β pH-responsive random copolymers of amino esters and their preparation and applications. Background technique [0002] Cancer has increasingly become the main killer that endangers human life and health, and chemotherapy is the most important and effective treatment method except surgery. However, there are two major problems: one is the toxic and side effects of drugs; the other is the drug resistance of tumors (cancer cells). Although many anticancer drugs can treat cancer pharmacologically, however, due to the hydrophobicity or poor water solubility of the drugs (such as doxorubicin, camptothecin, paclitaxel, etc.), the clinical therapeutic effect is affected, so for this kind of anticancer drugs application still faces great challenges. [0003] The nano-core-shell micelles formed by the amphiphilic copolymer are used as the car...

Claims

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Application Information

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IPC IPC(8): C08G73/00A61K47/34A61P35/00
Inventor 章莉娟张灿阳杨友强赵斌孙尧郭新东
Owner SOUTH CHINA UNIV OF TECH
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