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Preparation method of a microhydrogel capable of simultaneous loading and sustained release of hydrophilic and hydrophobic drugs

A hydrophobic drug, hydrophilic and hydrophobic technology, applied in the field of preparation of micro-hydrogels, can solve the problems of cumbersome synthesis process and affecting wide-scale use, and achieve the effects of reducing cytotoxicity, prolonging the drug delivery cycle, and improving stability

Active Publication Date: 2020-02-14
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the synthesis process of this material is relatively cumbersome, and it takes four steps of organic reactions to obtain polyethylene glycol monomethyl ether-S-trityl-L-cysteine-dopamine, and further micellization is required to obtain the final material, affecting its wide-ranging use

Method used

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  • Preparation method of a microhydrogel capable of simultaneous loading and sustained release of hydrophilic and hydrophobic drugs
  • Preparation method of a microhydrogel capable of simultaneous loading and sustained release of hydrophilic and hydrophobic drugs
  • Preparation method of a microhydrogel capable of simultaneous loading and sustained release of hydrophilic and hydrophobic drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] Hydroxyethyl methacrylate (1.3 g, 10 mmol) and sodium carbonate (2.1 g, 20 mmol) were dissolved in 40 ml of dichloromethane, and cooled to 0° C. in an ice bath. Weigh 4-dimethylaminopyridine (24 mg, 0.2 mmol) into the reaction flask, dissolve cinnamoyl chloride (0.34 g, 2 mmol) in 10 ml of dichloromethane, and slowly add it dropwise to the above solution with a constant pressure dropping funnel middle. After the dropwise addition, the ice bath was removed, and the reaction was stirred at room temperature for 24 hours. After the reaction was completed, sodium carbonate was removed by vacuum water pump filtration to obtain a colorless liquid. The colorless liquid was washed three times with 50 ml of saturated sodium chloride solution, separated to remove the inorganic phase, and the obtained organic layer was dried overnight with anhydrous magnesium sulfate to remove water. Magnesium sulfate was removed by vacuum water pump filtration, and dichloromethane was removed by...

Embodiment 2

[0063] Hydroxyethyl methacrylate (1.3 g, 10 mmol) and sodium carbonate (2.1 g, 20 mmol) were dissolved in 40 ml of dichloromethane and cooled to °C in an ice bath. Weigh 4-dimethylaminopyridine (24 mg, 0.2 mmol) into the reaction flask, dissolve cinnamoyl chloride (1.7 g, 10 mmol) in 10 ml of dichloromethane, and slowly add it dropwise to the above solution with a constant pressure dropping funnel middle. After the dropwise addition, the ice bath was removed, and the reaction was stirred at room temperature for 24 hours. After the reaction was completed, sodium carbonate was removed by vacuum water pump filtration to obtain a colorless liquid. The colorless liquid was washed three times with 50 ml of saturated sodium chloride solution, separated to remove the inorganic phase, and the obtained organic layer was dried overnight with anhydrous magnesium sulfate to remove water. Magnesium sulfate was removed by vacuum water pump filtration, and dichloromethane was removed by rot...

Embodiment 3

[0066] Hydroxyethyl acrylate (1.3 g, 10 mmol) and sodium carbonate (3.1 g, 30 mmol) were dissolved in 40 ml of dichloromethane and cooled to °C in an ice bath. Weigh 4-dimethylaminopyridine (24 mg, 0.2 mmol) into the reaction flask, dissolve cinnamoyl chloride (3.4 g, 20 mmol) in 10 ml of dichloromethane, and slowly add it dropwise to the above solution with a constant pressure dropping funnel middle. After the dropwise addition, the ice bath was removed, and the reaction was stirred at room temperature for 24 hours. After the reaction was completed, sodium carbonate was removed by vacuum water pump filtration to obtain a colorless liquid. The colorless liquid was washed three times with 50 ml of saturated sodium chloride solution, separated to remove the inorganic phase, and the obtained organic layer was dried overnight with anhydrous magnesium sulfate to remove water. Magnesium sulfate was removed by vacuum water pump filtration, and dichloromethane was removed by rotary ...

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Abstract

The invention relates to a drug loading and sustained release polymer material and provides a preparation method of microhydrogel capable of simultaneously loading and releasing hydrophilic and hydrophobic drugs. The preparation method comprises taking M1, M2 and an initiator, dissolving the M1, M2 and initiator in water, performing free radical copolymerization under anaerobic conditions at the copolymerization reaction temperature of 60-90 DEG C for 20 minutes, then adding a dichloromethane solution of M3 into the reaction system, continuing the reaction for 60 minutes, then adding a dichloromethane solution of M4 into the reaction system, continuing the reaction for 6-24 hours, after the copolymerization reaction, dialyzing the obtained product for one week, and carrying out freeze drying to obtain purified amphiphilic ion microhydrogel. The microhydrogel as a drug carrier can simultaneously load and release a plurality of hydrophobic and hydrophobic drugs, exert synergistic effectsof the drug combination and improve the therapeutic effect.

Description

technical field [0001] The invention relates to the field of polymer materials for drug loading and sustained release, in particular to a method for preparing a microhydrogel capable of simultaneously loading and releasing hydrophilic and hydrophobic drugs. Background technique [0002] Drug carrier is a kind of drug delivery system, which is mainly composed of lipid or polymer particle carrier and drug, and controls the release of drug by changing the way, route and binding mode of drug entering the organism. The introduction of drug carriers solves the problems of excessive toxicity of traditional preparations, poor stability in blood circulation, easy to be phagocytized by macrophages, and lack of targeting, etc., reduces cytotoxicity, prolongs the administration cycle, and slows down the drug release rate , improving the utilization of the drug. [0003] The complexity of pathology makes the treatment of diseases such as cancer a daunting challenge, and a single drug is...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K45/06A61K47/32A61P35/00A61P29/00C08F220/54C08F226/06C08F222/14
CPCA61K45/06A61K47/32A61P29/00A61P35/00C08F220/54C08F226/06C08F222/102
Inventor 杜滨阳周娴婧聂晶晶
Owner ZHEJIANG UNIV
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