Reduction response type ABC type segmented polymer as well as preparation method and application thereof

A block polymer and responsive technology, which is applied in the direction of drug combination, pharmaceutical formulation, medical preparations of non-active ingredients, etc., can solve the problems of difficult stability and limited application range of micelles, so as to improve drug release rate, Effect of reducing drug leakage and improving therapeutic effect

Inactive Publication Date: 2018-10-19
HENAN NORMAL UNIV
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  • Abstract
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Problems solved by technology

However, the structure of polymer micelles will change with the change of the surrounding environment, and it is difficult to keep stable, which limits the application range of micelles.

Method used

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  • Reduction response type ABC type segmented polymer as well as preparation method and application thereof
  • Reduction response type ABC type segmented polymer as well as preparation method and application thereof
  • Reduction response type ABC type segmented polymer as well as preparation method and application thereof

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Embodiment Construction

[0025] The above-mentioned contents of the present invention are described in further detail below through the embodiments, but this should not be interpreted as the scope of the above-mentioned themes of the present invention being limited to the following embodiments, and all technologies realized based on the above-mentioned contents of the present invention all belong to the scope of the present invention.

[0026] (1) Synthesis of amphiphilic block copolymer mPEG-b-PAGE:

[0027]

[0028] Weigh 0.12g of sodium hydride (NaH, containing mineral oil, 60%), add it into a 100mL Shrek bottle under nitrogen atmosphere, and draw 10mL of anhydrous THF with a syringe at the same time, add it into the bottle, stir and wash for about 20min , stop stirring and suck away the supernatant in the bottle, then weigh 10.00g mPEG (Mn=5000) into the Shrek bottle, and put the bottle into a 100°C oil bath for stirring until the liquid in the bottle After NaH was dissolved in molten mPEG, 2.4...

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Abstract

The invention discloses a reduction response type ABC type segmented polymer as well as a preparation method and application thereof, and belongs to the technical field of a reduction response type medicine carrier. The hydrophilic monomethyl ether polyethylene glycol (mPEG), hydrophobic lactide (LA) and allyl glycidyl ether (AGE) are selected to be used as raw materials; then, sulfydryl-olefin light click reaction and ring opening polymerization are combined to synthetize a polymer mPEG-b-PAGESH-b-PLLA with hydrosulphonyl groups at the side chain; then, the self assembly is performed to forma micelle; under the existence of hydrogen peroxide, hydrosulphonyl groups are oxidized into disulfide bonds; finally, the reduction response type crosslinking micelle with high stability is synthesized. The crosslinking micelle with the disulfide bonds is favorable for reducing the medicine leakage and initial fast release; in addition, the reduction response performance is also realized in the pathological change positions; under the existence of reducing agents DTT and glutathione, the medicine release behavior of the crosslinking micelle is obviously accelerated, so that the treatment effect is improved.

Description

technical field [0001] The invention belongs to the technical field of reduction-responsive drug carriers, and in particular relates to a reduction-responsive ABC type block polymer and its preparation method and application. Background technique [0002] As a drug delivery carrier, polymer micelles have attracted more and more attention because of their characteristics of improving the solubility of hydrophobic drugs and reducing protein adsorption. However, the structure of polymer micelles will change with the change of the surrounding environment, and it is difficult to keep stable, which limits the application range of micelles. Therefore, in order to enhance the stability and integrity of the micelle structure, we need to modify the polymer chain segment and introduce bifunctional groups to cross-link the polymer micelle, thereby immobilizing the structure of the polymer micelle. [0003] Stimuli-responsive polymer cross-linked micelles mainly refer to a class of drug...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G65/331C08G65/332A61P35/00A61K47/34A61K31/704A61K9/107
CPCA61K9/1075A61K31/704A61K47/34A61P35/00C08G65/331C08G65/3328
Inventor 胡志国喻永杰王小坤
Owner HENAN NORMAL UNIV
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