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A kind of pH-responsive polymer micelles for mucus penetration and preparation method thereof

A technology of polymer micelles and mucus penetration is applied in the field of stimuli-responsive amphiphilic polymer micelles and their preparation, which can solve the problems of hindering the interaction between nanoparticles and cells, reducing the efficiency of nanoparticles entering cells, and reducing drugs. Achieve good mucus permeability, play a carrier role, and increase the effect of cell endocytosis

Inactive Publication Date: 2018-02-16
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the coating of polyethylene glycol improves the mucus penetration efficiency while hindering the interaction between nanoparticles and cells, reducing the efficiency of nanoparticles entering cells, thus reducing the release of more drugs in cells and improving the therapeutic effect. its application

Method used

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  • A kind of pH-responsive polymer micelles for mucus penetration and preparation method thereof
  • A kind of pH-responsive polymer micelles for mucus penetration and preparation method thereof
  • A kind of pH-responsive polymer micelles for mucus penetration and preparation method thereof

Examples

Experimental program
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preparation example Construction

[0036] A method for preparing a pH-responsive amphiphilic polymer conjugate, the steps are as follows:

[0037] 1) Polylactic acid-glycolic acid copolymer (PLGA), 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride, N-hydroxysuccinimide, adipic acid di The molar ratio of hydrazide is 1:(1.2~5):(1.2~5):(3~10) respectively dissolved in dimethyl sulfoxide, stirred and reacted at room temperature for 24~36 hours, dialyzed in pure water for 24~48 hours and then freeze-dried A hydrazinolated PLGA polymer was obtained.

[0038]2) Polyethylene glycol (PEG), p-aldehyde benzoic acid, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride, 4-dimethylaminopyridine in molar ratio 1:(1.2~5):(1.2~5):(3~10) were dissolved in N,N-dimethylformamide respectively, stirred and reacted at room temperature for 24~36h, precipitated and filtered with glacial ether, and dried under vacuum to obtain aldehyde Kylated PEG.

[0039] 3) Dissolve hydrazinated PLGA and aldylated PEG in dimethy...

Embodiment 1

[0050] Synthesis of pH-responsive amphiphilic polymer conjugates.

[0051] 1) Depolylactic-co-glycolic acid (PLGA) 1g, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride 100mg, N-hydroxysuccinimide 60mg, hexyl 75 mg of diacid dihydrazide was dissolved in 10 ml of dimethyl sulfoxide, stirred at room temperature for 24 hours, dialyzed in pure water for 24 hours, and then freeze-dried to obtain a hydrazinolated PLGA polymer.

[0052] 2) Polyethylene glycol (PEG) 2g, p-aldehyde benzoic acid 200mg, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride 192mg, 4-dimethylaminopyridine 100mg, respectively dissolved in 8ml of N,N-dimethylformamide, stirred at room temperature for 24h, precipitated with glacial ether, filtered, and dried in vacuo to obtain alhydized PEG.

[0053] 3) Dissolve 500mg of hydrazinolated PLGA and 640mg of aldehydelated PEG in 10ml of dimethyl sulfoxide, and reflux at 70°C for 72h under the protection of argon. After the reaction is completed, t...

Embodiment 2

[0056] Synthesis of pH-responsive amphiphilic polymer conjugates.

[0057] 1) Depolylactic-co-glycolic acid (PLGA) 0.4g, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride 70mg, N-hydroxysuccinimide 45mg, 55 mg of adipic dihydrazide was dissolved in 8 ml of dimethyl sulfoxide, stirred at room temperature for 28 hours, dialyzed in pure water for 26 hours, and then freeze-dried to obtain a hydrazinolated PLGA polymer.

[0058] 2) 0.3g of polyethylene glycol (PEG), 60mg of p-aldehyde benzoic acid, 80mg of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride, 4-dimethylamino Dissolve 30 mg of pyridine in 6 ml of N,N-dimethylformamide, stir at room temperature for 28 h, precipitate and filter with glacial ether, and dry in vacuo to obtain alhydized PEG.

[0059] 3) Dissolve 420mg of hydrazinolated PLGA and 650mg of aldehydelated PEG in 8ml of dimethyl sulfoxide, and reflux at 75°C for 64h under the protection of argon. After the reaction is completed, the reaction ...

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Abstract

The invention relates to a pH-responsive polymer micelle for mucus penetration and a preparation method thereof; PLGA and PEG are combined through a pH-responsive hydrazone bond to form an amphiphilic polymer conjugate, and post-assembled to form a pH-responsive polymer micelle. polymer micelles. Hydrazylated PLGA and aldehydelated PEG were dissolved in dimethyl sulfoxide and reacted under nitrogen; the reaction solution was dialyzed in N,N-dimethylformamide for 12 to 24 hours, then precipitated with ice ether, and centrifuged Drying of the precipitate yielded a pH-responsive hydrazone-linked amphiphilic conjugate. The prepared self-assembled drug carrier maintains a uniform and small particle size, has better biocompatibility, and has pH responsiveness. It can break the hydrazone bond and remove the protection of PEG in the mucus microenvironment with a low pH value. The exposed positively charged groups interact electrostatically with the negatively charged cell membranes, increasing the endocytosis of the micelles, allowing more carriers to enter the cells for slow and controlled release of drugs, and play the role of carriers.

Description

technical field [0001] The invention relates to a stimulus-responsive amphiphilic polymer micelle for mucus penetration and a preparation method thereof, belonging to the technical field of preparation of drug carrier materials. Background technique [0002] Mucus is a viscoelastic and adhesive gel substance that covers the surface of the body that is not covered by the skin, such as the lungs and respiratory tract, stomach, eyes, nasopharynx, female vagina, etc., and protects these parts from pathogens, particles, etc. and Infect. Some of the mucus is acidic. When lesions occur in these parts and drug treatment is required, the adhesion protection mechanism will become an obstacle that prevents the drug from directly reaching the lesion tissue and cells for effective treatment. Both small molecule drugs and traditional nanocarriers loaded with drugs will be adhered to the surface. The mucus is removed quickly. Therefore, deep penetration of the mucus barrier without comp...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08G81/00A61K9/107A61K47/34
Inventor 常津房蕾宫晓群张健杨文涛
Owner TIANJIN UNIV
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