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Charge reversal type polymeric micelles, charge reversal type polymeric drug-loading micelles and their preparation methods

A flip-type, polymer technology, used in pharmaceutical formulations, non-active ingredients medical preparations, emulsion delivery, etc., can solve the problems of tumor accumulation and poor permeability, poor blood circulation stability, and no environmental responsiveness. Achieve the effect of improving drug release efficiency, strong reduction responsiveness, and good biocompatibility

Active Publication Date: 2019-01-04
SOUTHWEST UNIVERSITY FOR NATIONALITIES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In view of the problems of poor biocompatibility, poor blood circulation stability, poor tumor accumulation and permeability, and no environmental responsiveness existing in polymer micelles currently used as drug carriers, the primary purpose of the present invention is to provide a charge-reversal polymer Micelles and preparation method thereof, the method can prepare double responsiveness (reduction responsiveness and pH responsiveness) polymer micelles with good biocompatibility, low toxicity and side effects, and high responsiveness to tumor cell microenvironment

Method used

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  • Charge reversal type polymeric micelles, charge reversal type polymeric drug-loading micelles and their preparation methods
  • Charge reversal type polymeric micelles, charge reversal type polymeric drug-loading micelles and their preparation methods
  • Charge reversal type polymeric micelles, charge reversal type polymeric drug-loading micelles and their preparation methods

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] (1) Preparation of polybenzyloxycarbonyl lysine

[0054] Dissolve allylamine and benzyloxycarbonyllysine anhydride in DMF at a molar ratio of 1:15 to form a mixed solution with a total solute concentration of 0.50 g / mL, then react at 25°C for 12 hours, and then add to the reaction product Add diethyl ether for precipitation until the precipitated product no longer increases, and the resulting precipitated product is suction-filtered and dried at 60°C and 0.010MPa for 24 hours to obtain polybenzyloxycarbonyllysine.

[0055] (2) Preparation of polybenzyl glutamate

[0056] Dissolve allylamine and benzyl glutamate anhydride in DMF at a molar ratio of 1:20 to form a mixed solution with a total solute concentration of 0.50 g / mL, then react at 25°C for 12 hours, and then add Precipitate with diethyl ether until the precipitated product no longer increases, and the resulting precipitated product is suction-filtered and dried at 60°C and 0.010MPa for 24 hours to obtain polyben...

Embodiment 2

[0077] (1) Preparation of polybenzyloxycarbonyl lysine

[0078] Dissolve allylamine and benzyloxycarbonyllysine anhydride in CH at a molar ratio of 1:25 2 Cl 2 In this method, a mixed solution with a total solute concentration of 0.40g / mL was prepared, and then reacted at 30°C for 18 hours, and then added ether to the reaction product for precipitation until the precipitated product no longer increased. Dry at 60°C and 0.012MPa for 24 hours to obtain polybenzyloxycarbonyllysine.

[0079] (2) Preparation of polybenzyl glutamate

[0080] Dissolve allylamine and benzyl glutamate anhydride in CH at a molar ratio of 1:30 2 Cl 2 In this method, a mixed solution with a total solute concentration of 0.40g / mL was prepared, and then reacted at 30°C for 18 hours, and then added ether to the reaction product for precipitation until the precipitated product no longer increased. Dry at 60°C and 0.012MPa for 24 hours to obtain polybenzyl glutamate.

[0081] (3) Preparation of charge-re...

Embodiment 3

[0086] (1) Preparation of poly-tert-butoxycarbonyl lysine

[0087] Dissolve allylamine and tert-butoxycarbonyllysine cyclic anhydride in DMSO at a molar ratio of 1:35 to form a mixed solution with a total solute concentration of 0.30 g / mL, then react at 35°C for 24 hours, and then to the reaction product Diethyl ether was added to precipitate until the precipitated product no longer increased, and the obtained precipitated product was suction-filtered and dried at 60°C and 0.014MPa for 24 hours to obtain poly-tert-butoxycarbonyllysine.

[0088] (2) Preparation of poly tert-butyl glutamate

[0089] Dissolve allylamine and tert-butyl glutamate anhydride in THF at a molar ratio of 1:40 to form a mixed solution with a total solute concentration of 0.25 g / mL, then react at 25°C for 24 hours, and then add to the reaction product Add diethyl ether for precipitation until the precipitated product no longer increases, and the resulting precipitated product is suction-filtered and drie...

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Abstract

The invention discloses charge reversal type polymeric micelles, charge reversal type polymeric drug-loading micelles and their preparation methods. Alkaline polyamino acid containing protecting groups and acidic polyamino acid containing protecting groups are subjected to crosslinking reaction under the crosslinking action of BACy crosslinker so as to obtain a crosslinked polymer; the crosslinkedpolymer is hydrolyzed such that the protecting groups are removed separately from the alkaline polyamino acid and the acidic polyamino acid in the crosslinked polymer so as to obtain the charge reversible type polymeric micelles with three-dimensional mesh structure formed by crosslinking of positively charged polyamino acid and negatively charged polyamino acid. The charge reversal type polymeric micelles and the charge reversal type polymeric drug-loading micelles have good structural stability, good biocompatibility, low long-term toxicity and the like, also have reduction response and pHresponse, are available for long-term accumulation and high permeation in tumor cells, and provide a higher release rate of drugs.

Description

technical field [0001] The invention belongs to the technical field of drug carrier and its preparation, and relates to a reduction-responsive, pH-responsive polymer micelle and a drug-loaded micelle with a tumor cell microenvironment responsiveness, in particular to a charge-reversal polymer micelle And a drug-loaded micelle based on the charge-reversal polymer micelle and a preparation method thereof. Background technique [0002] Polymer micelles are nanoparticles formed by the self-assembly of amphiphilic polymers in aqueous solution. The particle size is generally 10-200 nm. Tumor areas clustered. At the same time, polymer micelles can not only use the hydrophobic core to encapsulate drug molecules, but the hydrophilic shell can make them stably dispersed in aqueous solution. Therefore, polymer micelles are widely used in the delivery of anticancer drugs. However, to complete the delivery of drugs in vivo, polymer micelles as carriers not only need to have excellent b...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08F283/04C08F222/38A61K47/34A61K9/107
CPCA61K9/1075A61K47/34C08F283/045C08F222/385
Inventor 周庆翰屈婧
Owner SOUTHWEST UNIVERSITY FOR NATIONALITIES
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