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5-boron pyridine carboxylic acid modified targeted drug delivery system and preparation method thereof

A boracic acid delivery system technology, applied in drug delivery, pharmaceutical formulation, drug combination, etc., can solve the problems of limited boric acid derivatives, improve biocompatibility and stability, improve drug delivery effect, good The effect of biocompatibility

Active Publication Date: 2020-09-29
INNER MONGOLIA UNIV FOR THE NATITIES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the current research on boronic acid derivatives is still limited, and their application in the field of tumor therapy needs further development

Method used

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  • 5-boron pyridine carboxylic acid modified targeted drug delivery system and preparation method thereof
  • 5-boron pyridine carboxylic acid modified targeted drug delivery system and preparation method thereof
  • 5-boron pyridine carboxylic acid modified targeted drug delivery system and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] This example is a control example. In this example, no modification with 5-boropyridine carboxylic acid is used, and only drug-loaded nanoparticles are used alone. The preparation method of this embodiment is:

[0033] S1, using two monomers of lactide (LA) and glycolide (GA) for ring-opening copolymerization to obtain a polymer (PLGA), which is then functionalized and reacted with polyethyleneimine (PEI) for amidation reaction, thereby Graft PEI to prepare PLGA-PEI amphiphilic copolymer.

[0034] The specific steps of S1 are:

[0035] ① Using 1,8-octanediol as the initiator and stannous octoate as the catalyst, the PLGA copolymer was synthesized by ring-opening polymerization of LA and GA monomers;

[0036] 2. Esterifying the terminal hydroxyl group of the PLGA polymer obtained in step 1. with succinic anhydride to obtain the polymer PLGA-COOH whose terminal group is a carboxyl group;

[0037] ③ using the terminal carboxyl group of the PLGA-COOH polymer obtained in ...

Embodiment 2

[0040] This example discloses a targeted drug delivery system modified with 5-boropyridine carboxylic acid and its preparation method. The system of this embodiment includes:

[0041] (a) an aqueous solution of 5-boropyridinecarboxylic acid;

[0042] (b) PLGA-PEI drug-loaded nanoparticles combined with drugs;

[0043] The 5-boropyridinecarboxylic acid has a negative charge, the drug-loaded nanoparticles have a positive charge, and the 5-bororopyridinecarboxylic acid and the drug-loaded nanoparticles are combined through electrostatic interaction.

[0044] The production and application method of this embodiment includes the following steps:

[0045] S1, using two monomers of lactide (LA) and glycolide (GA) for ring-opening copolymerization to obtain a polymer (PLGA), which is then functionalized and reacted with polyethyleneimine (PEI) for amidation reaction, thereby Graft PEI to prepare PLGA-PEI amphiphilic copolymer.

[0046] The specific steps of S1 are:

[0047] ① Usi...

Embodiment 3

[0053] This example discloses a targeted drug delivery system modified with 5-boropyridine carboxylic acid and its preparation method. The system of this embodiment includes:

[0054] (a) an aqueous solution of 5-boropyridinecarboxylic acid;

[0055] (b) PLGA-PEI drug-loaded nanoparticles combined with drugs;

[0056] The 5-boropyridinecarboxylic acid has a negative charge, the drug-loaded nanoparticles have a positive charge, and the 5-bororopyridinecarboxylic acid and the drug-loaded nanoparticles are combined through electrostatic interaction.

[0057] The production and application method of this embodiment includes the following steps:

[0058] S1, using two monomers of lactide (LA) and glycolide (GA) for ring-opening copolymerization to obtain a polymer (PLGA), which is then functionalized and reacted with polyethyleneimine (PEI) for amidation reaction, thereby Graft PEI to prepare PLGA-PEI amphiphilic copolymer.

[0059] The specific steps of S1 are:

[0060] ① Usi...

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Abstract

The invention discloses a 5-boron pyridine carboxylic acid modified targeted drug delivery system and a preparation method thereof. The system comprises a negatively charged 5-boron pyridine carboxylic acid aqueous solution and positively charged drug-loaded nanoparticles, and the two are combined through electrostatic interaction. The preparation method comprises the following steps: (1) carryingout ring-opening copolymerization on lactide (LA) and glycolide (GA) to obtain a polymer PLGA, carrying out amidation reaction on the polymer PLGA and polyethyleneimine (PEI) through functionalization, and performing grafting of the PEI to obtain a PLGA-PEI amphiphilic copolymer; (2) carrying out self-assembly on the PLGA-PEI amphiphilic polymer and a drug in a water phase to form drug-loaded nanoparticles with positive charges on the surfaces; and (3) adding the negatively charged 5-boron pyridine carboxylic acid into the drug-loaded nanoparticles with positive charges on the surfaces to form the drug delivery system. The drug delivery system disclosed by the invention has efficient targeting property and high biocompatibility on tumor cells, and is beneficial to carrying drugs to be efficiently enriched in tumor tissues and enter the tumor cells, so that the drug delivery effect is greatly improved, and the purpose of treatment of tumors is achieved.

Description

technical field [0001] The invention relates to the field of molecular biology, in particular to a targeted drug delivery system modified with 5-boropyridine carboxylic acid and a preparation method thereof. Background technique [0002] In recent years, nanoparticle-based drug delivery systems have become a very promising approach for tumor therapy due to their preferential accumulation at tumor sites. However, efficient tumor-specific drug delivery is still one of the major challenges for drug delivery to treat tumors. In general, nanoparticles with suitable particle size, shape and surface potential can be enriched in tumor tissue through the high permeability and long retention effect (EPR effect), thus possessing passive tumor targeting function. However, this passive tumor targeting is non-specific and cannot provide efficient tumor targeting for nanoparticles, thus greatly limiting the drug delivery efficiency. Therefore, in order to endow nanoparticles with active ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/54A61K47/69A61K45/00A61P35/00
CPCA61K47/545A61K47/6937A61K45/00A61P35/00
Inventor 郝雪芳盖微微
Owner INNER MONGOLIA UNIV FOR THE NATITIES
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