Nanometer carrier system for tumor in-situ assembly, medicine carrying system and application

A nanoparticle and polyethylene glycol technology, applied in the direction of anti-tumor drugs, nano-drugs, nano-technology, etc., can solve the problems of unsatisfactory drug delivery, the inability of drugs to reach extracellular target sites, and the inability to exert anti-tumor effects. Good biocompatibility and degradability, enhanced enrichment and retention, effects of avoiding uptake

Active Publication Date: 2022-08-02
GUANGZHOU FIRST PEOPLES HOSPITAL (GUANGZHOU DIGESTIVE DISEASE CENT GUANGZHOU FIRST PEOPLES HOSPITAL GUANGZHOU MEDICAL UNIV THE SECOND AFFILIATED HOSPITAL OF SOUTH CHINA UNIV OF TECH)
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Therefore, the traditional nano-delivery system of anti-tumor drugs with intracellular targets in the past can no longer meet the delivery of these drugs, and may deliver these drugs into the cells, resulting in the inability of the drugs to reach the extracellular target sites, thus failing to exert anti-tumor effects

Method used

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  • Nanometer carrier system for tumor in-situ assembly, medicine carrying system and application
  • Nanometer carrier system for tumor in-situ assembly, medicine carrying system and application
  • Nanometer carrier system for tumor in-situ assembly, medicine carrying system and application

Examples

Experimental program
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Effect test

Embodiment 1

[0053] Example 1: Synthesis and characterization of polyethylene glycol-polylactic acid modified with bioorthogonal groups

[0054] 1. Synthesis of polyethylene glycol-polylactic acid modified by bioorthogonal groups

[0055] DA Cys-PEG-b-PLA is a tert-butoxycarbonyl-protected cysteine ​​(Boc-Cys) and aminated polyethylene glycol-polylactic acid through an amidation reaction, further deprotected by Boc and treated with 2,3-diol Methylmaleic anhydride shielded cysteine ​​residues obtained.

[0056] DA The synthetic route of Cys-PEG-b-PLA polymer material is as follows figure 1 shown.

[0057] Preparation and pretreatment of the required components include:

[0058] (1) Synthesis of tert-butoxycarbonyl-protected cysteine:

[0059] To a 100 mL clean round-bottomed flask, add cysteine ​​(5 g, 0.029 mol) and 50 mL of ultrapure water, and add magnetic stirring to dissolve cysteine. Weigh NaHCO again 3 (2.436 g, 0.029 mol) was added to the above cysteine ​​aqueous solution, c...

Embodiment 2

[0073] Example 2: Nanoparticles and applications of polyethylene glycol-polylactic acid modified at the end of bioorthogonal groups

[0074] 1. Preparation of D-NP and C-NP nanoparticles

[0075] Two kinds of bioorthogonal group surface-modified nanoparticles and their drug-loaded nanoparticles were prepared by nanoprecipitation method or single emulsification method. The specific methods are as follows:

[0076] Weigh 10mg DA Cys-PEG-b-PLA or 10 mg CBT-PEG-b-PLA were dissolved in 1 mL of DMSO, respectively. After vortexing to dissolve completely, the material solution was dropped into the aqueous phase (10 mL, 1×PBS, pH 7.4) and stirred for 2 h. Two types of nanoparticles were obtained. The particle solution was put into a dialysis bag with MWCO=14000Da and put into 1×PBS (pH 7.4, 2L) for dialysis overnight. Then use YM-30 ultrafiltration centrifuge tube (Millipore, MWCO5000Da) for ultrafiltration concentration to prepare D-NP and C-NP nanoparticles.

[0077] 2. Character...

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Abstract

The invention belongs to the technical field of anti-tumor nano-carriers, and discloses a nano-carrier system for tumor in-situ assembly, a drug loading system and application. The tumor in-situ assembled nano drug delivery system disclosed by the invention is composed of nano particles prepared from a polyethylene glycol-polylactic acid material with a specific structure, so that long circulation of the nano particles in blood can be realized; when the nano-particles reach a weak acid environment of tumors, the nano-particles can be assembled into large-size particle aggregates in situ in the tumors, enrichment and retention of a nano drug carrying system and carried drugs in the tumors can be enhanced, and the nano-particles serve as an extracellular'drug warehouse 'to slowly release the carried drugs to reach extracellular target spots, so that the anti-tumor curative effect is achieved; and a new thought is provided for developing a delivery carrier system of extracellular / membrane target antitumor drugs.

Description

technical field [0001] The invention relates to the technical field of anti-tumor nano-carriers, in particular to a nano-carrier system assembled in situ for tumors, a drug-carrying system and applications. Background technique [0002] Tumor-targeted drugs refer to drugs or their preparations endowed with targeting ability. The purpose is to enable the drug or its carrier to target specific lesions and accumulate or release active ingredients at the target site. [0003] At present, most of the targets of antitumor drugs are located in the cell or nucleus, and it is necessary to deliver these drugs to the target site in the cell in order to exert their efficacy. The basic design principle of the vast majority of nano-anti-tumor drug carriers in the prior art is: encapsulating the drug through physical interaction or carrying the drug through chemical covalent bonding. After intravenous administration, it is modified by ligands. Or its scale effect (particle size is usuall...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G63/91C08G63/664C08G63/685A61K31/381A61K47/54A61K47/59A61K47/60A61K47/69A61P35/00A61P35/04B82Y5/00B82Y40/00
CPCC08G63/912C08G63/664C08G63/6852A61K47/6937A61K47/593A61K47/60A61K47/545A61K47/542A61K31/381A61P35/00A61P35/04B82Y5/00B82Y40/00Y02P20/55
Inventor 曹紫洋杨显珠郑允圣刘梦婷马鹏跃
Owner GUANGZHOU FIRST PEOPLES HOSPITAL (GUANGZHOU DIGESTIVE DISEASE CENT GUANGZHOU FIRST PEOPLES HOSPITAL GUANGZHOU MEDICAL UNIV THE SECOND AFFILIATED HOSPITAL OF SOUTH CHINA UNIV OF TECH)
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