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Weak acid ionizable amphiphilic zwitterionic carrier, micelle drug delivery system and preparation method and application thereof

A zwitterionic and amphiphilic technology, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., to reduce adsorption capacity and hemolysis ability, promote accumulation, and promote target cell uptake. Effect

Active Publication Date: 2020-06-23
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] At present, the design of protonated bifunctional zwitterion carriers based on high-efficiency anti-protein adsorption and lesion microacid environment response and its application in the field of tumor microenvironment regulation drug or biomacromolecule delivery have not been reported.

Method used

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  • Weak acid ionizable amphiphilic zwitterionic carrier, micelle drug delivery system and preparation method and application thereof
  • Weak acid ionizable amphiphilic zwitterionic carrier, micelle drug delivery system and preparation method and application thereof
  • Weak acid ionizable amphiphilic zwitterionic carrier, micelle drug delivery system and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Preparation of Polyethyleneimine Derivatives Modified by Sultaine (D-PEI)

[0047] Dissolve 0.4g PEI (MW 1800Da) in methanol solution, add 0.27g sulfobetaine monomer, react for 1-3 days, dialyze (MWCO=1kD) for 48-72h, freeze-dry to obtain sulfobetaine-modified polyethylene Amine derivatives (D-PEI).

Embodiment 2

[0049] Preparation of Carboxybetaine Modified Hydroxyethyl Chitosan Derivatives (D-HECS)

[0050] Dissolve 0.1g of hydroxyethyl chitosan in a mixed solution of dimethyl sulfoxide and methanol (v / v=1:3), add 0.59g of carboxybetaine monomer, react for 1-3 days, dialyze (MWCO= 14kD) for 48-72h, and freeze-dried to obtain carboxybetaine-modified hydroxyethyl chitosan derivatives (D-HECS).

Embodiment 3

[0052] Preparation of Carboxybetaine Modified Polylysine Derivatives (D-PLL)

[0053] Dissolve 0.5g polylysine (MW 10000Da) in a mixed solution of N,N-dimethylformamide and methanol (v / v=1:1), add 0.34g carboxybetaine monomer, and react 1- After 3 days, it was dialyzed (MWCO=3.5kD) for 48-72 hours, and freeze-dried to obtain carboxybetaine-modified polylysine derivatives (D-PLL).

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Abstract

The invention provides a weak-acid ionizable amphiphilic zwitterionic carrier, a micelle drug delivery system and a preparation method and an application thereof. The structural general formula of theamphiphilic zwitterionic carrier is as follows: Dn-CP-TAm, wherein CP is a hydrophilic cationic polymer skeleton, and D is a zwitterionic betaine monomer; wherein n is the grafting rate of a zwitterionic betaine monomer on a hydrophilic cationic polymer skeleton, TA is a pH-sensitive monomer molecule containing a tertiary amine structure, and m is the grafting rate of the pH-sensitive monomer molecule containing the tertiary amine structure on the cationic polymer; in the weak-acid ionizable amphiphilic zwitterionic carrier, the zwitterionic betaine monomer has an in-vivo protein adsorption resisting effect and can weaken the adsorption capacity and hemolysis capacity of the cationic polymer to protein, prolong the blood circulation time of the carrier and promote accumulation of the carrier at a disease part, so that the biomacromolecule drug delivery efficiency is improved.

Description

technical field [0001] The invention relates to an ion carrier and its preparation method and application, in particular to a weakly acid-ionizable amphiphilic amphoteric ion carrier, a micelle drug delivery system, its preparation method and its application. Background technique [0002] Tumor microenvironment refers to the internal and external environment of tumor cells. Tumor microenvironment-modulating drugs can inhibit tumors by regulating tumor-related immune cells, anti-tumor angiogenesis, and regulating the interaction between tumor cells and tumor-related cells in the microenvironment. role. Tumor microenvironment modulating drugs include natural drugs such as gambogic acid, celandine, quercetin, ceretin, curcumin, etc.; chemical drugs such as gemcitabine, pemetrexed, TGF-β inhibitors, and tinib, etc. Most of these drugs are poorly soluble, which is not conducive to in vivo delivery. As a commonly used drug delivery system, polymer micelles have the following adv...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G73/02C08G69/48C08B37/08A61K9/107A61K31/7088A61K45/00A61K47/34A61K47/36A61K47/40A61P35/00
CPCC08G73/0206C08G69/48C08B37/003A61K9/1075A61K45/00A61K31/7088A61K47/36A61K47/34A61K47/40A61P35/00
Inventor 殷婷婕周建平程节节褚旭新
Owner CHINA PHARM UNIV
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