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Polymer-functionalized modified mesoporous carbon nanoparticles and their preparation and application

A nanoparticle and mesoporous carbon technology, applied in the field of medicine, can solve the problems of limited absorption of nanoparticles by epithelial cells and reduced affinity between nanoparticles and cell membranes

Active Publication Date: 2022-08-02
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It has been reported that the modification of nanocarriers with hydrophilic neutral polymers such as PEG can enable rapid diffusion of nanoparticles through the mucus layer, but reduces the affinity of nanoparticles and cell membranes, resulting in limited epithelial cell uptake of nanoparticles

Method used

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  • Polymer-functionalized modified mesoporous carbon nanoparticles and their preparation and application
  • Polymer-functionalized modified mesoporous carbon nanoparticles and their preparation and application
  • Polymer-functionalized modified mesoporous carbon nanoparticles and their preparation and application

Examples

Experimental program
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Effect test

Embodiment 1

[0062] An appropriate amount of HPMA and MA-GG-OH were weighed and dissolved in absolute ethanol, so that the total amount of reactants accounted for 12.5 wt% of the system, and the molar ratio of HPMA to MA-GG-OH was 4:1. Then 2wt% of AIBN was added to the above system, and the reaction was carried out at 50°C for 24h. After the reaction, the product was purified by lyophilization by dialysis to obtain pHPMA with a molecular weight of 49.8 kDa and a PDI of 1.42.

Embodiment 2

[0064] An appropriate amount of HPMA and MA-GG-OH were weighed and dissolved in absolute ethanol, so that the total amount of reactants accounted for 10 wt% of the system, and the molar ratio of HPMA to MA-GG-OH was 6:1. Then 3wt% of AIBN was added to the above system, and the reaction was carried out at 50°C for 24h. After the reaction, the product was purified by lyophilization by dialysis to obtain pHPMA with a molecular weight of 48.5 kDa and a PDI of 1.76.

Embodiment 3

[0066] An appropriate amount of HPMA and MA-GG-OH were weighed and dissolved in absolute ethanol, so that the total amount of reactants accounted for 15wt% of the system, wherein the molar ratio of HPMA and MA-GG-OH was 8:1. Then 4wt% of AIBN was added to the above system, and the reaction was carried out at 50°C for 24h. After the reaction, the product was purified by lyophilization by dialysis to obtain pHPMA with a molecular weight of 45.2 kDa and a PDI of 1.57.

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Abstract

The invention belongs to the technical field of medicine, and relates to polymer functionalized modified mesoporous carbon nanoparticles and preparation and application thereof, in particular to a polymer functionalized modified mesoporous carbon nanoparticle that can overcome multiple gastrointestinal absorption barriers and the same The drug delivery system prepared by the nanoparticle also relates to the application of the nanoparticle as a poorly soluble drug carrier in promoting oral drug absorption. In the present invention, chitosan is first covalently modified on the surface of mesoporous carbon nano-particles to improve the intestinal uptake of the carrier; then a hydrophilic negatively charged N-(2-hydroxypropyl) methacrylamide is added. The copolymer (pHPMA) was adsorbed to the surface of nanocarriers by electrostatic force, which improved the mucus penetration ability of the carrier. The drug delivery system constructed by the invention enables the drug to be highly dispersed in the mesoporous channel of the carrier with nanometer size, so that the drug exists in an amorphous state, and the oral absorption of the poorly soluble drug is promoted.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to polymer functionalized modified mesoporous carbon nanoparticles and preparation and application thereof, in particular to a polymer functionalized modified mesoporous carbon nanoparticle that can overcome multiple gastrointestinal absorption barriers and the same The drug delivery system prepared by the nanoparticle also relates to the application of the nanoparticle as a poorly soluble drug carrier in promoting oral drug absorption. Background technique [0002] Among many routes of administration, oral administration has good safety and patient compliance, and is the preferred route of administration for most drugs in clinical practice. However, the oral administration of a considerable number of drugs is severely limited due to their poor solubility, permeability and stability in the gastrointestinal tract. Recent studies have shown that nanocarriers can be used as oral delive...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/04A61K47/36A61K47/32A61K9/14A61K31/10
CPCA61K47/02A61K47/36A61K47/32A61K9/143A61K9/146A61K31/10
Inventor 王思玲赵勤富冉富
Owner SHENYANG PHARMA UNIVERSITY