Polymer functionalized modified mesoporous carbon nanoparticles and preparation and application thereof

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

Active Publication Date: 2019-09-06
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 preparation and application thereof
  • Polymer functionalized modified mesoporous carbon nanoparticles and preparation and application thereof
  • Polymer functionalized modified mesoporous carbon nanoparticles and preparation and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0062] Weigh an appropriate amount of HPMA and MA-GG-OH and dissolve them in absolute ethanol so that the total amount of reactants accounts for 12.5wt% of the system, and the molar ratio of HPMA to MA-GG-OH is 4:1. Then add 2wt% AIBN to the above system, and react at 50° C. for 24 hours. After the reaction, the product was purified by dialysis and lyophilization to obtain pHPMA with a molecular weight of 49.8kDa and a PDI of 1.42.

Embodiment 2

[0064] Weigh an appropriate amount of HPMA and MA-GG-OH and dissolve them in absolute ethanol so that the total amount of reactants accounts for 10wt% of the system, and the molar ratio of HPMA to MA-GG-OH is 6:1. Then add 3wt% AIBN to the above system, and react at 50° C. for 24 hours. After the reaction, the product was purified by dialysis and lyophilization to obtain pHPMA with a molecular weight of 48.5 kDa and a PDI of 1.76.

Embodiment 3

[0066] Weigh an appropriate amount of HPMA and MA-GG-OH and dissolve them in absolute ethanol so that the total amount of reactants accounts for 15wt% of the system, and the molar ratio of HPMA to MA-GG-OH is 8:1. Then add 4wt% AIBN to the above system, and react at 50° C. for 24 hours. After the reaction, the product was purified by dialysis and lyophilization 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 medicines, relates to polymer functionalized modified mesoporous carbon nanoparticles and preparation and application thereof, particularly relates to polymer functionalized modified mesoporous carbon nanoparticles capable of overcoming multiple gastrointestinal absorption barriers and a drug delivery system prepared from the nanoparticles, and alsorelates to application of the nanoparticles as insoluble drug carriers in promoting oral drug absorption. According to the invention, firstly, chitosan is covalently modified on the surfaces of the mesoporous carbon nanoparticles for improving intestinal uptake of carriers; and a hydrophilic and negatively charged N-(2-hydroxypropyl) methacrylamide copolymer (pHPMA) is adsorbed to the surfaces ofthe nano carriers through electrostatic force, so that the mucus permeability of the carriers is improved. According to an administration system constructed by the invention, drug is highly dispersedin mesoporous pore channels of the carriers in a nanometer size, so that the drug exists in an amorphous state, and oral absorption of the insoluble drug is promoted.

Description

technical field [0001] The invention belongs to the technical field of medicine, relates to polymer functionalized modified mesoporous carbon nanoparticles and its preparation and application, in particular to a polymer functionalized modified mesoporous carbon nanoparticle capable of overcoming multiple gastrointestinal absorption barriers and its The drug delivery system prepared by nanoparticle also relates to the application of the nanoparticle as a poorly soluble drug carrier in promoting oral drug absorption. Background technique [0002] Among the 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, due to the poor solubility, permeability and stability in the gastrointestinal tract of a considerable number of drugs, their oral administration is severely limited. Recent studies have shown that nanocarriers can be used as oral delivery vehic...

Claims

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Application Information

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Patent Type & Authority Applications(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
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