A method for preparing nanomicelles with dual effects of mucus layer penetration and p-gp inhibition

A nano-micelle, dual-action technology, applied in the field of pharmacy, can solve the problems of retention, inaccessibility, and unfavorable phagocytosis and transport of small intestinal epithelial cells, and achieve the effect of simple operation, low manufacturing cost, and improved oral delivery efficiency

Active Publication Date: 2019-01-01
OCEAN UNIV OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Positively charged nano-preparations adhere to small intestinal epithelial cells through electrostatic interaction, and promote the phagocytosis and transport of nano-preparations by cells, but are easily trapped in the mucous layer of the mucous membrane and cannot reach the absorption site; it has a hydrophilic surface The electrically neutral or weakly negatively charged nano-preparations can quickly penetrate the mucosal mucus layer and reach the apical side of the small intestinal epithelial cells, but its electrically neutral hydrophilic surface is not conducive to the phagocytosis and transport of the small intestinal epithelial cells

Method used

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  • A method for preparing nanomicelles with dual effects of mucus layer penetration and p-gp inhibition
  • A method for preparing nanomicelles with dual effects of mucus layer penetration and p-gp inhibition

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Experimental program
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Embodiment 1

[0012] Weighed 60 mg of quercetin and dissolved it in 5 mL of dimethyl sulfoxide, added 20.2 mg of succinic anhydride and stirred at 40 °C for 4 hours. Weigh 38.4 mg EDC and 46 mg NHS and add into the reaction solution, and stir the reaction at room temperature for 30 minutes. Weigh 0.2 g of chitosan and dissolve it in 5 mL of water, add chitosan aqueous solution dropwise to the reaction solution, adjust the pH of the reaction solution to 5.0 with HCl, stir and react at room temperature for 6 hours, and place in dimethyl sulfoxide solution Dialyze for 2 days, then fully dialyze in deionized water, and freeze-dry to obtain chitosan-succinate; weigh 6 mg trisodium 6-phosphogluconate and dissolve it in 1.5 mL water, add 3.4 mg EDC, and adjust the pH to 5.0, stirred and reacted at 40°C for 30 minutes, weighed 30 mg of chitosan-quercetin succinate and dissolved it in 3 mL of water, added the aqueous solution of chitosan-quercetin succinate to the reaction solution drop by drop, Th...

Embodiment 2

[0014] Weighed 150 mg of quercetin and dissolved it in 5 mL of dimethyl sulfoxide, added 40.4 mg of succinic anhydride and reacted with stirring at 40 °C for 4 hours. 76.8 mg EDC and 9.2 mg NHS were weighed and added to the reaction solution, and the reaction was stirred at room temperature for 30 minutes. Weigh 0.2 g of chitosan and dissolve it in 5 mL of water, add chitosan aqueous solution dropwise to the reaction solution, adjust the pH of the reaction solution to 5.0 with HCl, stir and react at room temperature for 6 hours, and place in dimethyl sulfoxide solution Dialyze for 2 days, then fully dialyze in deionized water, and freeze-dry to obtain chitosan-succinate; weigh 20 mg trisodium 6-phosphogluconate and dissolve it in 2 mL water, add 22.4 mg EDC, and adjust the pH to 5.0, stirred and reacted at 40°C for 30 minutes, weighed 28 mg of chitosan-quercetin succinate and dissolved it in 4 mL of water, added the chitosan-quercetin succinate solution dropwise to the reactio...

Embodiment 3

[0016] Weighed 7.6 mg of quercetin and dissolved it in 7.6 mL of dimethyl sulfoxide, added 3 mg of succinic anhydride and stirred at 40 °C for 4 hours. 11.6 mg EDC and 7 mg NHS were weighed and added to the reaction solution, and the reaction was stirred at room temperature for 30 minutes. Weigh 0.1 g of chitosan and dissolve it in 5 mL of water, add chitosan aqueous solution dropwise to the reaction solution, adjust the pH of the reaction solution to 5.0 with HCl, stir and react at room temperature for 6 hours, and place in dimethyl sulfoxide solution Dialyze for 2 days, then fully dialyze in deionized water, and freeze-dry to obtain chitosan-succinate; weigh 2 mg trisodium 6-phosphogluconate and dissolve it in 2 mL water, add 11.2 mg EDC, and adjust the pH to 5.0, stirred and reacted at 40°C for 30 minutes, weighed 9.6 mg of chitosan-quercetin succinate and dissolved it in 4 mL of water, added the chitosan-quercetin succinate solution dropwise to the reaction solution, and k...

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Abstract

The invention discloses a preparation technology of nano-micelles for conveying anti-tumor medicines through oral administration, namely a preparation method of nano-micelles with mucous layer permeation and P-gp inhibition dual effects. Chitosan, quercetin and 6-phosphogluconic acid are used as raw materials to prepare an amphiphilic chitosan-quercetin succinate-6-phosphogluconic acid copolymer through a condensation and esterification method and a target product is synthesized through a self-assembling technology; the nano-micelles have a good mucous layer permeation capability and also has the P-gp inhibition effect; the oral administration conveying efficiency of the anti-tumor medicines can be effectively improved. The nano-micelles can be used for medical biological materials and medicine carriers and have good research and development application prospects.

Description

technical field [0001] The invention belongs to the field of pharmacy, and belongs to the preparation technology of nano micelles with dual functions of mucus layer penetration and P-gp inhibition. Background technique [0002] With the continuous deepening of the research and application of nanotechnology in the field of biomedicine, nanocarrier materials have shown unique efficacy in solving the difficulty of transporting hydrophobic drugs in vivo, destroying the activity of drug molecules in the gastrointestinal tract environment, and improving bioavailability. effects that cannot be achieved with other formulations. It is generally believed that the intestinal mucosal barrier is the main factor restricting the intestinal absorption efficiency of nano-preparations. Positively charged nano-preparations adhere to small intestinal epithelial cells through electrostatic interaction, and promote the phagocytosis and transport of nano-preparations by cells, but are easily trap...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K47/36A61K47/22A61K47/26A61P35/00
CPCA61K9/1075A61K47/22A61K47/26A61K47/36
Inventor 冯超穆愈之陈西广孔明程晓杰刘雅
Owner OCEAN UNIV OF CHINA
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