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Preparation method of nano-micelles with mucous layer permeation and P-gp inhibition dual effects

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

Active Publication Date: 2016-10-26
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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  • Preparation method of nano-micelles with mucous layer permeation and P-gp inhibition dual effects
  • Preparation method of nano-micelles with mucous layer permeation and P-gp inhibition dual effects
  • Preparation method of nano-micelles with mucous layer permeation and P-gp inhibition dual effects

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Experimental program
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Effect test

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. 38.4 mg EDC and 46 mg NHS were weighed and added to the reaction solution, the pH of the reaction solution was adjusted to 5.0 with HCl, 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, stir and react at room temperature for 6 hours, dialyze in dimethyl sulfoxide solution for 2 days, and then dissolve in deionized water Fully dialyzed and freeze-dried to obtain chitosan-succinate; weighed 6 mg trisodium 6-phosphogluconate and dissolved it in 1.5 mL water, added 3.4 mg EDC, adjusted the pH to 5.0 with HCl, and stirred at 40 °C for 30 Minutes, weigh 30 mg chitosan-quercetin succinate and dissolve in 3mL water, add the chitosan-quercetin succinate aqueous solution dropwise to the reaction solut...

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, the pH of the reaction solution was adjusted to 5.0 with HCl, 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, stir and react at room temperature for 6 hours, dialyze in dimethyl sulfoxide solution for 2 days, and then dissolve in deionized water Fully dialyzed and freeze-dried to obtain chitosan-succinate; weighed 20 mg trisodium 6-phosphogluconate and dissolved it in 2 mL water, added 22.4 mg EDC, adjusted the pH to 5.0 with HCl, and stirred at 40°C for 30 Minutes, weigh 28 mg chitosan-quercetin succinate and dissolve in 4 mL of water, add the chitosan-quercetin succinate aqueous solution dropwise to...

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, the pH of the reaction solution was adjusted to 5.0 with HCl, 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, stir and react at room temperature for 6 hours, dialyze in dimethyl sulfoxide solution for 2 days, and then dissolve in deionized water Fully dialyzed and freeze-dried to obtain chitosan-succinate; weighed 2 mg trisodium 6-phosphogluconate and dissolved it in 2 mL water, added 11.2 mg EDC, adjusted the pH to 5.0 with HCl, and stirred at 40°C for 30 Minutes, weigh 9.6 mg chitosan-quercetin succinate and dissolve in 4 mL of water, add the chitosan-quercetin succinate aqueous solution dropwise to the reaction sol...

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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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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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