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Application of using amphiphilic N-long-chain alkyl-N-arginine chitosan as solubilizing and absorption prompting carrier of gambogic acid

A technology of arginine chitosan and long-chain alkyl, which can be applied to medical preparations containing active ingredients, organic active ingredients, and pharmaceutical formulas, and can solve problems such as the unclear mechanism of arginine penetration enhancement

Inactive Publication Date: 2013-06-12
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The guanidine group of arginine and the phospholipid of the lipid bilayer can form hydrogen bonds. The formation of hydrogen bonds and the strong basicity (pKa~12.5) of the guanidine group play a very important role in the control of cell membrane transport, but arginine The detailed permeation mechanism of acid is still unclear (Umezawa N, Gelman M A, Haigis M C, et al.Translocation of a beta-peptide across cell membranes.J Am Chem Soc, 2002,124(3):368-369; Zhu Dun Wan, Zhang Hailing, Bai Jingen, et al. Study on Arginine Modified Chitosan to Improve Gene Transfection Efficiency. Science Bulletin, 2007, 52: 2199-2205)

Method used

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  • Application of using amphiphilic N-long-chain alkyl-N-arginine chitosan as solubilizing and absorption prompting carrier of gambogic acid
  • Application of using amphiphilic N-long-chain alkyl-N-arginine chitosan as solubilizing and absorption prompting carrier of gambogic acid
  • Application of using amphiphilic N-long-chain alkyl-N-arginine chitosan as solubilizing and absorption prompting carrier of gambogic acid

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Example 1: Direct dissolution method:

[0054] (1) Weigh 1 gram of OACS, add 50 ml of water, and stir in a water bath at 50°C for 30 minutes to prepare a carrier solution;

[0055] (2) Add 1 gram of gambogic acid to the carrier solution, sonicate the probe under ice bath for 30 minutes, dialyzed with distilled water, and filter to obtain the drug-loaded micelle solution.

Embodiment 2

[0056] Example 2: Solvent emulsification and volatilization method: Weigh 1 gram of OACS, add 50 ml of water, stir in a water bath at 50°C for 30 minutes, weigh 1 gram of gambogic acid, and dissolve it in a dichloromethane solution to make 10g / L of gambogic acid The dichloromethane solution was added dropwise to the carrier solution, the probe was sonicated for 10 minutes in an ice bath, the dichloromethane was evaporated and the dichloromethane was evaporated overnight, and the drug-loaded micelle solution was obtained by filtering with a 0.45μm filter membrane.

Embodiment 3

[0057] Example 3: Dialysis method: Weigh 1 gram of OACS, add 50ml of water, stir for 30min in a water bath at 50°C, weigh 1 gram of GA and dissolve it in an appropriate amount of ethanol to make the concentration 10g / L, and add the ethanol solution of GA to the carrier dropwise In the solution, the probe was sonicated for 10 minutes in an ice bath, redistilled water was dialyzed overnight, and filtered with a 0.45 μm filter membrane to obtain the drug-loaded micelle solution.

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Abstract

The invention discloses a natural and biodegradable N-long-chain alkyl-N-arginine chitosan derivative as well as a micellar preparation method thereof and application of using the natural and biodegradable N-long-chain alkyl-N-arginine chitosan derivative as a solubilizing and absorption prompting nanometer carrier of gambogic acid which is difficult to dissolve by being taken orally and difficult to absorb.

Description

Technical field [0001] The present invention relates to the use of amphiphilic N-long-chain alkyl-N-arginine chitosan derivatives (OACS) as a solubilization and absorption-promoting nano carrier for the poorly soluble drug gambogic acid (GA) to prepare a highly soluble nano-carrier , GA-OACS nano-medicine that absorbs well. Background technique [0002] Chitosan is the only basic polysaccharide in nature. It is a cationic polymer with bioadhesive properties, which can extend the residence time of drugs on the surface of biological mucosa. The positively charged groups of chitosan can also be attached to the surface. The negatively charged cell membrane interacts to enhance the permeability of the membrane, thereby enhancing the absorption of the drug by the mucosa. The penetration enhancement effect of chitosan is likely to be due to its significant impact on membrane proteins. The positive charge interacts with the open structure of the tight junctions between cells, which make...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K47/36A61K31/352A61P35/00
Inventor 吕慧侠喻樊周建平
Owner CHINA PHARM UNIV
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