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Nanostructured lipid carrier modified by glycolipid polymer as well as preparation method and application of nanostructured lipid carrier

A technology of nanostructured lipids and polymers, applied in liposome delivery, drug combination, diseases, etc., can solve problems, have effective distribution and other problems

Inactive Publication Date: 2017-09-01
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Nanostructured lipid carriers enable effective encapsulation of A-317491, but P2X targeting endometriosis 3 Effective distribution of highly expressed sites

Method used

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  • Nanostructured lipid carrier modified by glycolipid polymer as well as preparation method and application of nanostructured lipid carrier
  • Nanostructured lipid carrier modified by glycolipid polymer as well as preparation method and application of nanostructured lipid carrier
  • Nanostructured lipid carrier modified by glycolipid polymer as well as preparation method and application of nanostructured lipid carrier

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] (1) Synthesis of chitosan-stearic acid graft

[0020] Take 0.13g of stearic acid and 0.54g of carbodiimide (EDC), accurately weighed, dissolve in 10mL of absolute ethanol, and activate at 60°C for 50min. Another 0.3 g of the above-mentioned chitosan was taken, weighed accurately, dissolved in 20 mL of deionized water, and heated to 60° C. Slowly add the above ethanol solution dropwise to the chitosan aqueous solution, and react with magnetic stirring at 60° C. for 12 hours. The final reaction solution was placed in a dialysis bag and dialyzed against deionized water for 48 hours. The dialysate was freeze-dried, and the freeze-dried powder was dispersed in 20 mL of absolute ethanol, ultrasonicated in a water bath, heated, and filtered through a 0.45 μm microporous membrane while hot to remove unreacted stearic acid, and repeated three times. The filter cake is redissolved in water, freeze-dried to obtain chitosan-stearic acid graft.

[0021] (2) Preparation of nanostr...

Embodiment 2

[0027] (1) Preparation of nanostructured lipid carrier

[0028] Take 24mg of glyceryl monostearate and 6mg of oleic acid, accurately weighed, dissolve in 3.0mL of absolute ethanol, and dissolve in a 50°C water bath. Take 30mg of poloxamer 188, accurately weighed, put in 30mL of deionized water, and heat to 50°C. Under the condition of 400rpm magnetic stirring, the ethanol solution in which the lipid is dissolved is injected into the aqueous solution, and stirred for 5 minutes to obtain a nanostructured lipid carrier dispersion.

[0029] (2) Preparation of Glycolipid Polymer Modified Nanostructured Lipid Carrier

[0030] Take 25mg chitosan-stearic acid graft, add 5mL deionized water to dissolve, obtain 5mg / mL micellar solution, add 5mL concentration to be 2.5mg / mL nano-structured lipid carrier dispersion liquid, shake slowly at room temperature for 10min, The nanostructured lipid carrier modified by glycolipid polymer was obtained.

[0031] The measured potential of the glyc...

Embodiment 3

[0033] (1) Preparation of nanostructured lipid carrier

[0034] Take 24mg of glyceryl monostearate and 6mg of oleic acid, accurately weighed, dissolve in 3.0mL of absolute ethanol, and dissolve in a 50°C water bath. Take 30mg of poloxamer 188, accurately weighed, put in 30mL of deionized water, and heat to 50°C. Under the condition of 400rpm magnetic stirring, the ethanol solution in which the lipid is dissolved is injected into the aqueous solution, and stirred for 5 minutes to obtain a nanostructured lipid carrier dispersion.

[0035] (2) Preparation of Glycolipid Polymer Modified Nanostructured Lipid Carrier

[0036] Take 25mg chitosan-stearic acid graft, add 5mL deionized water to dissolve, obtain 5mg / mL micellar solution, add 2mL concentration to be 2.5mg / mL nano-structured lipid carrier dispersion liquid, shake slowly at room temperature for 10min, The nanostructured lipid carrier modified by glycolipid polymer was obtained.

[0037] The measured potential of the glyc...

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Abstract

The invention provides a nanostructured lipid carrier modified by a glycolipid polymer. The carrier is prepared from the following components: 50.0 to 90.9 percent by weight of chitosan-stearic acid graft, 7.27 to 40.0 percent by weight of glyceryl monostearate, 1.82 to 10.0 percent by weight of oleic acid and 0 to 3.23 percent by weight of hydrophobic drug A-317491. The preparation method of the carrier comprises the following steps: by using a solvent diffusion method, selecting 0.1 percent of poloxamer as a surfactant to prepare a nanostructured lipid carrier encapsulated with the A-317491; dissolving the chitosan-stearic acid graft into water and then adding a nanostructured lipid carrier solution encapsulated with the A-317491, and slowly oscillating a mixed solution at normal temperature for 10 minutes, thus obtaining the nanostructured lipid carrier modified by the glycolipid polymer. The nanostructured lipid carrier modified by the glycolipid polymer has the advantages that the hydrophobic drug A-317491 can be effectively encapsulated, the drug concentration in ectopic endometrium tissues is improved and the effect of the A-317491 resisting endometriosis pain is enhanced.

Description

technical field [0001] The invention belongs to the preparation and application of a polymer-modified nano-structure lipid carrier, in particular to a glycolipid polymer-modified nano-structure lipid carrier and a preparation method for encapsulating hydrophobic drug A-317491. Background technique [0002] Pain is the main clinical symptom of endometriosis, which is mainly treated with hormones and surgery. Hormone therapy has large side effects, uncertain curative effect, and surgical treatment is prone to recurrence. Therefore, exploring new methods of drug treatment is an important direction for the development of new treatments for endometriosis. ATP and its P2X 3 The receptor may play an important role in endometriosis pain sensitization and information transmission, [0003] A-317491 is P2X 3 Selective receptor antagonist that inhibits ATP-activated P2X 3 receptor-induced Ca 2+ Influx, inhibition of action potential generation, inhibition of pain. A-317491 (5-[(3...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/36A61K47/14A61K47/12A61K31/194A61K9/127A61P15/00A61P29/00
CPCA61K47/36A61K9/1271A61K31/194A61K47/12A61K47/14
Inventor 胡富强孟廷廷袁弘袁铭
Owner ZHEJIANG UNIV