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Preparation method of medicine-carrying ethosome modified by galactosed polyethyleneimine

A technology of polyethylenimine and galactose, which is applied in the direction of pharmaceutical formulations, liposome delivery, medical preparations of non-active ingredients, etc., can solve the problems of limited application of cytotoxicity, and achieve simple experimental equipment, convenient operation, and improved The effect of treatment

Inactive Publication Date: 2017-09-22
DONGHUA UNIV
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Problems solved by technology

However, its high cytotoxicity limits its application in gene therapy

Method used

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  • Preparation method of medicine-carrying ethosome modified by galactosed polyethyleneimine
  • Preparation method of medicine-carrying ethosome modified by galactosed polyethyleneimine
  • Preparation method of medicine-carrying ethosome modified by galactosed polyethyleneimine

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Embodiment

[0030] A preparation method of drug-loaded ethosomes modified by galactosylated polyethyleneimine:

[0031] Lecithin, cholesterol and octadecylamine were mixed and dissolved in ethanol at a mass ratio of 25:2.5:1, and rotary evaporation was used to obtain a layer of liposome film, and rhodamine B (model drug) was added at 0.5mg / ml 30% (v / v) aqueous ethanol solution, stirred to obtain the ethosome loaded with rhodamine B;

[0032] 2.0g of lactobionic acid (LA) was dissolved in 50mL of TEMED / HCl buffer (PH4.7), and activated by a mixture of NHS (0.14g) and EDC (0.6g). Finally, 1.0 g of polyethyleneimine (PEI) was added to the solution in an equivalent molar ratio of LA. After reacting at room temperature for 72 hours, the product was placed in a 1.4kD dialysis bag and dialyzed for 2-3 days to obtain galactosylated polyethyleneimine (Gal-PEI) after freeze-drying.

[0033] Galactosylated polyethyleneimine was dissolved in deionized water at a concentration of 10 mg / mL, and 9 mL ...

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Abstract

The invention discloses a preparation method of a medicine-carrying ethosome modified by galactosed polyethyleneimine. The method is characterized by mixing lecithin, cholesterol and octadecylamine, then dissolving the mixture in alcohol, carrying out rotary evaporation to obtain a liposome membrane, and then adding the liposome membrane into a medicine-containing solution to obtain medicine-carrying ethosome; dropwise adding the medicine-carrying ethosome into a galactosed polyethyleneimine solution by using a layer-by-layer self-assembly technique, simultaneously stirring and carrying out ultrasonic dispersion, then adding nucleic acid medicines to obtain the medicine-carrying ethosome modified by galactosed polyethyleneimine. Through the preparation method of the medicine-carrying ethosome modified by galactosed polyethyleneimine, galactosed polyethyleneimine and nucleic acid medicines are successively assembled outside the medicine-carrying ethosome through electrostatic adsorption by mainly using an ethosome preparation technique and the layer-by-layer self-assembly technique; a plurality of medicines (including gene medicines) are effectively loaded and delivered; and the therapy targeted to liver tumor cells of the medicines can be improved.

Description

technical field [0001] The invention relates to a method for preparing drug-loaded ethosomes modified by galactosylated polyethyleneimine, and belongs to the technical field of preparation technology of drug-loaded ethosomes. Background technique [0002] Liver cancer is the third leading cause of death among all tumors. Globally, more than 35% of liver cancer cases occur in my country. Therefore, finding an effective treatment is urgently needed. The galactose ligand can bind to the asialoglycoprotein receptor specifically expressed by liver cancer cells, actively target liver cancer, and increase the uptake of tumor cells at the same time. [0003] Polyethyleneimine (PEI) is one of the non-viral gene carriers. Because of its good gene binding ability and transfection ability, it has been widely used in cell delivery and transfection of nucleic acid drugs. It has long been considered the gold standard in gene transfection reagents. But its high cytotoxicity limits its ...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K45/06A61K48/00A61K47/34A61K31/7088A61P35/00
CPCA61K9/1271A61K31/7088A61K45/06A61K47/34
Inventor 王红声马琳琳杨兴兴张东东余凡潘潇涵骆格杰
Owner DONGHUA UNIV
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