Preparation of dual-hepatic-targeting long-circulation gypenoside liposome and preparation method of liposome

A long-circulation liposome and liver-targeting technology, which is applied in liposome delivery, medical preparations containing active ingredients, pharmaceutical formulations, etc., can solve the double liver-targeting long-circulation gypenoside liposome report that has not been seen and other issues, to achieve the effects of prolonging the circulation time in the body, enhancing stability, and enhancing targeting efficiency

Inactive Publication Date: 2015-03-25
YANCHENG TEACHERS UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] So far, there are no related reports on dual liver-targeted long-circulating gypenoside liposomes

Method used

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  • Preparation of dual-hepatic-targeting long-circulation gypenoside liposome and preparation method of liposome
  • Preparation of dual-hepatic-targeting long-circulation gypenoside liposome and preparation method of liposome
  • Preparation of dual-hepatic-targeting long-circulation gypenoside liposome and preparation method of liposome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] (1) (4.15g, 0.01mol) β-sitosterol, (0.80g, 0.008mol) succinic anhydride, (0.98g, 0.008mol) 4-dimethylaminopyridine are mixed in 100ml dichloromethane, in 45 ° C reaction, stirring for 48h. The dichloromethane solution was washed with 1mol / L (3×100mL) hydrochloric acid solution, Na 2 SO 4 Dry, filter and spin dry. Obtain the white solid compound shown in formula IV;

[0056] (2) (5.14g, 0.01mol) compound of formula IV, (16g, 0.008mol) double-ended amino polyethylene glycol 2000, (0.98g, 0.008mol) 4-dimethylaminopyridine, (1.53g, 0.008mol) ) 1-ethyl-(3-dimethylaminopropyl) carbodiimide hydrochloride was mixed in dichloromethane, reacted at 45°C, and stirred for 48h. The dichloromethane solution was washed with 1mol / L (3×100mL) hydrochloric acid solution, Na 2 SO 4 Dry, filter and spin dry. The crude product was subjected to flash column chromatography on silica gel (300-400 mesh), eluting with dichloromethane-methanol (100:1), and the collected solution was concent...

Embodiment 2

[0060] (1) Mix (4.15g, 0.01mol) β-sitosterol, (1.0g, 0.0125mol) succinic anhydride, (2.44g, 2mol) 4-dimethylaminopyridine in 100ml dichloromethane, at 45°C The reaction was stirred for 48h. The dichloromethane solution was washed with 1mol / L (3×100mL) hydrochloric acid solution, Na 2 SO 4 Dry, filter and spin dry. Obtain the white solid compound shown in formula IV;

[0061] (2) (5.14g, 0.01mol) compound of formula IV, (60g, 0.03mol) double-ended amino polyethylene glycol 2000, (3.67g, 0.03mol) 4-dimethylaminopyridine, (5.75g, 0.03mol) ) 1-ethyl-(3-dimethylaminopropyl) carbodiimide hydrochloride was mixed in dichloromethane, reacted at 45°C, and stirred for 48h. The dichloromethane solution was washed with 1mol / L (3×100mL) hydrochloric acid solution, Na 2 SO 4 Dry, filter and spin dry. The crude product was subjected to flash column chromatography on silica gel (300-400 mesh), eluting with dichloromethane-methanol (100:1), and the collected solution was concentrated und...

Embodiment 3

[0065] (1) (4.15g, 0.01mol) β-sitosterol, (5.0g, 0.05mol) succinic anhydride, (3.05g, 0.025mol) 4-dimethylaminopyridine are mixed in 100ml dichloromethane, at 45 ° C reaction, stirring for 48h. The dichloromethane solution was washed with 1mol / L (3×100mL) hydrochloric acid solution, Na 2 SO 4 Dry, filter and spin dry. Obtain the white solid compound shown in formula IV;

[0066] (2) (5.14g, 0.01mol) compound of formula IV, (30g, 0.015mol) double-ended amino polyethylene glycol 2000, (1.83g, 0.015mol) 4-dimethylaminopyridine, (2.88g, 0.015mol) ) 1-ethyl-(3-dimethylaminopropyl) carbodiimide hydrochloride was mixed in dichloromethane, reacted at 45°C, and stirred for 48h. The dichloromethane solution was washed with 1mol / L (3×100mL) hydrochloric acid solution, Na 2 SO 4 Dry, filter and spin dry. The crude product was subjected to flash column chromatography on silica gel (300-400 mesh), eluting with dichloromethane-methanol (100:1), and the collected solution was concentra...

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PUM

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Abstract

The invention discloses a method for preparing a dual-hepatic-targeting long-circulation gypenoside liposome by modifying beta-sitosterol by virtue of galacturonic acid, glycyrrhetinic acid and polyethylene glycol. Compared with a normal gynostemma liposome, the targeting efficiency to parenchymal hepatic cells and long-circulation effect of the gypenoside liposome are greatly improved. The novel long-circulation liposome is good in hepatic targeting property, and can also obviously prolong the retention time of the gypenoside in a body, so that the gypenoside can actively target to hepatic tumor cells, and an effect of treating tumors is enhanced.

Description

technical field [0001] The present invention relates to the field of pharmaceutical preparations, in particular to a method for producing double liver targeting long circulation gypenoside liposomes, more specifically, the present invention relates to double liver targeting long circulation gypenoside liposomes and containing double liver targeting Pharmaceutical formulations towards long-circulating gypenoside liposomes. Background technique [0002] The liver is composed of parenchymal cells and non-parenchymal cells (endothelial cells, Kupffer cells). Liver cancer and hepatitis all occur in hepatic parenchymal cells. The asialoglycoprotein receptor (ASGPR) exists in large numbers on the surface of the liver parenchymal cell membrane of mammals. The receptor can specifically recognize liposomes with galactose as the end group, so the As a carrier, the drug can be directed to the liver parenchymal cells. However, ASGPR receptor binding alone is not sufficient. Studies ha...

Claims

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Application Information

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IPC IPC(8): A61K47/34A61K9/127A61K36/424A61K31/704A61P1/16A61P35/00A61P9/00C08G65/48
Inventor 喻樊
Owner YANCHENG TEACHERS UNIV
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