Preparation method of oxymatrine active targeting lipidosome

An oxymatrine and active targeting technology, applied in the field of medicine, can solve the problems of poor stability and unsatisfactory targeting distribution.

Inactive Publication Date: 2014-06-25
CHONGQING MEDICAL UNIVERSITY
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Problems solved by technology

In order to overcome the disadvantages of unsatisfactory target distribution and poor stability of liposomes as carriers, some new l

Method used

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  • Preparation method of oxymatrine active targeting lipidosome
  • Preparation method of oxymatrine active targeting lipidosome

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Experimental program
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Embodiment 1

[0023] 1.1 Synthesis and purification of glycolipids

[0024] Dissolve 50mg of phosphatidylethanolamine in 4ml of 2:1 chloroform-methanol, then add 13ml, 0.2mol / l, pH9.0 sodium bicarbonate buffer solution, remove the organic solvent with a rotary evaporator at 40°C, and add lactose 500mg and sodium borohydride 250mg were thoroughly mixed, and incubated in a 25°C incubator for 400h. The reaction solution was put into a dialysis bag, and dialyzed at room temperature for 3 days under magnetic stirring. It was purified by a silicic acid column, and the eluent was a gradient ratio of chloroform-methanol (9:1, 7:3, 5:5, 3:7) and finally eluted with methanol. Collect the eluate obtained in 3:7, which is the glycolipid solution, and freeze-dry to obtain a white powder, which is stored in a low-temperature refrigerator for later use. 1.2 Preparation of oxymatrine active targeting liposomes by pH gradient method

[0025] Cholesterol and phospholipids were added with 10% mol glycolipi...

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Abstract

The invention belongs to the technical field of medicines, and discloses a preparation method of an oxymatrine active targeting lipidosome. The active targeting oxymatrine lipidosome is prepared by a pH gradient method. The optimal prescription for preparing the oxymatrine active targeting lipidosome is as follows: the ratio of medicine to lipidosome is 1:10, the ratio of phospholipid to cholesterol is 3:1 with additionally 10% mol of Lac-PE, the pH value of the outer aqueous phase is 6.8, the incubation temperature is 60 DEG C, and the average encapsulation efficiency is 55.48% under the optimal prescription. The oxymatrine active targeting lipidosome prepared by the method provided by the invention is relatively stable. In vitro drug release experiments of the active targeting lipidosome show that oxymatrine wrapped by the glycosylated lipidosome has a slow release effect. Through observation by a transmission electron microscope, the oxymatrine active targeting lipidosome prepared by the method provided by the invention is a single chamber lipidosome with the average grain size of 80nm, and meets the demand of lipidosome. In vitro dissolution experiments show that the oxymatrine active targeting lipidosome wrapped has a certain slow release feature.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a preparation method of oxymatrine actively targeting liposomes. Background technique [0002] Oxymatrine (Oxymatrine.OM.Fig.1) is a quinolizidine alkaloid extracted from the traditional Chinese medicine Sophora flavescens or Sophora flavescens root, colorless dice-like crystals (acetone). The melting point is 208°C, and it is also reported that the melting point is 207-208°C (decomposition). Optical rotation +47.7° (ethanol). It is easily soluble in water and has strong water absorption. The aqueous solution is strongly alkaline, but it is difficult to dissolve in ether. The melting point of oxymatrine containing 1 molecule of crystal water is 77-78°C. Oxymatrine exists in the roots of leguminous plants Sophora flavescensAit. and the root of S.subprostratachunetT.Chen. Pharmacological studies have shown that oxymatrine has significant anti-cancer activity; it has anti-arrhy...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/4375
Inventor 尚京川张梦胡茂华王兰马赟
Owner CHONGQING MEDICAL UNIVERSITY
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