Preparation method of oxymatrine active targeting lipidosome

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...

AI Technical Summary

Problems solved by technology

In order to overcome the disadvantages of unsatisfactory target distribution and poor stability of liposomes as carriers, some new liposomes have been developed in recent years, such as temperature-sensitive, PL-sensitive, immune, and polymeric membrane liposomes.

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