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Norcantharidin oleanolic acid complex lipidosome and preparation method thereof

A technology of norcantharidin and oleanolic acid, applied in the preparation of norcantharidin oleanolic acid complex liposomes, can solve the problem of increasing peripheral leukocytes Quantity and other issues, to achieve the effect of enhancing liver targeting, treating liver cancer, and good encapsulation rate

Inactive Publication Date: 2014-12-17
CHONGQING MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

It is worth noting that norcantharidin can stimulate bone marrow and significantly increase the number of peripheral leukocytes, which makes norcantharidin important in combination chemotherapy, because many chemotherapy drugs currently used have side effects of bone marrow suppression

Method used

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  • Norcantharidin oleanolic acid complex lipidosome and preparation method thereof
  • Norcantharidin oleanolic acid complex lipidosome and preparation method thereof
  • Norcantharidin oleanolic acid complex lipidosome and preparation method thereof

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Effect test

Embodiment 1

[0033] Weigh the following components in parts by mass: 240g of lecithin, 41g of cholesterol, 14g of norcantharidin, 14g of oleanolic acid; dissolve in 30mL of dichloromethane, and place this solution in a 250mL round bottom flask; 35°C After the lipidoid film was formed by rotary evaporation in a water bath, 15 mL of PBS solution was added, hydrated for 2 hours, ultrasonicated for 20 minutes, and passed through a 0.45 μm microporous membrane to prepare norcantharidin oleanolic acid complex liposomes.

Embodiment 2

[0035] Take by weighing the following components respectively according to mass parts: lecithin 230g, cholesterol 45g, norcantharidin 12g, oleanolic acid 16g; Weigh dichloromethane, the volume mass ratio of dichloromethane and above-mentioned each component total amount ( ml / mg) was 9:100, the above-mentioned components were dissolved in dichloromethane; the above-mentioned solution was subjected to water-bath rotary evaporation at 30°C to form a lipid-like film; PBS solution, PBS solution and dichloromethane were weighed. The volume ratio is 3:5, adding PBS solution, water and reaction for 105min to the lipid film, ultrasonication for 30min, and passing through a 0.45μm microporous membrane to prepare norcantharidin oleanolic acid complex liposomes.

Embodiment 3

[0037] Take by weighing the following components respectively according to mass parts: lecithin 250g, cholesterol 35g, norcantharidin 16g, oleanolic acid 12g; Weigh dichloromethane, dichloromethane and the volume mass ratio of above-mentioned each component total amount ( ml / mg) was 10:100, the above components were dissolved in dichloromethane; the above solution was subjected to water bath rotary evaporation at 40°C to form a lipid-like film; PBS solution, PBS solution and dichloromethane were weighed The volume ratio is 2:5, adding PBS solution, water and reaction for 135min to the lipid film, ultrasonication for 15min, and passing through a 0.45μm microporous membrane to prepare norcantharidin oleanolic acid complex liposomes.

[0038] The beneficial effect of the present invention will be discussed in detail below in conjunction with the kinetics and tissue distribution of norcantharidin liposome intravenously injected into mice.

[0039] 1 Instruments and materials

[0...

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Abstract

The invention discloses a norcantharidin oleanolic acid complex lipidosome. The lipidosome is prepared from the following components in parts by weight: 230-250 parts of lecithin, 35-45 parts of cholesterol, 12-16 parts of norcantharidin and 12-16 parts of oleanolic acid, wherein the pH value of the lipidosome is 7.4. The invention further discloses a method for preparing the norcantharidin oleanolic acid complex lipidosome. The norcantharidin oleanolic acid complex lipidosome has relatively good encapsulation efficiency, has liver targeting property, and is capable of effectively treating liver cancer since the liver targeting property of norcantharidin is enhanced by oleanolic acid.

Description

technical field [0001] The invention belongs to the technical field of traditional Chinese medicine, and in particular relates to a norcantharidin oleanolic acid complex liposome, and also relates to a preparation method of a norcantharidin oleanolic acid complex liposome. Background technique [0002] Liver cancer is the third leading cause of cancer death in the world, and the number of patients with liver cancer ranks sixth in the number of cancer patients. It is estimated that 695,900 people died of cancer and 748,300 people suffered from cancer worldwide in 2008. What's more serious is that the incidence of most cancers in the world is still increasing, including Central Europe and the United States. In the past 20 years, the incidence of cancer in Europe has doubled. The situation is even more worrisome in Asian countries, where half of liver cancer cases and deaths occur in China. Norcantharidin is a demethylated analogue of cantharidin, which can inhibit the prolif...

Claims

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Application Information

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IPC IPC(8): A61K31/56A61K9/127A61P35/00A61K31/34
Inventor 尚京川马赟辜鹏程唐直婕王兰
Owner CHONGQING MEDICAL UNIVERSITY
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