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Herba Epimedii aglycone liposome and preparation method thereof

A technology of icariin and icariin lipid, which is applied in the directions of liposome delivery, pharmaceutical formulations, medical preparations with inactive ingredients, etc. The problems such as oral absorption and drug effect exertion, to achieve the effect of low cost, simple and easy preparation method, and good biocompatibility

Inactive Publication Date: 2009-07-22
贾晓斌
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, its water solubility is very poor, which affects its oral absorption and efficacy.
There is no clinical preparation of icarigenin

Method used

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  • Herba Epimedii aglycone liposome and preparation method thereof
  • Herba Epimedii aglycone liposome and preparation method thereof
  • Herba Epimedii aglycone liposome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Weigh 20 mg of icariin, 200 mg of soybean lecithin, and 100 mg of cholesterol, dissolve them in 20 mL of dichloromethane, transfer the dichloromethane solution to a syringe, and slowly inject the dichloromethane solution into 25 mL of 0.5% P-188 (provided by Nanjing Weier Chemical Industry Co., Ltd.) aqueous solution, continue to hydrate for 0.5 hour after the addition, to obtain a liposome suspension. Add 20% mannitol of the volume of the suspension to the liposome suspension, freeze-dry to obtain the icarigenin liposome, see its particle size distribution and Zeta potential figure 1 , figure 2 . The transmission electron microscope images before and after freeze-drying are shown in image 3 , Figure 4 .

Embodiment 2

[0044] Weigh 20 mg of icariin, 200 mg of soybean lecithin, and 100 mg of cholesterol, dissolve them in 10 mL of dichloromethane, transfer the dichloromethane solution to a syringe, and slowly inject the dichloromethane solution into 25 mL of 0.5% P-188 (provided by Nanjing Weier Chemical Industry Co., Ltd.) aqueous solution, continue to hydrate for 0.5 hour after the addition, to obtain a liposome suspension. Add 15% mannitol of the suspension volume to the liposome suspension, and freeze-dry to obtain icarigenin liposomes. The particle size distribution and Zeta potential are shown in Figure 5 , Image 6 .

Embodiment 3

[0046] Weigh 20 mg of icariin, 600 mg of soybean lecithin, and 100 mg of cholesterol, dissolve them in 10 mL of dichloromethane, transfer the dichloromethane solution to a syringe, and slowly inject the dichloromethane solution into 25 mL of 0.5% P-188 (provided by Nanjing Weier Chemical Industry Co., Ltd.) aqueous solution, continue to hydrate for 0.5 hour after the addition, to obtain a liposome suspension. Add 10% mannitol of the suspension volume to the liposome suspension, and freeze-dry to obtain icarigenin liposomes. The particle size distribution and Zeta potential are shown in Figure 7 , Figure 8 .

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Abstract

The invention provides an epimedium aglycone liposome. The liposome consists of the following components in percentage by weight: 50 to 85 percent of soya bean lecithin, 10 to 35 percent of cholesterin and 2 to 25 percent of epimedium aglycone; the surface of the liposome is a phospholipid bimolecular layer, and hydrophilic groups on the outer part of the bimolecular layer form a hydrophilic cap; hydrophilic groups on the inner part of the bimolecular layer form an inner water phase, and hydrophobic groups between the bimolecular layer form a hydrophobic region; and the epimedium aglycone is coated between the phospholipid double layer of the liposome, and the absolute value of the Zeta electric potential is more than 40mV after the liposome is hydrated. The epimedium aglycone liposome has the characteristics that: 1, the preparation method is simply and easily implemented, the raw material, namely the soya bean lecithin has good bio-compatibility, and can be biodegradable, and the raw material is also wide in source and low in cost; 2, by utilizing the nanometer technology, the traditional Chinese medicine active ingredient, namely epimedium aglycone is coated between the phospholipid double layer of the liposome, so that the water solubility is improved; and 3, the epimedium aglycone liposome has better physical stability, and after being stood for quite a long time, the epimedium aglycone liposome has no delamination and flocculation. The invention also discloses a method for preparing the epimedium aglycone liposome.

Description

Technical field: [0001] The invention relates to icariin, liposome and nanometer technology. Background technique: [0002] Osteoporosis is a worldwide disease. With the aging society, osteoporosis has been listed as one of the three major senile diseases. Icariin is a flavonoid monomer component extracted from Epimedium Herba, a commonly used medicine in clinical medicine. Many studies at home and abroad have shown that icaritin has obvious anti-osteoporosis pharmacological activity [see: JianHuang, Lan Yuan, Xi Wang, et al. Icaritin and its glycosides enhance osteoclastic, but suppress osteoclastic, differentiation and activity in vitro[ J]. Life Sciences, 2007, 81:832-840.]. However, its water solubility is very poor, which affects its oral absorption and efficacy. There is no clinical preparation of icarigenin yet. Invention content: [0003] The technical problem to be solved by the present invention is to provide a liposome with simple preparation process, high d...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/352A61K47/28A61P19/10
Inventor 贾晓斌兰雪莲孙娥陈彦
Owner 贾晓斌
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