Icariin bone-targeting nano-liposome, and preparation method and application thereof

A nano-liposome and icariin technology, which is applied in liposome delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc., can solve the problem of poor absorption of icariin, unsuitable for long-term administration, etc. problems, to achieve the effect of improving solubility and absorption problems, controlled release, and good targeting

Active Publication Date: 2018-03-16
GUANGDONG MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The purpose of the present invention is to overcome the defects of poor icariin absorption, rapid elimination, unsuitability for long-term administration and no targeting in the prior art, and provide a bone-targeted nanoliposome of icariin

Method used

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  • Icariin bone-targeting nano-liposome, and preparation method and application thereof
  • Icariin bone-targeting nano-liposome, and preparation method and application thereof
  • Icariin bone-targeting nano-liposome, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Example 1 Icariin bone-targeted nanoliposome I

[0042] The icariin bone-targeting nanoliposome provided in this embodiment has passive bone targeting function, including icariin, soybean lecithin, cholesterol and sodium cholate, icariin, soybean lecithin, cholesterol and The mass ratio of sodium cholate is 7.5:100:20:20, and the particle size of the nanoliposome is less than 80nm, which is prepared by the following method:

[0043] Weigh 400 mg of soybean lecithin and 80 mg of cholesterol and dissolve them in an appropriate amount of absolute ethanol, and weigh 30 mg of icariin and dissolve them in absolute methanol. Mix the above components in a 250 ml eggplant-shaped bottle, evaporate under reduced pressure at 60 r / min in a water bath at 45°C to form a uniform film, add 20 ml of PBS solution (phosphate buffer) containing 80 mg sodium cholate to hydrate, and probe The ultrasonic instrument controls the temperature not to exceed 50°C, intermittent ultrasonication for ...

Embodiment 2

[0044] Example 2 Icariin bone-targeted nanoliposome II

[0045] The icariin bone-targeting nanoliposome provided in this example has passive bone targeting function, including icariin, dipalmitoylphosphatidylethanolamine, cholesterol and sodium deoxycholate, icariin, di The mass ratio of palmitoylphosphatidylethanolamine, cholesterol and sodium deoxycholate is 10:100:25:20, and the particle diameter of nanoliposomes is less than 80nm, which is prepared by the following method:

[0046] Weigh 500 mg of dipalmitoylphosphatidylethanolamine and 125 mg of cholesterol and dissolve them in an appropriate amount of absolute ethanol, and weigh 50 mg of icariin and dissolve them in absolute methanol. Mix the above components in a 250 ml eggplant-shaped bottle, evaporate under reduced pressure at 60 r / min in a 45°C water bath to form a uniform film, add 50 ml of PBS solution (phosphate buffer) containing 100 mg sodium cholate to hydrate, and probe Control the temperature of the ultrason...

Embodiment 3

[0047] Example 3 Icariin bone-targeted nanoliposomes with long circulation properties

[0048] The icariin bone-targeted nanoliposomes provided in this example have long-circulation and passive bone-targeting functions, including icariin, double-saturated lecithin, cholesterol, sodium deoxycholate and liposome surface modification The polyethylene glycol derivative (MPEG2000-DSPE), the mass ratio of icariin, double saturated lecithin, cholesterol, sodium deoxycholate and MPEG2000-DSPE is 8:100:24:10:20, nano lipid The particle size of the plastid is less than 80nm, and it is prepared by the following method:

[0049] Weigh 500 mg of double-saturated lecithin and 120 mg of cholesterol and dissolve them in an appropriate amount of absolute ethanol, weigh 40 mg of icariin and 100 mg of MPEG2000-DSPE and dissolve them in absolute methanol respectively. Mix the above components in a 500 ml eggplant-shaped bottle, evaporate under reduced pressure at 60 r / min in a water bath at 45°C...

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Abstract

The invention relates to an icariin bone-targeting nano-liposome, and a preparation method and an application thereof. The nano-liposome comprises icariin, phosphatidylcholine, cholesterol and a solubilizer according to a mass ratio of (6-20):(100-120):(20-30):(10-80), and the particle size of the nano-liposome is less than 80 nm. The icariin is processed to form the nano-liposome dosage form, andthe particle size is controlled to be less than 80 nm in order to make the nano-liposome have good bone tissue passive targeting ability. The modification effect of bone target makes the nano-liposome have active targeting ability; and the modification effect of a polyethylene glycol derivative makes the nano-liposome have a long-cycle characteristic. The nano-liposome has good targeting ability,can load the icariin to improve the solubility and the absorption problem of the icariin, also can control the in vivo process of the icariin, and has sustained release and controlled release effects.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and more specifically relates to a bone-targeting nanoliposome of icariin and its preparation method and application. Background technique [0002] It has become a hot spot to research and develop new drugs for preventing and treating osteoporosis with high efficiency, low toxicity and no side effects from traditional Chinese medicine. Epimedium is extremely rich in medicinal resources in my country, and Icariin (ICA), as its representative flavonoid component, has high medicinal value. However, due to the poor water solubility and low bioavailability of icariin, its further clinical application is limited. [0003] The water solubility of icariin is poor, the equilibrium solubility in water at 25 ℃ is 15.04 mg / L, and the apparent oil-water partition coefficient is 77.31 [Chinese Journal of Traditional Chinese Medicine. 2008, 23(9):777-779]. Pharmacokinetic studies in rats h...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/7048A61K47/10A61K47/54A61P35/00
CPCA61K9/1271A61K31/7048
Inventor 张大威郑明彬林坚涛王冠海李莉
Owner GUANGDONG MEDICAL UNIV
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