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Silybin nanostructured lipid carrier and preparation method thereof

A technology of lipid carrier and silibinin, which is applied in the directions of liposome delivery, pharmaceutical formulations, and medical preparations containing active ingredients, can solve problems such as not being easy, and achieves low cost, good stability, and improved The effect of the ability to hold the drug

Inactive Publication Date: 2010-01-27
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although it is a conventional technical means to make a drug into a nano-lipid carrier, it is not easy to develop a formula and a preparation method with the advantages of good effect, good biocompatibility, stability, and controllable drug release. creative labor required

Method used

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  • Silybin nanostructured lipid carrier and preparation method thereof
  • Silybin nanostructured lipid carrier and preparation method thereof
  • Silybin nanostructured lipid carrier and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Example 1 Preparation of silibinin nano lipid carrier:

[0031] Take 15mg of silibinin, 200mg of stearic acid, 100mg of oleic acid, 120mg of lecithin and 5ml of absolute ethanol in a 10ml test tube, and heat it on a constant temperature water bath at 70°C to fully dissolve it to form an organic phase; take another 20ml of distilled water, The water bath is heated to the same temperature as the organic phase to form the aqueous phase. Slowly inject the organic phase into the water phase with a No. 5 needle under stirring at 800r / min, and stir at a constant temperature of (70±2)°C to volatilize the organic solvent. After 6 hours, quickly disperse the obtained translucent emulsion in 15ml of 0-2°C water phase, and stirred for 2 h under an ice bath to obtain the silibinin nano-lipid carrier.

Embodiment 2

[0032] Example 2 Preparation of silibinin nano lipid carrier:

[0033] Take 25mg of silibinin, 400mg of glyceryl monostearate, 200mg of medium-chain fatty acid glycerides, 200mg of lecithin and 5ml of acetone in a 10ml test tube, and heat it on a constant temperature water bath at 75°C to fully dissolve it to form an organic phase; Take 20ml of distilled water and heat it in a water bath to the same temperature as the organic phase to form the water phase. Slowly inject the organic phase into the water phase with a No. 5 needle under stirring at 800r / min, and stir at a constant temperature of (75±2)°C to volatilize the organic solvent. After 6 hours, quickly disperse the obtained translucent emulsion in 15ml of 0-2°C water phase, and stirred for 2 h under ice bath to obtain silibinin nano-lipid carrier.

Embodiment 3

[0034] Example 3 Preparation of silibinin nano lipid carrier:

[0035]Take 20mg of silibinin, 250mg of stearic acid, 50mg of oleic acid, 160mg of Span80 and 5ml of ethyl acetate in a 10ml test tube, and heat it on a constant temperature water bath at 75°C to fully dissolve to form an organic phase; Heating to the same temperature as the organic phase constitutes the aqueous phase. Slowly inject the organic phase into the water phase with a No. 5 needle under stirring at 900r / min, and stir at a constant temperature of (75±2)°C to volatilize the organic solvent. After 4 hours, quickly disperse the obtained translucent emulsion in 15ml of 0-2°C water phase, and stirred for 2 h under ice bath to obtain silibinin nano-lipid carrier.

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Abstract

The invention discloses a silybin nanostructured lipid carrier, comprising the following components: 0.05-0.5wt% of silybin, 0.1-5wt% of a solid lipid material, 0.02-2wt% of liquid lipid, 0.2-5wt% of liposoluble emulsifier, 0.2-5wt% of water-soluble emulsifier, and the balance of water. The preparation method is an improved microemulsion technology-emulsification and evaporation-low-temperature curing method. The silybin nanostructured lipid carrier prepared by the method has the advantages of a particle size of about 200nm, a slow release function in vivio, prolonged cycle time of medicines, passive targeting in a hepatic tissue, improved bioavailability of the silybin, good biocompatibility, easy degradation, high encapsulation rate, high drug-loading rate and the like.

Description

technical field [0001] The invention relates to a silibinin nano-lipid carrier and a preparation method thereof. Background technique [0002] Silymarin (silymarin) is a kind of flavonoid lignans extracted from the seeds of the Compositae plant Silybum marianum (L.) Gaertn. Silybin (isosilibin, isosilibin), silidianim (silidianim) and silichristim (silichristim), of which silybin has the most content and the highest activity. Silybin is composed of one molecule of taxifolin (a flavonoid component) and one molecule of coniferyl alcohol (a lignan component); this type of compound has the ability to scavenge active oxygen and resist lipid peroxidation , Inhibit the production of nitric oxide (NO), inhibit 5'-lipoxygenase, protect liver cell membrane, promote liver cell repair, regeneration, immune regulation, anti-hepatic fibrosis, etc. It is mainly used clinically for acute and chronic hepatitis, Treatment of liver diseases such as alcoholic and toxic liver damage, fatty liv...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K9/19A61K31/357A61P1/16
Inventor 张典瑞贾乐姣程惠玲段存贤王言才冯飞飞
Owner SHANDONG UNIV
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