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A kind of wedelia lactone nano-liposome jointly modified with chitosan and polyethylene glycol and preparation method thereof

A technology of isthrin and nano-liposomes is applied in the directions of liposome delivery, medical preparations of inactive ingredients, drug combinations, etc., and can solve the problems of unfavorable drug absorption, frequent medication times, low bioavailability, and the like, To achieve the effect of improving the therapeutic effect, reducing the dosage, and the preparation method is simple

Inactive Publication Date: 2016-04-06
YANSHAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, the extremely low solubility of wedelolide in water is not conducive to the absorption of the drug by the human body, and the bioavailability is low, resulting in a large dosage and frequent medication times, which limits the full play of its pharmacological effects

Method used

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  • A kind of wedelia lactone nano-liposome jointly modified with chitosan and polyethylene glycol and preparation method thereof
  • A kind of wedelia lactone nano-liposome jointly modified with chitosan and polyethylene glycol and preparation method thereof
  • A kind of wedelia lactone nano-liposome jointly modified with chitosan and polyethylene glycol and preparation method thereof

Examples

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Effect test

example 1

[0024] Take 1 mg of wedelolide (purchased from Shanghai Zhanshu Chemical Technology Co., Ltd.), 50 mg of soybean lecithin (purchased from Shenyang Tianfeng Biopharmaceutical Co., Ltd.) and 10 mg of cholesterol (purchased from Tianjin Damao Chemical Instrument Supply Station) Dissolve in 2 ml of absolute ethanol, and stir magnetically at a constant temperature of 43°C to obtain a uniform oil phase, ie lipid ethanol solution. Get 10 mg of polyethylene glycol-2000 (purchased from Tianjin Kemiou Chemical Reagent Co., Ltd.) and 10 mg of chitosan, the chitosan is dissolved with 0.1% acetic acid solution, and the pH value is controlled at 4, and the above poly Ethylene glycol-2000 and chitosan acetic acid solution were added to phosphate buffer (0.1M, pH 6.5) as a hydration medium at 48°C, and magnetically stirred at a constant temperature of 48°C to obtain an aqueous phase. The lipid ethanol solution obtained above was dropped dropwise into the obtained aqueous phase to obtain a lip...

example 2

[0026] Take 1 mg of wedelolide (purchased from Shanghai Zhanshu Chemical Technology Co., Ltd.), 65 mg of soybean lecithin (purchased from Shenyang Tianfeng Biopharmaceutical Co., Ltd.) and 6 mg of cholesterol (purchased from Tianjin Damao Chemical Instrument Supply Station) Dissolve in 2 ml of absolute ethanol, and stir magnetically at a constant temperature of 38° C. to obtain a uniform oil phase, namely lipid ethanol solution. Get 2 mg of polyethylene glycol-2000 (purchased from Tianjin Kemiou Chemical Reagent Co., Ltd.) and 2 mg of chitosan, the chitosan is dissolved with 0.1% acetic acid solution, the pH value is controlled at 4, the above poly Ethylene glycol-2000 and chitosan acetic acid solution were added to phosphate buffer (0.1M, pH 6.5) as a hydration medium at 38°C, and magnetically stirred at a constant temperature of 38°C to obtain an aqueous phase. The lipid ethanol solution obtained above was dropped dropwise into the obtained aqueous phase to obtain a liposome...

example 3

[0028] Take 1 mg of wedelolide (purchased from Shanghai Zhanshu Chemical Technology Co., Ltd.), 80 mg of soybean lecithin (purchased from Shenyang Tianfeng Biopharmaceutical Co., Ltd.) and 2 mg of cholesterol (purchased from Tianjin Damao Chemical Instrument Supply Station) Dissolve in 5 ml of absolute ethanol, and stir magnetically at a constant temperature of 48°C to obtain a uniform oil phase, ie lipid ethanol solution. Get 10 mg of polyethylene glycol-2000 (purchased from Tianjin Kemiou Chemical Reagent Co., Ltd.) and 10 mg of chitosan, the chitosan is dissolved with 0.5% acetic acid solution, and the pH value is controlled at 4, and the above poly Ethylene glycol-2000 and chitosan acetic acid solution were added to phosphate buffer (0.1M, pH 6.5) as a hydration medium at 43°C, and magnetically stirred at a constant temperature of 43°C to obtain an aqueous phase. The lipid ethanol solution obtained above was dropped dropwise into the obtained aqueous phase to obtain a lipo...

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Abstract

The invention relates to a wedelolactone nanoliposome modified by combining chitosan and polyethylene glycol, which comprises long circulating liposome and a medicine active component wrapped in the long circulating liposome, the long circulating liposome is liposome modified by combining chitosan and polyethylene glycol on surface of liposome, the active component is wedelolactone, and wedelolactone is encapsulated between a bilaminar membrane of liposome. The preparation method of nanoliposome comprises the following steps: dissolving wedelolactone, soya lecithin and cholesterol in absolute ethyl alcohol, performing constant temperature magnetic stirring to obtain homogeneous oil phase, adding polyethylene glycol-2000 and chitosan in a hydration medium phosphoric acid buffer, performing constant temperature magnetic stirring to obtain the water phase; dropping the oil phase in the water phase to obtain a lipid suspension; removing absolute ethyl alcohol, and employing a cell ultrasonic pulverizer for performing interval ultrasound under ice bath. The preparation method can be carried out under normal temperature, normal pressure and mild condition, and has the advantages of simple technology and easy control, the obtained liposome has an ideal morphology, and the bioavailability is increased.

Description

technical field [0001] The invention relates to a liposome of medicine and a preparation method thereof. Background technique [0002] Wedelolactone (wedelolactone, WL), molecular formula C16H10O7, molecular weight 314.25, belongs to furanocoumarins, and its distribution in plants is relatively limited. Carbon tetrachloride, galactosamine, and phalloidin induce hepatotoxicity and stimulate hepatocyte regeneration. In the study of MorsWB and partner MeloPA, it was found that wedelolide has antivenom effect. In addition, its immune regulation, anti-inflammation, selective enzyme inhibition and other effects provide more options for the development of new drugs for human beings. [0003] Studies have found that the inhibitory effect of wedelide on topoisomerase IIα can hinder the synthesis of DNA, thereby inhibiting tumor growth and inducing tumor cell apoptosis. Recently, the latest scientific research results published by Yu Qiang's research group at the Shanghai Institute...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/37A61K47/36A61K47/34A61P35/00
Inventor 高大威李楠刘艳平边艳红赵婷婷
Owner YANSHAN UNIV
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