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Cordycepin nanometer liposome, preparation method, and antitumor activity applications thereof

A nano-liposome and cordycepin technology, which is applied in the direction of anti-tumor drugs, liposome delivery, organic active ingredients, etc., can solve the problem that the encapsulation rate of liposomes can only be reached, but the encapsulation rate of liposomes cannot be reached, and there is no further progress Issues such as the verification of the activity of cordycepin liposomes in vivo, to achieve short half-life, inhibit the growth of tumors, and facilitate absorption

Inactive Publication Date: 2017-06-06
王春梅
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Wang Chengming from Shandong University of Light Industry prepared cordycepin liposomes by using the reverse evaporation method, that is, the lecithin and cholesterol used were purified, and on this basis, the concentration of lecithin / cholesterol, cordycepin, organic phase / water The three factors were investigated, and the formula was optimized, but the encapsulation efficiency only reached 50.81%, which was far below the liposome encapsulation efficiency required by the Pharmacopoeia, and it did not continue to carry out the activity of cordycepin liposomes in vivo. Verification (Wang Chengming; Cordycepin / liposome preparation and biological activity research [D]; Shandong Institute of Light Industry)

Method used

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  • Cordycepin nanometer liposome, preparation method, and antitumor activity applications thereof
  • Cordycepin nanometer liposome, preparation method, and antitumor activity applications thereof
  • Cordycepin nanometer liposome, preparation method, and antitumor activity applications thereof

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Experimental program
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Effect test

Embodiment 1

[0026] Preparation of cordycepin liposomes whose phospholipid is hydrogenated soybean lecithin by pH gradient method or reverse evaporation method

[0027]

[0028] Preparation method: (1) pH gradient method

[0029] ① Take the prescribed amount of lecithin, cholesterol, Tween 80 and V E Dissolve in 10ml of chloroform to form a clear solution, and remove the chloroform by rotary evaporation under reduced pressure in a 45°C water bath to form a uniform lipid film.

[0030]② Add 10ml of pH4.0 citric acid buffer, hydrate in a 45°C water bath under normal pressure for 20 minutes, and then hydrate with magnetic stirring in a 45°C water bath for 1 hour. Ultrasonic the probe for 70 seconds (power 360W, super 3 seconds stop 4 second), and then pass through the microporous membrane method of 0.45 μm and 0.22 μm respectively to size the particles to obtain blank liposomes.

[0031] ③ Add the cordycepin solution, adjust the pH value to 7-7.4 with 1mol / L disodium hydrogen phosphate s...

Embodiment 2

[0036] Cordycepin liposomes whose phospholipid is hydrogenated soybean lecithin were prepared by the combination of "PH gradient method-reverse evaporation method"

[0037]

[0038]

[0039] Preparation method: ① Combine lecithin, cholesterol, Tween 80, V E The fat-soluble components are dissolved in 10ml of chloroform to form a clear solution.

[0040] ② Dissolve cordycepin in 5ml of citric acid buffer solution with pH 4.0, slowly add to the oil phase, and shear emulsify until a stable W / O emulsion is formed.

[0041] ③Place the emulsion in a 37°C water bath to remove the chloroform by rotary evaporation under reduced pressure, and form a gel on the bottle wall (a little PBS solution with pH 7.4 can be added), and continue the rotary evaporation to make the gel on the bottle wall fall off.

[0042] ④ 1mol / L disodium hydrogen phosphate solution to adjust the pH value of the external water phase to about 7.0, and PBS buffer solution with pH 7.4 to adjust the concentratio...

Embodiment 3

[0045] Determination of Liposome Encapsulation Efficiency

[0046] The method used Sephadex gel method, the specific steps are as follows:

[0047] 1. Take 0.5ml of the prepared cordycepin liposome, slowly add it to the pre-saturated Sephadex G-25 column, elute with normal saline at a flow rate of 0.9ml / min, collect the free drug part, and repeat the collection for three times. The parts were recorded as sample 1, sample 2, and sample 3, and the content of cordycepin in the free drug eluent was determined by high performance liquid chromatography. In addition, take 0.125ml of cordycepin liposome, demulsify with 0.875ml of methanol, and pass through a 0.45μm organic filter to obtain a sample, which is recorded as the total sample. After liquid phase quantitative determination, 4 times its value is regarded as 0.5ml lipid The total cordycepin content in the body.

[0048] 2. Liquid chromatography conditions for determination of cordycepin content

[0049] Instrument: Agilent ...

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Abstract

The present invention belongs to the technical field of medicine, and discloses a cordycepin nanometer liposome, a preparation method, and antitumor activity applications thereof. The cordycepin is easily degraded in vivo so as to deactivate. According to the present invention, the in vitro and in vivo antitumor activity results of the product show that the cordycepin liposome provides significant inhibition effects on liver cancers, and the in vivo activity of the cordycepin is well retained through the liposome dosage form; the cordycepin liposome difficultly achieves the high encapsulation rate through the existing preparation method; the cordycepin nanometer liposome of the present invention comprises cordycepsin, phospholipid, cholesterol, a surfactant, and an antioxidants; and the preparation method combines a pH gradient method and a reverse evaporation method, wherein the cordycepin nanometer liposome obtained through the preparation method has characteristics of high encapsulation rate (more than or equal to 90%), uniform particle size, and good stability.

Description

[0001] Technical field: [0002] The invention belongs to the technical field of new drug research and development, and in particular relates to a cordycepin nano liposome, a preparation method thereof and application of antitumor activity. [0003] Background technique: [0004] Cordycepin, also known as cordycepin and cordycepin, is the earliest active monomer component extracted from Cordyceps militaris. Studies have shown that cordycepin can promote cell differentiation, inhibit mRNA synthesis, and induce cell apoptosis , thereby inhibiting the growth of various tumor cells (Tuli HS, Sharma AK, Sandhu SS, Kashyap D. Cordycepin: Abioactive metabolite with therapeutic potential. Life Sci. 2013, 93(23): 863-869.). However, there are also related reports that cordycepin, which has a broad and powerful inhibitory effect on tumor cell growth in vitro, has little activity in vivo. Studies have shown that cordycepin is easily degraded by adenosine deaminase (ADA) in the body into ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/7076A61P35/00A61P35/02
Inventor 王春梅武鹏凯陶志欧阳召
Owner 王春梅
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