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A kind of preparation method of cordycepin proliposome

A proliposome and cordycepin technology, applied in the field of medicine, can solve the problem of limiting pharmacological activity such as anti-tumor, achieve the effect of increasing tumor targeting performance, increasing activity, and avoiding degradation

Active Publication Date: 2017-09-12
LIAONING UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, as a nucleoside alkaloid, cordycepin is metabolized very quickly in the body, which limits its pharmacological activities such as anti-tumor.

Method used

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  • A kind of preparation method of cordycepin proliposome
  • A kind of preparation method of cordycepin proliposome
  • A kind of preparation method of cordycepin proliposome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Embodiment 1 Cordycepin liposome process screening

[0026] 1. Ethanol injection method: mix and dissolve lecithin and cholesterol in a mass ratio of 4:1 in an appropriate amount of absolute ethanol to obtain a lipid solution. Add an appropriate amount of cordycepin pH 7.4 phosphate buffer into the three-necked flask. Under stirring, slowly inject the above-mentioned lipid solution into the cordycepin buffer solution, continue to stir, and after heating up to volatilize ethanol, cordycepin liposomes are obtained with an encapsulation efficiency of 28.5%.

[0027] 2. Film dispersion method: dissolve lecithin and cholesterol in an appropriate amount of chloroform at a mass ratio of 4:1, remove the organic solvent with a rotary evaporator, and form a uniform phospholipid film in an eggplant-shaped bottle. Add cordycepin phosphate buffer, stir and elute the phospholipid membrane to obtain liposomes. The encapsulation efficiency was 33.2%.

[0028] 3. pH gradient method: ...

Embodiment 2

[0033] Example 2 Process optimization for preparation of cordycepin liposomes by reverse-phase evaporation combined with freeze-drying

[0034] (1) General method:

[0035] Lecithin and cholesterol are dissolved in an appropriate amount of chloroform (oil phase) according to a certain mass ratio, and cordycepin phosphate buffer (water phase) is added. Control the volume ratio of the oil phase to the water phase, short-time ultrasound for 5 minutes to form an emulsion, and then remove the organic solvent on a rotary evaporator under reduced pressure to form a colloidal state, add an appropriate amount of distilled water, and continue to rotate to hydrate to form liposomes. Add an appropriate amount of lyoprotectant to the above-mentioned cordycepin liposome suspension, pre-freeze at -40°C for 6-12 hours, vacuumize, and continue to freeze-dry at -40°C for 40 hours to obtain cordycepin proliposomes.

[0036] (2) Optimization of liposome preparation process:

[0037] In order to...

Embodiment 3

[0069] Embodiment 3 The preparation method of cordycepin proliposome

[0070] (1) Preparation method

[0071] Dissolve 196.8 mg of lecithin and 32 mg of cholesterol in 14.0 ml of chloroform as the oil phase; 2.5 ml of cordycepin phosphate buffer with a concentration of 0.5 mg / mL as the water phase; mix the oil phase with the water phase, and ultrasonicate for 5 minutes to form milk. Then, under the condition of 37°C, remove chloroform under reduced pressure on a rotary evaporator with a vacuum degree of 0.05-0.06Mpa and a rotation speed of 60rpm, and form a colloidal state on the bottle wall without the pungent smell of chloroform. Add 15ml of distilled water and continue to rotate. Evaporate to form cordycepin liposome suspension;

[0072] Add 2ml of 8% lactose solution to the above-mentioned cordycepin liposome suspension, pre-freeze at -40°C for 6h, vacuumize, and continue to freeze-dry at -40°C for 40h to obtain cordycepin proliposomes.

[0073] (2) Physical and chemical...

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Abstract

The invention discloses a preparation method of cordycepin precursor liposome. The technical scheme adopted is: dissolving lecithin and cholesterol in an appropriate amount of chloroform as the oil phase; the cordycepin phosphate buffer as the water phase; ultrasonically forming an emulsion, placing it on a rotary evaporator to remove the chloroform under reduced pressure, and forming it on the bottle wall colloidal, add an appropriate amount of distilled water, and continue to rotary evaporation to form a cordycepin liposome suspension; add a lactose solution to the cordycepin liposome suspension, pre-freeze at ‑20~‑70°C for 4‑24 hours, and pump Vacuum, continue freeze-drying for 40-60h to obtain cordycepin proliposomes. The cordycepin liposome prepared by the method of the invention is relatively stable, and the results of pharmacokinetic study in rats show that the cordycepin liposome can increase the bioavailability of cordycepin, and has a certain long-acting and slow-release effect in vivo .

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a preparation method of cordycepin proliposome. Background technique [0002] Cordycepin, also known as cordycepin, is a nucleoside alkaloid with the molecular formula C 10 h 13 N 5 o 3 (Molecular structure shown in I), relative molecular weight 251, melting point 231 ℃. [0003] [0004] Studies have shown that, as an active ingredient in Cordyceps militaris, cordycepin has a variety of pharmacological effects: such as anti-virus, antibacterial, immune regulation and anti-tumor. It has potential therapeutic effects on many clinical diseases, and has very broad application prospects and markets. [0005] The anti-tumor effect of cordycepin is more significant. Studies have shown that cordycepin has a significant inhibitory effect on human tissue lymphoma cells U937, Ehrlich ascites tumor cells, leukemia cells HL-60 and human cervical cancer HeLa cells, and has inhibitor...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/7076A61P35/00
Inventor 郝爱军陈长兰邱马超佟丽孟雪莲
Owner LIAONING UNIVERSITY
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