Method for applying artemisinin derivative and lipidosome of artemisinin derivative to preparation of sound sensitive agent

A technology of artemisinin derivatives and liposomes, applied in liposome delivery, antifungal agents, antiviral agents, etc., can solve the problems of clinical practical application limitations, skin phototoxicity, unstable composition and properties, etc.

Active Publication Date: 2015-05-20
FUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, sonodynamic therapy has not been able to enter clinical application, and the key problem is the lack of sound sensitizers with good properties
At present, the sonosensitizers widely used in experimental research are the first-generation photosensitizers such as hematoporphyrin and gallium porphyrin derivatives. These sensitizers have disadvantages: they have strong absorption in the 400-500nm region (the light in this band is positively absorbed). It is rich in natural light), resulting in greater skin phototoxicity under natural light (need to avoid light for 2-4 weeks), unstable composition and properties (hematoporphyrin derivatives are mixtures), and the sound sensitization ability needs to be improved. Practical applications are limited
However, there is no research report on them as sonodynamic antitumor drugs in the literature at present.

Method used

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  • Method for applying artemisinin derivative and lipidosome of artemisinin derivative to preparation of sound sensitive agent

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Preparation of artemisinin liposomes

[0034] Mix and dissolve 80 mg soybean lecithin, 20 mg cholesterol, 0.5 mg vitamin E, and 10 mg artemisinin in 5 ml chloroform solution, and transfer the mixed solution into a 250 ml round bottom flask. After the organic solvent was removed by rotary evaporation under reduced pressure, the round bottom flask was immersed in a constant temperature water bath at 30 °C and rotated at a speed of 60 r / min until the dry lipid film was deposited on the wall of the bottle to form a thin film. Place the film-forming round-bottom flask in a vacuum drying oven, and dry at room temperature under high vacuum for 1-2 h. Add 5 ml of PBS and 0.5 g of glass beads into a round-bottomed flask that forms a lipid film, and rotate at 60 r / min for 30-40 min at room temperature and normal pressure, so that all the lipids attached to the wall are detached from the wall of the bottle and formed Milky white suspension, let the suspension stand at room temper...

Embodiment 2

[0038] Preparation of dihydroartemisinin liposomes

[0039] According to the method of Example 1, using dihydroartemisinin instead of artemisinin in Example 1, dihydroartemisinin liposomes with an encapsulation efficiency of 20-85% (particle size is about 130-160 nm ).

Embodiment 3

[0041] Preparation of artemether liposomes

[0042] According to the method in Example 1, artemether was used instead of artemisinin in Example 1 to obtain artemether liposomes (with a particle size of about 130-160 nm) with an encapsulation efficiency of 20-85%.

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Abstract

The invention discloses a method for applying artemisinin derivative and lipidosome of the artemisinin derivative to preparation of a sound sensitive agent. When the artemisinin derivative and the lipidosome of the artemisinin derivative are used as the sound sensitive agent to prepare sound power drugs, the safety performance is high, and sound power antitumor activity is high.

Description

technical field [0001] The invention belongs to the field of functional materials and medicines, in particular to the application of an artemisinin derivative and its liposome in the preparation of a sound sensitizer. Background technique [0002] Sonodynamic Therapy (SDT) is the use of non-thermal ultrasound to activate the sound sensitizer in the target site, trigger a series of reactions, generate reactive oxygen species or other active substances, thereby killing tumor cells or other abnormal cells, and achieve therapeutic effect. Purpose. As an emerging non-invasive and highly selective treatment method, the application prospect of sonodynamic therapy in the treatment of tumors has attracted attention. [0003] Sonodynamic therapy is established and developed on the basis of photodynamic therapy. Photodynamic therapy (PDT) uses light to activate the photosensitizer enriched in the target tissue to generate active oxygen and destroy the target tissue. With the develop...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/357A61K41/00A61K9/127A61P35/00A61P17/00A61P31/12A61P31/04A61P31/10A62D3/13A62D101/28
Inventor 黄剑东黄秀蓉
Owner FUZHOU UNIV
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