Curcumin active drug-loading liposome and preparation method thereof

A technology of curcumin lipid and curcumin, which is applied in the field of curcumin active drug-loaded liposomes and its preparation, can solve problems such as poor stability, decreased cell activity of drug-loaded preparations, and general drug effects, so as to improve accumulation and benefit The effect of cellular uptake

Active Publication Date: 2021-03-09
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Passive drug-loaded liposomes have disadvantages such as low encapsulation efficiency and poor stability; and usually after loading curcumin with nanocarriers, the cell activity of drug-loaded preparations will decrease, resulting in mediocre drug effects in animals.

Method used

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  • Curcumin active drug-loading liposome and preparation method thereof
  • Curcumin active drug-loading liposome and preparation method thereof
  • Curcumin active drug-loading liposome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 2

[0065] Inner aqueous phase concentration of embodiment 2 has influence on curcumin liposome particle size and encapsulation efficiency

[0066] According to the method in Example 1 and using copper acetate as the internal water phase, the concentration of the internal water phase was set according to the table below to prepare blank liposomes. The prepared blank liposomes and curcumin were co-incubated at 65°C for 30 minutes according to the drug-to-lipid ratio of 1:10. After the drug loading was completed, the drug loading was terminated in ice bath, and the liposome particle size and encapsulation efficiency were measured. The results were See image 3 .

[0067]

[0068]

[0069] The result shows: along with the increase of internal aqueous phase concentration, curcumin encapsulation efficiency also increases, and when concentration is greater than 200mM, liposome encapsulation efficiency declines to some extent, and particle diameter also increases significantly.

Embodiment 3

[0070] The effect of embodiment 3 drug-lipid ratio on liposome particle size encapsulation efficiency

[0071] Weigh 68.1mg of HSPC, 22.8mg of Chol, and 1.2mg of DSPE-PEG2000, dissolve them in chloroform, remove the organic solvent by rotary evaporation under reduced pressure at 37°C to form a phospholipid film, and hydrate with 200mM copper acetate solution at 65°C for 30min to obtain the crude product The liposome solution passes through 0.4, 0.2, 0.1 μm polycarbonate membranes sequentially in the extrusion device, and the particle size is measured. The metal ions outside the liposomes were removed by Sephadex chromatography column exchange, and the outer water phase was exchanged with HEPES buffer to obtain blank liposomes. Dissolve curcumin in DMSO, prepare 20mg / mL curcumin solution, add 50μL curcumin solution to 1mL 10mg / mL blank liposomes, incubate at 65°C for 30 minutes, stop drug loading in ice bath, and measure particle size. diameter and encapsulation efficiency, th...

Embodiment 4

[0073] The impact of embodiment 4 external water relative curcumin liposome encapsulation efficiency

[0074] Weigh 68.1mg HSPC, 22.8mg Chol, 1.2mg DSPE-PEG2000, dissolve in chloroform, remove the organic solvent by rotary evaporation under reduced pressure at 37°C to form a phospholipid film, and hydrate with 200mM copper acetate or zinc acetate solution at 65°C for 30min , The resulting crude liposome solution passed through 0.4, 0.2, and 0.1 μm polycarbonate membranes in sequence in an extrusion device, and the particle size was measured. Remove liposome external metal ions by Sephadex chromatographic column exchange and exchange the external water phase for HEPES buffer (pH 5.0), HEPES buffer (pH 6.0), HEPES buffer (pH 7.0), HEPES buffer ( pH 8.0), to obtain blank liposomes. Dissolve curcumin in DMSO, prepare 20mg / mL curcumin solution, add 50μL curcumin solution to 1mL 10mg / mL blank liposomes, incubate at 65°C for 30 minutes, stop drug loading in ice bath, and measure par...

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Abstract

The invention relates to the field of liposome drug delivery, in particular to a curcumin active drug-loading liposome and a preparation method thereof. The curcumin active drug-loading liposome is prepared from the following components of curcumin, phospholipid, cholesterol (Chol), a metal ion salt solution and an external water phase buffer solution, wherein the weight ratio of the curcumin to total phospholipid (the sum of phospholipid and cholesterol) is 0.5-1:10, the metal ion salt solution can be a sulfate, gluconate or acetate solution of copper ions or zinc ions, and the concentrationof the copper ions or the zinc ions in the metal ion salt solution is 50-300 mM. The curcumin active drug-loading liposome and the preparation method thereof have the characteristics that a curcumin active drug-loading liposome preparation with petal-like conformation is successfully prepared for the first time, cell experiments show that the curcumin active drug-loading liposome preparation has stronger active oxygen production capability and stronger tumor cell inhibition activity, and tumor-bearing mouse experiments show that the preparation has remarkable subcutaneous tumor growth inhibiting and metastatic tumor progress relieving effects.

Description

technical field [0001] The invention relates to the field of liposome drug delivery, in particular to a curcumin active drug-loading liposome and a preparation method thereof. Background technique [0002] Curcumin (Curcumin, Cur) is a chemical component extracted from the rhizomes of some plants in Zingiberaceae and Araceae. It is a diketone compound. It is an orange-yellow crystalline powder with a slightly bitter taste and is insoluble in water. Dissolved in ethanol, soluble in DMSO, DMF, PEG400 and other solvents. A large number of studies have proved that curcumin has many important biological effects, including anti-inflammation, anti-coagulation, anti-oxidation, anti-angiogenic and anti-tumor activities, promoting wound healing, reducing blood lipids, preventing cardiovascular diseases and nervous system degenerative diseases, etc. It is used to treat liver disease, digestive system, infection, rheumatoid arthritis, etc. Studies have shown that it can prevent the oc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/12A61K47/52A61P35/00A61P35/04
CPCA61K31/12A61K9/1277A61K47/52A61P35/00A61P35/04
Inventor 刘洪卓周双何仲贵王永军
Owner SHENYANG PHARMA UNIVERSITY
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