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Method for preparing albumin nanoparticles and freeze-dried powder of piperlongumine

A technology of albumin nanoparticles and perylene amide, which is applied in the field of biomedicine, can solve problems such as allergic contact dermatitis, high toxicity, and pollution, and achieve the effects of improving solubility, improving drug efficacy, and reducing adverse reactions

Pending Publication Date: 2019-07-26
LIAONING UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among them, glutaraldehyde is mostly used as a cross-linking agent, but glutaraldehyde itself has relatively high toxicity, which can cause allergic contact dermatitis, asthma, etc.
In addition, the pollution of glutaraldehyde to the environment is also relatively serious.

Method used

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  • Method for preparing albumin nanoparticles and freeze-dried powder of piperlongumine
  • Method for preparing albumin nanoparticles and freeze-dried powder of piperlongumine
  • Method for preparing albumin nanoparticles and freeze-dried powder of piperlongumine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Effects of organic solvent types on the particle size and zeta potential of albumin nanoparticles with perylene amide.

[0038] The preparation method is as follows:

[0039] (1) Get 14.7mg of perylene amide crude drug and dissolve in 4mL of organic solvent as the organic phase. The organic solvents are absolute ethanol, absolute ethanol-dichloromethane (v:v=3:1), and absolute ethanol-dichloromethane (v:v=6:1).

[0040] (2) Dissolve 0.4 g of bovine serum albumin in 40 mL of pure water, adjust the pH to 6 with a pH regulator, and use it as the water phase.

[0041] (3) Slowly drop the organic phase into the water phase under the action of high-speed shear at 7000r / min, and then shear and disperse at 10000r / min for 15min to obtain colostrum.

[0042] (4) Gained colostrum is transferred to a high-pressure micro-fluidic nano-disperser, homogenized 9 times at 80 psi. After the homogenization was completed, the organic solvent was removed by rotary evaporation at 50° C. to...

Embodiment 2

[0047] Effects of bovine serum albumin concentration on the particle size and zeta potential of albumin nanoparticles

[0048] The preparation method is as follows:

[0049] (1) Get 14.7mg of perylene amide crude drug and dissolve in 3mL of absolute ethanol and 1mL of dichloromethane as the organic phase.

[0050] (2) Take 0.2g bovine serum albumin, 0.4g bovine serum albumin, and 0.8g bovine serum albumin and dissolve them in 40mL pure water respectively to obtain bovine serum with mass volume percentage concentration of 0.5%, 1%, and 2%. The serum albumin solution, adjusted to pH 6 with a pH regulator, was used as the aqueous phase.

[0051](3) Slowly drop the organic phase into the water phase under the action of high-speed shear at 7000r / min, and then shear and disperse at 10000r / min for 15min to obtain colostrum.

[0052] (4) Gained colostrum is transferred to a high-pressure micro-fluidic nano-disperser, homogenized 9 times at 80 psi. After the homogenization was compl...

Embodiment 3

[0057] Effect of volume ratio of organic phase to aqueous phase on particle size and zeta potential of albumin nanoparticles

[0058] The preparation method is as follows:

[0059] (1) Get 14.7mg of perylene amide crude drug and dissolve in 3mL of absolute ethanol and 1mL of dichloromethane as the organic phase.

[0060] (2) By volume ratio, organic phase: water phase=1:4, 1:10, 1:15, get the bovine serum albumin solution that mass volume percent concentration is 1% respectively, adjust PH to be 6 with PH regulator , as the aqueous phase.

[0061] (3) Slowly drop the organic phase into the water phase under the action of high-speed shear at 7000r / min, and then shear and disperse at 10000r / min for 15min to obtain colostrum.

[0062] (4) Gained colostrum is transferred to a high-pressure micro-fluidic nano-disperser, homogenized 9 times at 80 psi. After the homogenization was completed, the organic solvent was removed by rotary evaporation at 50° C. to obtain an aqueous solut...

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Abstract

The invention discloses a method for preparing albumin nanoparticles and freeze-dried powder of piperlongumine and belongs to the technical field of medicine. The method includes: dissolving the raw material medicine of piperlongumine in an appropriate amount of an organic solvent as an organic phase; dissolving bovine serum albumin in pure water as a water phase; slowly dripping the organic phaseinto the water phase under the action of high speed shear, and performing shear dispersion to obtain colostrum; transferring the colostrum to a high pressure micro-jet nano-dispersion instrument to be homogenized at appropriate pressure; after homogenization, removing the organic solvent by rotating evaporation to obtain albumin nanoparticles of the piperlongumine, and freeze drying the albumin nanoparticles to obtain the albumin freeze-dried powder of the piperlongumine. The albumin nanoparticles of the piperlongumine can improve water solubility of the piperlongumine and improve the bioavailability of the medicine; the preparation process is simple, the use of glutaraldehyde is avoided, and good safety is achieved.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to a preparation method of pinionamide albumin nanoparticles and freeze-dried powder thereof. Background technique [0002] Piperonamide is a natural alkaloid compound extracted from plants of the family Piperaceae. Molecular formula is C 17 h 19 NO 5 , the chemical name is 5,6-dihydro-1-[1-oxo-3-(3,4,5-trimethoxyphenyl)-2-propenyl]-2(1H)pyridone, the melting point is 24°C, the structural formula is as shown in (I): [0003] [0004] Studies have shown that perylene amide can play an anti-cancer role by increasing the level of reactive oxygen species (ROS) in cells, and effectively inhibit tumor growth in vivo. Perylene amide has significant cytotoxic effect on glioblastoma, colon cancer, ovarian cancer, prostate cancer, breast cancer, liver cancer and other malignant tumors, but has almost no effect on normal cells. Therefore, perylene amide has great devel...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K9/19A61K47/42A61K31/4412A61P35/00
CPCA61K9/19A61K9/5052A61K31/4412A61P35/00
Inventor 郭忠秋刘宇
Owner LIAONING UNIVERSITY
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