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Silymarin nano-crystal self-stabilizing Pickering emulsion and preparation method thereof

A technology of silibinin and nanocrystal suspension, applied in the field of medicine, can solve the problems of complex process flow, limited drug efficacy, intestinal cytotoxicity, etc., and achieves fast release rate, good bioavailability and stability Good results

Inactive Publication Date: 2014-06-25
MACAU UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Tests have shown that the bioavailability of this type of preparation is only about 5%, which seriously limits the efficacy of the drug.
At present, the new preparations prepared by silibinin mainly include emulsions, microemulsions, self-microemulsions, microspheres, etc. However, the preparation process of such preparations is complicated, and it is difficult to carry out effective quality control; Organic reagents are represented by active agents, and surfactants may cause toxic and side effects such as allergies, hemolysis, and intestinal cytotoxicity, which is not conducive to long-term use

Method used

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  • Silymarin nano-crystal self-stabilizing Pickering emulsion and preparation method thereof
  • Silymarin nano-crystal self-stabilizing Pickering emulsion and preparation method thereof
  • Silymarin nano-crystal self-stabilizing Pickering emulsion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] A preparation method for silibinin nanocrystal self-stabilizing Pickering emulsion, comprising the following steps:

[0045] (1) Weigh 300mg of silibinin raw material drug into 80ml of ultrapure water, vortex shake for 2min, use high-speed shearing machine at 13000rpm·min -1 After shearing for 2 minutes, primary suspension A was obtained;

[0046] (2) The primary suspension A is homogeneously circulated 10 times under the condition of 1000bar to prepare the nanocrystal suspension B;

[0047] (3) Mix the prepared nanocrystal suspension B with 5ml Capmul MCM C8, and then use a high-pressure homogenizer to circulate 10 times under the condition of 1000bar to prepare a self-stable Pickering emulsion formulation.

[0048] The particle size was detected by photon correlation spectroscopy (PCS): the average particle size of the obtained emulsion was 35.8±4.2 μm, and the average particle size of the nanocrystals was 336.3±20.7 nm.

Embodiment 2

[0050] A preparation method for silibinin nanocrystal self-stabilizing Pickering emulsion, comprising the following steps:

[0051] (1) Weigh 800mg of silibinin raw material drug into 80ml of ultrapure water, vortex shake for 2min, use high-speed shearing machine at 13000rpm·min -1 After shearing for 2 minutes, primary suspension A was obtained;

[0052] (2) The primary suspension A is homogeneously circulated 10 times under the condition of 1000bar to prepare the nanocrystal suspension B;

[0053] (3) Mix the prepared nanocrystal suspension B with 5ml Capmul MCM C8, and then use a high-pressure homogenizer to circulate 10 times under the condition of 1000bar to prepare a self-stable Pickering emulsion formulation.

[0054] The particle size was detected by photon correlation spectroscopy (PCS): the average particle size of the obtained emulsion was 32.4±2.7 μm, and the average particle size of the nanocrystals was 350.4±4.8 nm.

Embodiment 3

[0056] A preparation method for silibinin nanocrystal self-stabilizing Pickering emulsion, comprising the following steps:

[0057] (1) Add 800 mg of silybin raw material drug to 80 ml of ultrapure water, vortex shake for 2 min, and use a high-speed shearing machine at 13000 rpm·min -1 After shearing for 2 minutes, primary suspension A was obtained;

[0058] (2) The primary suspension A is homogeneously circulated 10 times under the condition of 1000bar to prepare the nanocrystal suspension B;

[0059] (3) Mix the prepared nanocrystal suspension B with 5ml Capmul MCM C10, and then use a high-pressure homogenizer to circulate 10 times under the condition of 1000bar to prepare a self-stable Pickering emulsion formulation.

[0060] The particle size was detected by photon correlation spectroscopy (PCS): the average particle size of the obtained emulsion was 30.5±2.8 μm, and the average particle size of the nanocrystals was 338.4±14.3 nm.

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Abstract

The invention discloses a silymarin nano-crystal self-stabilizing Pickering emulsion and a preparation method thereof. The emulsion is an oil-in-water type Pickering emulsion consisting of silymarin nano-crystal, an oil phase and water. According to the preparation method of the Pickering emulsion, nano-crystal is prepared from silymarin by utilizing a high pressure homogenization method, so that silymarin nano-crystal is adsorbed to the surface of an oil drop, the oil drop is coated with a medicine, the medicine is partially dissolved in the oil phase and partially adsorbed to the surface of the oil drop in a nano-crystal mode, and the oil drop can be stably distributed in water to form a stable emulsion; the medicine in the emulsion is an effective component, and can play a role in stabilizing the emulsion. The emulsion prepared by the method does not contain a surfactant or an organic solvent, and has stability, quick release speed and excellent bioavailability.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a silibinin nanocrystal self-stabilizing Pickering emulsion and a preparation method thereof. Background technique [0002] Silybin, English name: silybin, is a flavonoid lignan compound extracted from milk thistle Silybum marianum (L) Genrtn, its structural formula is: [0003] [0004] Silybin is a liver cell membrane stabilizer, which can effectively protect and strengthen the liver cell mucosa, protect the enzyme system of liver cells and remove active oxygen free radicals in liver cells. At the same time, silybin can not only reduce blood cholesterol Concentration, can further remove fat deposits in liver tissue. Clinically, it is mainly used in hepatitis and cholecystitis. It has also recently been shown that silibinin has antitumor effects, especially for prostate cancer. Therefore, silibinin has attracted much attention since its discovery, but due to its extremely...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/357A61P1/16A61P35/00
Inventor 易涛刘川
Owner MACAU UNIV OF SCI & TECH
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