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Phosphatidylserine-modified curcumin nanoparticles

A technology of phosphatidylserine and curcumin is applied in the field of biomedicine to achieve the effects of increasing intake, improving anti-inflammatory efficacy and low cost

Inactive Publication Date: 2016-10-12
FOURTH MILITARY MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

After patent search and literature search, the applicant found that the nano-carrier that actively targets macrophages and uses drugs and carriers to exert a synergistic anti-inflammatory effect - phosphatidylserine-modified curcumin nanoparticles has not been reported

Method used

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  • Phosphatidylserine-modified curcumin nanoparticles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Embodiment 1: the preparation method selection of the curcumin nanoparticle of phosphatidylserine modification

[0037] The common preparation methods of nano-lipid carriers mainly include high-pressure homogenization method, melt emulsification method, melt ultrasonic method, solvent diffusion method, solvent emulsification evaporation method, high-speed stirring ultrasonic method, microemulsion method, etc. Among them, the high-pressure homogenization method requires a higher temperature, usually about 80°C, and heat-sensitive drugs are not suitable for preparation by this method. However, it is difficult to prepare nanostructured lipid carriers with smaller particle size and narrower distribution by cold high-pressure homogenization method. Therefore, in combination with the characteristics of the drug, the following preparation methods were screened out for investigation.

[0038]1.1 Emulsification evaporation method - low temperature curing method

[0039] In mol...

Embodiment 2

[0045] Embodiment 2: Screening of phosphatidylserine / phospholipid molar ratio in curcumin nanoparticles modified by phosphatidylserine

[0046] According to the result in Example 1, the curcumin nanoparticles modified by PS are prepared by film dispersion method, and other conditions are fixed, and the preparation of PS modified amount (mol%) is respectively 0%, 4%, 8%, 12%, 20% curcuma prime nanoparticles. The particle size was measured with a laser particle size analyzer, and the encapsulation efficiency was determined. Investigate the effect of PS mole ratio on the particle size and encapsulation efficiency of curcumin nanoparticles, so as to determine the range of effective PS mole ratio for follow-up experiments.

[0047] Table 1: Particle size, polydispersity coefficient and encapsulation efficiency of curcumin nanoparticles with different PS modification amounts (mol%) (Mean±SD, n=3)

[0048] PS modification amount (mol%)

[0049] The results showed that whe...

Embodiment 3

[0050] Example 3: Phosphatidylserine-modified curcumin nanoparticles formulation optimization

[0051] The amount of fixed PS (mol%) is 8%, and the particle size and encapsulation rate are used to investigate the indicators, and the film dispersion method is used to prepare curcumin nanoparticles. , pH value of phosphate buffer solution and other prescription factors were optimized.

[0052] 3.1 Selection of phospholipid types

[0053] Fix other conditions unchanged, respectively use domestic common soybean phospholipids, soybean phospholipid S100 from Lipoid Company of Germany, and egg phospholipid PC 98-T from Shanghai AVT Company to prepare PS-modified curcumin nanoparticles by thin film dispersion method, and use laser particle size analyzer Measure its particle size and determine its encapsulation efficiency.

[0054] Table 2: Particle size, polydispersity coefficient and encapsulation efficiency of curcumin nanoparticles of different phospholipid types (Mean±SD, n=3) ...

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Abstract

The invention discloses phosphatidylserine-modified curcumin nanoparticles; with biological endogenous phosphatidylserine (PS) as a membrane material, an anti-inflammatory drug curcumin is coated, and the PS-modified curcumin nanoparticle targeted drug delivery system is prepared; through simulating apoptotic cells, curcumin nanoparticles are identified by specific receptors on the surface of macrophages, and in virtue of the receptor mediated macrophage active targeting effect, macrophage uptake is enhanced; the drug curcumin enters the macrophages, then the anti-inflammatory effect is exerted, at the same time, a PS carrier is taken in, then the macrophages are induced to produce anti-inflammatory response, that is to say, release of pro-inflammatory cytokines is reduced, secretion of anti-inflammatory cytokines is increased, and the drug and carrier synergistic anti-inflammatory effect is reached; the PS-modified curcumin nanoparticles can be used for application of drugs for treating macrophage mediated related diseases.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and specifically relates to a phosphatidylserine-modified curcumin nanoparticle, which can specifically target macrophages and exert the synergistic anti-inflammatory effect of drugs and carriers to treat macrophage-mediated related diseases. Background technique [0002] Current studies have found that many diseases are related to inflammatory responses, such as atherosclerosis, cancer, diabetes, rheumatoid arthritis, etc., which need to be treated with anti-inflammatory drugs. As the main immune cells of the body, macrophages play an important role in these inflammatory diseases, can promote pathogenic inflammatory responses, and are the target cells of many anti-inflammatory drugs. Using a novel targeted drug delivery system to target anti-inflammatory drugs to macrophages can improve the efficacy of anti-inflammatory drugs and reduce their toxic side effects. Therefore, the development ...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/12A61K9/14A61K47/24A61P29/00
CPCA61K9/145A61K31/12
Inventor 王晓娟王济冯斌
Owner FOURTH MILITARY MEDICAL UNIVERSITY
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