A traditional Chinese medicine-magnetic nanocluster chemoimmunodrug delivery system and preparation method thereof

A technology for immune drugs and delivery systems, applied in the field of medicine, to achieve the effects of efficient tumor aggregation, precise targeting, and stable circulation in the body

Active Publication Date: 2021-10-15
JIANGSU PROVINCE INST OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, small-sized (50nm) nanoparticles are difficult to penetrate into hypoxic regions, which is also a hot issue in the field of nano-preparation in recent years.

Method used

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  • A traditional Chinese medicine-magnetic nanocluster chemoimmunodrug delivery system and preparation method thereof
  • A traditional Chinese medicine-magnetic nanocluster chemoimmunodrug delivery system and preparation method thereof
  • A traditional Chinese medicine-magnetic nanocluster chemoimmunodrug delivery system and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] This example takes ganoderma acid A-magnetic nanoparticles (G-SPIONs) as an example to illustrate the preparation method and characterization of traditional Chinese medicine-magnetic nanoparticles.

[0068] with FeCl 2 and FeCl 3 Mixed aqueous solution as raw material, pullulan as stabilizer, 3-aminopropyltriethoxysilane as amino source, precipitated by NaOH solution, NH 3 ·H 2 O adjust the pH and other steps to prepare SPIONs. Under magnetic stirring, the chloroform solution of ganoderma acid A was slowly dropped into the chloroform solution of SPIONs. After rotary evaporation, the aqueous solution was redissolved, and G-SPIONs were obtained after passing through the membrane. The G-SPIONs were observed by transmission electron microscopy to be round in shape and uniform in particle size ( figure 2 A); Conventional pharmaceutical analysis results show that when ganoderma acid A accounts for 6% of the mass fraction of iron oxide, its encapsulation efficiency is 82....

Embodiment 2

[0071] This example illustrates the preparation method of mannose-modified ganoderma acid A-magnetic nanoparticles (MG-SPIONs).

[0072] Disperse the G-SPIONs prepared in Example 1 in deionized water, slowly add equimolar amounts of succinic acid, 1.1eq of EDC and 1.3eq of NHS at room temperature, add equimolar amounts of mannose after stirring for 2 hours, and continue Stir at room temperature for 24 hours, then dialyze with running water to remove unreacted small molecules, and prepare MG-SPIONs.

[0073] With the same preparation and detection method, ganoderma acid A can also be replaced by ganoderma acid B, ganoderma acid, ganoderma triterpenes, ursolic acid, oleanolic acid, coroic acid, tripterine, ginseng triterpene saponins, Bupleurum Triterpene saponins, astragalus triterpene saponins, etc.

[0074] Succinic acid can also be substituted by malonic acid, glutaric acid, suberic acid, and the like.

Embodiment 3

[0076] This example takes Ganoderma acid A-magnetic nanoparticles (MG-SPIONC) as an example to illustrate the preparation method and characterization of traditional Chinese medicine-magnetic nanoclusters

[0077] The MG-SPIONs prepared in Example 2 were dispersed in 5% dimercaptosuccinic acid, stirred at room temperature for 24 hours, and the free cross-linking agent was removed by running water dialysis to prepare MG-SPIONC. The results of routine dialysis pharmaceutical analysis showed that the encapsulation rate of ganoderma acid A was 80.4±4.4%, and the drug loading was 2.2±0.3%; the particle size of MG-SPIONC was 146.4±5.5nm, the PDI was 0.191±0.001, and the zeta potential was -14.45±1.64mV; MG-SPIONC was stored for 7 days and obvious settlement was observed.

[0078] With the same preparation and detection method, ganoderma acid A can also be replaced by ganoderma acid B, ganoderma acid, ganoderma triterpenes, ursolic acid, oleanolic acid, coroic acid, tripterine, ginsen...

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Abstract

The invention relates to a traditional Chinese medicine-magnetic nano-cluster chemoimmunomedicine delivery system and a preparation method thereof, comprising superparamagnetic oxide nanoparticles; the surface of the superparamagnetic oxide nanoparticles anchors drugs and targeting ligands of TAMs; The superparamagnetic oxide nanoparticles form a nano-cluster structure through a disulfide bond; the nano-cluster structure encapsulates proteins. The traditional Chinese medicine-magnetic nanocluster chemoimmunopharmaceutical delivery system of the present invention integrates the targeting advantages of magnetic tendency, ligand modification, and reduction sensitivity, and is a traditional Chinese medicine chemoimmunopharmaceutical delivery system with stable internal circulation, efficient tumor aggregation, and precise targeting of TAMs system.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a traditional Chinese medicine-magnetic nano-cluster chemoimmunomedicine delivery system and a preparation method thereof. Background technique [0002] Tumor tissue is not simply aggregates of tumor cells. According to the classic "seed-soil" theory of oncology, tumor cells are "seeds" and the tumor microenvironment is "soil", which plays a decisive role in the occurrence, development, and metastasis of tumors. The tumor microenvironment mainly includes some immune cells (such as tumor-associated macrophages (TAMs), T cells, dendritic cells, etc.), tumor-associated fibroblasts (TAFs), extracellular matrix, cytokines, and chemokines. Among them, TAMs play a central role in regulating the breast cancer immune network. TAMs are a diverse cell population, mainly divided into the classically activated M1 type and the alternatively activated M2 type. The former can activate tumor...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/54A61K47/69A61K47/02A61K9/51A61K31/575A61K41/00A61K45/00A61K47/42A61P35/00
CPCA61K9/5169A61K31/575A61K41/00A61K45/00A61K47/02A61K47/549A61K47/6939A61P35/00
Inventor 瞿鼎陈彦刘玉萍黄萌萌刘聪燕
Owner JIANGSU PROVINCE INST OF TRADITIONAL CHINESE MEDICINE
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