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Multicomponent lipid complex system with controlled particle size and drug release by tumor microenvironment, its preparation method and application

A tumor microenvironment and composite system technology, applied in the field of multi-component lipid composite systems, to achieve the effects of optimizing efficiency, reducing toxic and side effects, and improving safety

Active Publication Date: 2019-04-09
JIANGSU PROVINCE INST OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Obviously, it is difficult for the nanocarriers currently under development or on the market to satisfy the efficient accumulation and deep penetration of active ingredients in tumor tissues. Anti-tumor nano-preparation with synergistic effect and reduced toxicity

Method used

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  • Multicomponent lipid complex system with controlled particle size and drug release by tumor microenvironment, its preparation method and application
  • Multicomponent lipid complex system with controlled particle size and drug release by tumor microenvironment, its preparation method and application
  • Multicomponent lipid complex system with controlled particle size and drug release by tumor microenvironment, its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051]Example 1, the preparation scheme of the sensitive lipid complex system (TC-L) embedding coix seed oil-tripteryglide microemulsion and tanshinone 2A sulfonate sodium:

[0052] Take coix seed oil, RH40, PEG400 and tripterygne in mass ratio (20 / 20 / 5 / 2), stir at room temperature for 5 hours until completely mixed, slowly inject 10 times the total equivalent of water under high-speed stirring; take PEG-FsP- Octadecanol, DOPA, cholesterol (2 / 20 / 5), dissolved in an organic solvent, prepared into a sensitive lipid film, and the residual organic solvent was removed under reduced pressure for 24 hours; The aqueous phase of milk and sodium tanshinone 2A sulfonate (tripterylide / tanshinone 2A sodium sulfonate=1 / 3) was added to the lipid film (tripterylide / lipid=1 / 20), and hydrated at room temperature for 0.5 h, after ultrasonic pulverization at 10% power for 5 min, the lipid complex system was prepared.

[0053] Similarly, the anti-tumor microparticles were replaced with one of zed...

Embodiment 2

[0054] Example 2, the preparation scheme of the sensitive lipid complex system (TS-L) embedding coix seed oil-tripteryglide microemulsion and schisandrin A:

[0055] Take coix seed oil, RH40, PEG400 and tripterygne in mass ratio (20 / 20 / 5 / 2), stir at room temperature for 5 hours until completely mixed, slowly inject 10 times the total equivalent of water under high-speed stirring; take PEG-FsP- Octadecanol, DOPA, cholesterol (2 / 20 / 5), dissolved in an organic solvent, prepared into a sensitive lipid film, and the residual organic solvent was removed under reduced pressure for 24 hours; Add the aqueous phase of milk and schisandrin (triptolide / schisandrin=1 / 3) to the lipid film (triptolide / lipid=1 / 20), hydrate at room temperature for 0.5h, power 10 % after ultrasonic pulverization for 5 min, the lipid complex system was prepared.

[0056] Similarly, the anti-tumor microparticles were replaced with one of zedoary oil, javanica oil, linseed oil, nepeta oil, atractylodes oil or clo...

Embodiment 3

[0057] Example 3, the preparation scheme of the sensitive lipid complex system (TG-L) embedding coix seed oil-tripteryglide microemulsion and ginsenoside Rh2:

[0058] Take coix seed oil, RH40, PEG400 and tripterygne in mass ratio (20 / 20 / 5 / 2), stir at room temperature for 5 hours until completely mixed, slowly inject 10 times the total equivalent of water under high-speed stirring; take PEG-FsP- Octadecanol, DOPA, cholesterol (2 / 20 / 5), dissolved in an organic solvent, prepared into a sensitive lipid film, and the residual organic solvent was removed under reduced pressure for 24 hours; The aqueous phase of milk and ginsenoside Rh2 (tripterylide / ginsenoside Rh2=1 / 3) was added to the lipid film (tripteryline / lipid=1 / 20), hydrated at room temperature for 0.5h, power 10 % after ultrasonic pulverization for 5 min, the lipid complex system was prepared.

[0059] Similarly, the anti-tumor microparticles were replaced with one of zedoary oil, javanica oil, linseed oil, nepeta oil, at...

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Abstract

The present invention takes the anti-tumor microemulsion as the core, and co-encapsulates the microemulsion and certain active drugs in liposomes with the help of lipid materials sensitive to the tumor microenvironment, and the formed lipid complex system can Realize the change in size and the gradual release of drugs, transport different types of drugs to different parts, make the core part complete deeper tumor penetration, and finally release anti-tumor components in tumor cells to exert synergistic anti-tumor drug effects.

Description

technical field [0001] The invention relates to a multi-component lipid complex system whose particle size and drug release are controlled by the tumor microenvironment, its preparation method and its application in pharmacy. Background technique [0002] Anti-tumor nano-preparations can significantly reduce the toxicity of treatment, and in recent years, they have gradually replaced traditional preparations and become the first choice in clinical practice. However, commercially available nano-preparations have not really improved the survival of patients. There are two main reasons: 1. The "natural contradiction" between the aggregation and penetration efficiency of anti-tumor nano-preparations restricts the anti-tumor efficacy; Synergistic treatment efficiency between divisions. [0003] Generally speaking, the particle size is the most critical factor that determines whether it can efficiently accumulate and penetrate in tumor tissue: nanoparticles with larger particle ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K9/107A61K45/06A61K36/8994A61K31/56A61K31/09A61K31/704A61K31/58A61K47/24A61K47/42A61P35/00
CPCA61K9/0002A61K9/1075A61K9/1272A61K31/09A61K31/56A61K31/58A61K31/704A61K36/8994A61K45/06A61K47/24A61K47/42A61K2300/00
Inventor 陈彦瞿鼎黄萌萌刘玉萍
Owner JIANGSU PROVINCE INST OF TRADITIONAL CHINESE MEDICINE
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