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A cu (ddc) 2 Nano core liposome and its preparation method and application

A nano-nucleus and liposome technology, which is applied in the field of medicine, can solve the problems of insignificant solubilization effect of surfactants, difficult preparation of physical and chemical properties, and poor fat solubility, so as to achieve reduced dosage, strong anti-tumor activity, and encapsulation high rate effect

Active Publication Date: 2022-02-01
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But Cu(DDC) 2 The water solubility is extremely poor, the solubility is less than 1μg / mL, and the solubilization effect of surfactant is not significant. In addition, Cu(DDC) 2 The fat solubility is also poor, this Cu(DDC) 2 The physical and chemical properties of it bring great difficulties to its preparation

Method used

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  • A cu (ddc) <sub>2</sub> Nano core liposome and its preparation method and application
  • A cu (ddc) <sub>2</sub> Nano core liposome and its preparation method and application
  • A cu (ddc) <sub>2</sub> Nano core liposome and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] A Cu(DDC) 2 Nano core liposome preparation, its preparation method step is as follows:

[0065] (1) DOPA-coated Cu(DDC) 2 Preparation of nanoparticles

[0066] 150 μL 500 mM CuCl 2 The aqueous solution was added to the mixed solution (70:30, V:V) of 8ml cyclohexane and Igepal CO-520 to prepare CuCl 2 Inverse microemulsion, 150 μL 500 mM sodium diethyldithiocarbamate (DDTC) aqueous solution, 320 μL 20 mg / ml DOPA chloroform solution was added to 8 ml cyclohexane and IgepalCO-520 mixed solution (70:30, V:V) to prepare two Sodium dithiocarbamate (DDTC) reverse phase microemulsion, CuCl 2 Add the inverse microemulsion dropwise into sodium diethyldithiocarbamate (DDTC) inverse microemulsion and stir for 24 hours, add 16ml of isopropanol to break the emulsion, and collect by centrifugation at 17500g / 30min to obtain DOPA-Cu(DDC) 2 nanoparticles. Use isopropanol to wash the excess cyclohexane and surfactant on the surface, N 2 Blow dry the isopropanol.

[0067] (2) Cu(DD...

Embodiment 2

[0086]A Cu(DDC) 2 Nano core liposome preparation, its preparation method step is as follows:

[0087] (1) DOPA-coated Cu(DDC) 2 Preparation of nanoparticles

[0088] 150 μL 500 mM CuCl 2 The aqueous solution was added to the mixed solution (70:30, V:V) of 8ml cyclohexane and Igepal CO-520 to prepare CuCl 2 Reverse microemulsion, 150 μL 500mM sodium diethyldithiocarbamate (DDTC) aqueous solution, 200 μL 20mg / ml DOPA chloroform solution was added to 8ml cyclohexane and IgepalCO-520 mixed solution (70:30, V:V) to prepare two Sodium dithiocarbamate (DDTC) reverse phase microemulsion, CuCl 2 Add the inverse microemulsion dropwise into sodium diethyldithiocarbamate (DDTC) inverse microemulsion and stir for 24 hours, add 16ml of isopropanol to break the emulsion, and collect by centrifugation at 17500g / 30min to obtain DOPA-Cu(DDC) 2 nanoparticles. Use isopropanol to wash the excess cyclohexane and surfactant on the surface, N 2 Blow dry the isopropanol.

[0089] (2) Cu(DDC) ...

Embodiment 3

[0092] A Cu(DDC) 2 Nano core liposome preparation, its preparation method step is as follows:

[0093] (1) DOPA-coated Cu(DDC) 2 Preparation of nanoparticles

[0094] 150 μL 400 mM CuCl 2 The aqueous solution was added to the mixed solution (70:30, V:V) of 8ml cyclohexane and Igepal CO-520 to prepare CuCl 2 Inverse microemulsion, 150 μL 400mM sodium diethyldithiocarbamate (DDTC) aqueous solution, 320 μL 20mg / ml DOPA chloroform solution was added to 8ml cyclohexane and IgepalCO-520 mixed solution (70:30, V:V) to prepare two Sodium dithiocarbamate (DDTC) reverse phase microemulsion, CuCl 2 Add the inverse microemulsion dropwise into sodium diethyldithiocarbamate (DDTC) inverse microemulsion and stir for 24 hours, add 16ml of isopropanol to break the emulsion, and collect by centrifugation at 17500g / 30min to obtain DOPA-Cu(DDC) 2 nanoparticles. Use isopropanol to wash the excess cyclohexane and surfactant on the surface, N 2 Blow dry the isopropanol.

[0095] (2) Cu(DDC) ...

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Abstract

The invention belongs to the technical field of medicine and relates to a Cu(DDC) 2 Nano-core liposome and its preparation method and application, specifically related to Cu(DDC) 2 Nano core liposome, its preparation method and its application in the preparation of medicine for treating liver cancer. The Cu(DDC) 2 Nanonuclear liposomes contain Cu(DDC) as an inner layer 2 Nanoparticles and the outer layer of phospholipids. The Cu(DDC) 2 Nanoparticles contain: CuCl 2 , sodium diethyldithiocarbamate (DDTC), and phospholipids, the weight ratio of each component is: (12‑51): (17‑68): (10‑20). The phospholipid layer comprises cholesterol, DSPE‑PEG 2000 , Phospholipids, Phospholipids, Cholesterol, DSPE‑PEG 2000 The mass ratio of is: (10‑20): (5‑10): (18‑42). The present invention prepares Cu(DDC) coated with phospholipids in the inner layer by reverse phase microemulsion polymerization 2 Nanoparticles, further by membrane hydration, encapsulate the outer layer of phospholipids. Cu(DDC) of the present invention 2 Nano-nuclear liposomes can significantly prolong the circulation time of drugs in the body and increase Cu(DDC) 2 antitumor effect.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to a Cu(DDC) 2 Nano-core liposome and its preparation method and application, specifically related to Cu(DDC) 2 Nano core liposome, its preparation method and its application in the preparation of medicine for treating liver cancer. Background technique [0002] Primary liver cancer is a multiple tumor disease. Malignant tumors that occur on stem cells or bile duct cells of patients have a very high incidence rate, ranking the top six in cancer incidence, ranking fourth in incidence rate and third in mortality rate in my country, and have a great impact on human life and health , and frequently occurs, so it has certain harmfulness and seriously threatens people's life and health. [0003] In terms of treatment methods, patients with early primary liver cancer tend to adopt surgical treatment, and the 5-year survival rate after surgery is 50% to 70%, but the tumor recurrence and met...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K47/24A61K31/555A61P35/00
CPCA61K9/127A61K9/1277A61K47/24A61K9/0019A61K31/555A61P35/00
Inventor 张宇尹湉何海冰苟靖欣唐星孔艺涵
Owner SHENYANG PHARMA UNIVERSITY
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