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Preparation method of double-target modified liposome

A technology of liposome and blank liposome, which is applied in the research and development of targeted tumor drugs, can solve the problems of normal tissue damage, no targeted modification, and low targeting efficiency, and achieve liver cancer cell inhibition, simple operation, and high connection efficiency high effect

Inactive Publication Date: 2019-10-29
高志芹
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] It can be seen from the above that the liposome preparations currently on the market are all traditional liposomes, without targeting modification, and the targeted cells are passively targeted, the targeting efficiency is low, and it is easy to cause damage to normal tissues
In addition, the current basic research is mostly single-target modified liposomes, which are inaccurate, low in targeting efficiency, and easy to cause damage to normal tissues.

Method used

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  • Preparation method of double-target modified liposome
  • Preparation method of double-target modified liposome
  • Preparation method of double-target modified liposome

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Embodiment Construction

[0037] The preparation method of double-target modified liposome of the present invention comprises the following steps:

[0038] Step 1) Link target molecules to phospholipid molecules, including glycyrrhetinic acid and peanut lectin, and obtain DSPE-PEG after linking 2000 -GA and DSPE-PEG 2000 -PNA;

[0039] Step 2) Take the DSPE-PEG obtained in step 1) 2000 -GA and DSPE-PEG 2000 -PNA, dissolved in chloroform with soybean phospholipids and cholesterol, and prepared blank liposomes by film dispersion method;

[0040] Step 3) Take the blank liposome obtained in step 2), and prepare the drug-loaded liposome by ammonium sulfate gradient method.

[0041] The connection of glycyrrhetinic acid in step 1) specifically includes the following process: take 0.1g of DSPE-PEG 2000 -NH 2 Dissolve in 2 mL of chloroform, add 0.11 g of glycyrrhetinic acid, 0.11 g of EDC and 0.055 g of DMAP, stir at room temperature for 24 hours, wash with pure water 2-4 times, collect the organic phase...

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Abstract

The invention relates to a preparation method of a double-target modified liposome. The preparation method includes the steps that (1) target molecules are respectively connected to phospholipid molecules, target molecules include glycyrrhetinic acid and peanut agglutinin, and DSPE-PEG<2000>-GA and DSPE-PEG<2000>-PNA are obtained after connection; the DSPE-PEG<2000>-GA and the DSPE-PEG<2000>-PNA obtained in the step (1) are taken and dissolved in chloroform with soybean phospholipid and cholesterol, and a blank liposome is prepared by adopting a thin film dispersion method; and (3) the obtained blank liposome in the step (2) is taken, and a drug carrying liposome is prepared by adopting an ammonium sulfate gradient method. According to the preparation method, the target molecules are firstly connected to phospholipid and added with the soybean phospholipid and the cholesterol when the liposome is prepared, the connection efficiency is high, operation is convenient, and transformation is facilitated; and the two-target modified liposome obtained by the preparation method improves the targeting efficiency, and has obvious inhibitory effect on liver cancer cells.

Description

technical field [0001] The invention relates to the field of research and development of targeted tumor drugs, in particular to a method for preparing double-target modified liposomes. Background technique [0002] Cancer is a major disease that threatens human health, and liver cancer is the fourth leading cause of death after lung cancer, colorectal cancer and gastric cancer. Hepatocellular carcinoma (Hepatocellular carcinoma HCC) has a high incidence rate, accounting for about 90% of primary liver cancers worldwide, and is one of the major cancers that threaten human life and health. Drugs have low selectivity to tumors and are prone to multi-drug resistance. The current conventional methods of cancer treatment include surgery, radiotherapy and chemotherapy, all of which have many disadvantages. Targeted drug delivery brings new hope to cancer treatment. [0003] Liposome is a double-layer artificial membrane formed by phospholipid molecules in the water phase. It can e...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/24A61K47/28A61K47/42A61K47/10A61K31/704A61P35/00
CPCA61K9/127A61K47/24A61K47/28A61K47/42A61K47/10A61K31/704A61P35/00
Inventor 李肖成刁文彬薛晗韬武敬亮于文静曲梅花高志芹
Owner 高志芹
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