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Amphiphilic nano-medicine and its preparation method and application

A nano-drug, amphiphilic technology, applied in nano-drugs, drug combinations, nano-technology, etc., can solve problems such as affecting drug efficacy, and achieve the effects of easy repeatability and characterization, strong hydrophobicity, and low bioavailability

Inactive Publication Date: 2020-05-08
CHONGQING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Reduction, interruption or withdrawal of sorafenib treatment may affect the efficacy of the drug

Method used

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  • Amphiphilic nano-medicine and its preparation method and application
  • Amphiphilic nano-medicine and its preparation method and application
  • Amphiphilic nano-medicine and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] The cleavable disulfide bond was connected to the amino-functionalized PEG through Michael addition reaction to prepare a terminal-functionalized and amphiphilic PEG molecule (compound I). The specific route is as follows:

[0029]

[0030] Then compound I is reacted with Sorafenib a part amide hydrogen to obtain the final compound SCNS, the specific route is as follows:

[0031]

[0032] The results of the compound SCNS hydrogen spectrum are as follows figure 1 shown. The results showed that: after Michael addition reaction, Sorafenib was successfully connected to PEG.

Embodiment 2

[0034] The water solubility of the SCNS synthesized in Example 1 was compared with that of Sorafenib, and the results are shown in Table 1.

[0035] Table 1. Comparison of water solubility of SCNS and Sorafenib

[0036]

[0037]

[0038] The results showed that Sorafenib was almost completely insoluble in water, while the improved compound SCNS had good water solubility.

Embodiment 3

[0040] The morphology of SCNS in aqueous solution was measured for particle size, the results are as follows figure 2 shown. Experimental results show that the obtained compound forms nanoparticles of about 200nm in water solubility, which is beneficial for entering cells and intravenous administration.

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Abstract

The invention relates to an amphipathic nano-medicine, as well as a preparation method and application thereof. The nano-medicine with good amphipathic performance can be improved by bonding an amphipathic group to the structure of a hydrophobic drug, and by taking sorafenib as an example, the modified sorafenib has good amphipathic performance. The method provides a new thought for hydrophobic drug modification, which aims at improving the medicine utilization and reducing the side effect while the curative effect is not reduced, and has an important meaning for target treatment of tumors.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, relates to amphiphilic nano-medicine, and also relates to a preparation method and application of the amphiphilic nano-medicine. Background technique [0002] With the improvement of people's living standards, health problems have become increasingly prominent. Cancer is one of the major diseases that currently affect human health and threaten human life. Therefore, the World Health Organization and the health departments of various countries regard conquering cancer as a top priority. At present, there are three main methods to treat cancer: one is surgical treatment, which is also the oldest cancer treatment method, that is, surgical resection is used to remove cancerous tissue and prevent the spread of cancer cells. The second is to use chemotherapy or radiotherapy, and the third is drug treatment. The method of surgical resection is relatively traumatic to the human body, leading to a de...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/60A61K31/17A61K31/337A61K31/4745A61K31/585A61K31/704A61K31/7068A61P35/00B82Y5/00A61K31/44
CPCA61K31/17A61K31/337A61K31/44A61K31/4745A61K31/585A61K31/704A61K31/7068B82Y5/00
Inventor 冯旭利汤嘉堃
Owner CHONGQING UNIV
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