Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Non-virogene carrier for complexation platinum series antineoplastic medicament and preparing method thereof

An anti-tumor drug, non-viral technology, used in anti-tumor drugs, drug combinations, pharmaceutical formulations, etc., can solve problems such as toxic degradability, no transfection efficiency, etc., to reduce toxicity, reduce drug immunogenicity, and water solubility. Good results

Inactive Publication Date: 2008-10-29
ZHEJIANG UNIV
View PDF0 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Non-viral gene carriers have problems such as toxicity, biocompatibility, and degradability. At present, there is a synthetic material polyethyleneimine. Experiments have found that polyethyleneimine with a molecular weight of 22000-25000 has a very high transfection efficiency, but it is toxic. And the problem of degradability, polyethyleneimine with small molecular weight (600, 1200, 2000) has low toxicity and is easy to metabolize in vivo, but has almost no transfection efficiency

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1: PtCl 4 -Synthesis of PEI600-PEG3400 complex (numbers such as 600, 3400 indicate the molecular weight of the corresponding raw materials, the same below).

[0029] 1) PtCl 4 -Synthesis of PEI600 complex

[0030] 0.2mmolPtCl 4and 0.2mmolPEI600 were dissolved in 5mL of absolute ethanol, and the PtCl 4 The ethanol solution was slowly dropped into the PEI600 ethanol solution, and the stirring reaction was continued for 1 h to obtain PtCl 4 - suspension of PEI600 complex. Filter, and collect the solid after natural evaporation to dryness.

[0031] 2) PtCl 4 -PEGylation of PEI600 complexes

[0032] The above prepared PtCl 4 All solids of the -PEI600 complex are dissolved in 30mL of dichloromethane, and can be slightly heated to increase its solubility. Then, under the condition of stirring, a dichloromethane solution of PEG3400 (0.01 mmol in amount) (the amount of dichloromethane is 1 mL) was slowly added therein, and the stirring reaction was continued for...

Embodiment 2

[0033] Example 2: PEG3400-PEI1200-PtCl 4 Synthesis of complexes.

[0034] 1) Synthesis of PEG3400-PEI1200 complex

[0035] Dissolve 0.2mmol PEI1200 in 10mL of dichloromethane, and 0.002mmol of PEG3400 in 0.4mL of dichloromethane. Slowly drop the PEG3400 dichloromethane solution into the PEI1200 dichloromethane solution under stirring conditions, and continue stirring for 1 hour to obtain PEG3400- PEI1200 complex solution.

[0036] 2) PEG3400-PEI1200-PtCl 4 Synthesis of complexes

[0037] 0.4mmol PtCl 4 Dissolve with 10mL absolute ethanol, under the condition of stirring, PtCl 4 Slowly drop the ethanol solution into the above-mentioned PEG3400-PEI1200 complex solution, continue stirring for 2 hours, and let stand until the dichloromethane and ethanol are evaporated to obtain a slightly viscous solid product, that is, PEG3400-PEI1200-PtCl 4 Complex.

Embodiment 3

[0038] Example 3: PtCl 2 (NH 3 ) 2 - Synthesis of PEI1200-PEG5000 complex.

[0039] 1) PtCl 2 (NH 3 ) 2 -Synthesis of PEI1200 complex

[0040] 0.6mmol cisplatin PtCl 2 (NH 3 ) 2 Dissolve with 20mL of absolute ethanol, 0.2mmolPEI1200 with 5mL of absolute ethanol, under the condition of stirring, the PtCl 2 (NH 3 ) 2 Slowly drop the ethanol solution into the PEI1200 ethanol solution, continue to stir and react for 3 hours to obtain PtCl 2 (NH 3 ) 2 - suspension of PEI1200 complex. Filter, and collect the solid after natural evaporation to dryness. 2) PtCl 2 (NH 3 ) 2 -PEGylation of PEI1200 complexes

[0041] The above prepared PtCl 2 (NH 3 ) 2 All the solids of the -PEI1200 complex are dissolved in 30mL of dichloromethane, and can be slightly heated to increase its solubility. Under the condition of stirring, the dichloromethane solution of PEG5000 (consumption 0.005mmol) (dichloromethane consumption 1mL) was slowly added therein, continued to stir and rea...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention relates to a non-viral gene drug carrier of a complexing platinum-based anti-tumor drug, which is the Pt-PEI-PEG or PEG-PEI-Pt complex carrier, PEI is taken as a framework to connect polyethylene glycol and complex the platinum anti-tumor drug for constitution; and the molar percentage of all the components of the complex are: Pt: 48.8 to 83.2 percent, PEI: 16.5 to 49.8 percent, PEG: 0.17 to 2.44 percent respectively. The preparation method is that the platinum compound and the PEI are carried out the coordination, the reaction with the PEG is further carried out, thus generating the Pt-PEI-PEG complex carrier; or the platinum compound and the PEG-PEI complex are carried out the coordination reaction, thus generating the PEG-PEI-Pt complex carrier. The non-viral gene drug carrier has the advantages of effects of the anti-tumor drug, high stability, good water solubility, long cycle in vivo and lowering toxicity.

Description

technical field [0001] The invention relates to a new type of non-viral gene drug carrier, in particular to a class of non-viral gene drug carrier complexed with platinum antitumor drugs. Background technique [0002] Tumor is a common and frequently-occurring disease that seriously threatens human health, and overcoming it has always been a research hotspot attracting worldwide attention. In 1995, the World Health Organization evaluated nearly 100 anti-tumor drugs in the world, and the comprehensive evaluation of cisplatin anti-tumor drugs ranked second in terms of efficacy and market. According to statistics, in my country's anti-tumor chemotherapy regimens, cisplatin-based or compatible anti-tumor drug regimens account for 70%-80% of all chemotherapy regimens. It can be seen that the efficacy of platinum antineoplastic drugs has been recognized by everyone. At present, there have been three generations of clinical drugs, of which the first generation: cisplatin; the seco...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K33/24A61K31/282A61K31/555A61P35/00A61K47/60
Inventor 赵璐汤谷平胡秀荣周峻
Owner ZHEJIANG UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com