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

Anti-tumor predrug by taking novel amphipathic dendritic macromolecules as carriers based on malic acid as branching unit and preparation method thereof

A branched unit and dendritic technology, applied in the field of anti-tumor prodrugs and preparation, achieves the effects of low biological toxicity, improved hydrophilicity, and avoided toxic and side effects

Inactive Publication Date: 2010-01-06
XIANGTAN UNIV
View PDF1 Cites 3 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The prodrug is amphiphilic and can be made into a water-based preparation, which overcomes the shortcomings of the existing paclitaxel preparations such as poor water solubility and severe allergic reactions

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

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Anti-tumor predrug by taking novel amphipathic dendritic macromolecules as carriers based on malic acid as branching unit and preparation method thereof
  • Anti-tumor predrug by taking novel amphipathic dendritic macromolecules as carriers based on malic acid as branching unit and preparation method thereof
  • Anti-tumor predrug by taking novel amphipathic dendritic macromolecules as carriers based on malic acid as branching unit and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Example 1: Preparation of amphiphilic dendrimer paclitaxel prodrug containing glycolic acid oligomer

[0031] 1. Carboxylation of Polyethylene Glycol Monomethyl Ether

[0032]In a 100ml three-necked flask equipped with a reflux condensing device and a magnetic stirrer, under gas protection, add 5g of polyethylene glycol monomethyl ether and 1g of pre-weighed succinic anhydride, and an equimolar amount of 4,4' -Dimethylaminopyridine, add 60ml of refined tetrahydrofuran, reflux reaction. After the reaction was completed, the solvent was concentrated, and then the residue was dissolved in an aqueous alkali solution, the organic phase was discarded, the aqueous phase was acidified with acid, and the pH value of the solution was adjusted to acidic, then the aqueous layer was washed three times with ethyl acetate, and the ethyl acetate solution was combined Wash twice with saturated sodium chloride solution, add anhydrous magnesium sulfate to dry, then filter the desiccant, ...

Embodiment 2

[0043] Example 2: Preparation of amphiphilic dendrimer paclitaxel prodrug containing lactic acid oligomer

[0044] 1. Preparation of lactic acid oligomers with terminal hydroxyl groups replaced by bromine (taking pentamer as an example)

[0045] Add 5g of lactic acid and 100ml of anhydrous tetrahydrofuran into a 250ml single-necked flask. After completely dissolving, add an equimolar alkali to form a salt, then add 11.50g of tert-butyl 2-bromopropionate and a catalyst, and reflux the reaction. After the reaction was completed, it was separated by column chromatography to obtain 9.5 g of a colorless transparent liquid (glycolic acid dimer with carboxyl protected by tert-butyl group). Take 5g of this lactic acid dimer, 3.52g of 2-bromopropionic acid, and add dichloromethane into a 250ml single-necked flask, stir, and after completely dissolving, add 4.80g of dicyclohexylcarbodiimide, with a catalytic amount of 4,4'- Dimethylaminopyridine, ice-bath reaction, the reaction is over...

Embodiment 3

[0051] Example 3: Preparation of amphiphilic dendrimer camptothecin prodrug containing glycolic acid oligomer

[0052] In a 100ml round bottom flask, add 0.5g of amphiphilic dendrimers containing glycolic acid oligomers, camptothecin in an equal carboxyl molar amount, and 50ml of anhydrous dichloromethane. After stirring and dissolving, add 0.18g of dicyclohexyl carbon Diimine, catalytic amount of 4,4'-dimethylaminopyridine, reaction in ice bath, after the reaction is over, filter to remove the precipitate in the reaction system, concentrate dichloromethane by rotary evaporation, and then drop it into a large amount of anhydrous ether to precipitate , freeze and stand still, and suction filter to obtain a biodegradable amphiphilic dendrimer loaded with camptothecin.

[0053] Other steps are the same as in Example 1.

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 provides an anti-tumor predrug by taking novel amphipathic dendritic macromolecules as carriers based on malic acid as a branching unit and a preparation method thereof. The novel amphipathic dendritic macromolecules that are biodegradable are constructed based on malic acid and glycolic acid oligomer, lactic acid oligomer, amino acid oligomer, alternation and copolymerization oligomer of all as well as polyethylene glycol or polyethylene glycol monomethyl ether; and the amphipathic dendritic macromolecules are in bonding reaction with anti-tumor medicines under the existence of a condensing agent, thereby obtaining the predrug of the anti-tumor medicines. The anti-tumor predrug improves the biocompatibility of medicinal carrier materials better, regulates and controls the degradation speed of the medicinal carrier materials in the human body by regulating the polymerization degree and the chemical compositions of oligomer simultaneously, realizes the regulation and control functions to release speed of medicines, has better medicinal slowly-controlled release function and avoids causing toxic and side effects to normal cells due to burst release of anti-tumor medicines.

Description

Technical field: [0001] The invention relates to a novel amphiphilic dendritic macromolecule-carrier antitumor prodrug and a preparation method thereof. technical background: [0002] In recent years, with the emergence of many new performance polymer materials and the rapid development of the pharmaceutical preparation industry, polymer carriers have been more and more widely used in the research and development of new drugs. Polymer prodrugs refer to the use of polymers that do not have pharmacological effects and do not react chemically with drugs as drug carriers, relying on weak hydrogen bonds between the two to form, or linking drugs to polymers through polycondensation reactions. A class of polymers obtained. The use of polymer materials as drug carriers needs to achieve the following goals: ① prolong the action time of drugs; ② improve the selectivity of drugs; ③ reduce the toxic and side effects of drugs; ④ increase the absorption of drugs in the body; With the de...

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): A61K47/48A61P35/00A61K47/59
Inventor 张雪飞张英伟王海波钟冠群张海良
Owner XIANGTAN 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