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PEGylated dendrimer drug carrier and preparation method thereof

A macromolecular and dendritic technology, which is applied in the field of PEGylated dendritic macromolecular drug carrier and its preparation, can solve the problems of increasing hydrophobic drugs, complicated preparation process, limited application prospect, etc., and achieves easy reaction, single molecular weight distribution, Efficient effect of synthetic method

Active Publication Date: 2021-08-24
惠州卫生职业技术学院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the particle size distribution of the polymer drug carrier structure is too wide, especially during the carrier formation process, when the polymer concentration is lower than the critical concentration, the dilution of the drug carrier itself will seriously affect its drug loading effect
Chinese patent CN106943601 A reports a carrier and a preparation method for improving protein bioavailability and water solubility of poorly soluble drugs, including the synthesis of polyethylene glycol-polybenzyl glutamate block copolymer, the synthesis of aminolysis products, and the synthesis of linear polybenzyl glutamate. Synthesis of ethylene glycol-brush polybenzyloxycarbonyl lysine block copolymer, synthesis of linear polyethylene glycol-brush polybenzyloxycarbonyl lysine and polylysine block copolymer; the advantage is to solve The bioavailability of protein drugs and the water solubility of insoluble drugs can be solved, so that a variety of injections can be prepared, which has the characteristics of improving protein bioavailability, increasing water solubility of hydrophobic drugs, reducing injection frequency, reducing the economic burden of clinical patients, and enhancing drug efficacy. , but its preparation process is complex and its application prospects are limited
[0006] At present, there is no research on acrylate-terminated and amino-terminated dendrimers, PEGylated acrylate-terminated and amino-terminated dendrimers to load insoluble anticancer drugs such as camptothecin and L-shikonin. Published reports and patent applications

Method used

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  • PEGylated dendrimer drug carrier and preparation method thereof
  • PEGylated dendrimer drug carrier and preparation method thereof
  • PEGylated dendrimer drug carrier and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Embodiment 1 is G2.0 (NH 2 ) Synthesis of 18

[0050] 1. Weigh 3.0g of TMPTA monomer, dissolve it in 2.4g of methanol, add 12g of ethylenediamine in an ice-water bath, stir and mix evenly in a 50mL three-necked bottle, raise the temperature to 45°C, and protect it under nitrogen The mixture was stirred and reacted for 18 hours, methanol and most of ethylenediamine were distilled off under reduced pressure, washed three times with 8 g, 6 g, and 6 g of ethyl acetate respectively, and vacuum-dried at 30°C to obtain G1.0 (NH 2 ) 3, its HPLC test result is as figure 1 as shown in a.

[0051] 2. Weigh G1.0 (NH 2 0.5 g of )3 dendrimers were dissolved in 4.0 g of methanol, and then 12.0 g of TMPTA was added, and stirred and reacted at 25° C. for 18 h. First, methanol and most of ethylenediamine were distilled off under reduced pressure, then washed three times with 8g, 6g, and 6g of ethyl acetate respectively, and dried in vacuum at 30°C to obtain G1.5 (acrylate) 18. The HP...

Embodiment 2

[0053] Example 2 The amino-terminated dendrimer with ethylenediamine as the core is G2.0 (NH 2 ) Synthesis of 18

[0054] Prepare G2.0 (NH 2 )18, the difference is:

[0055] In step 1, the mass ratio of TMPTA, ethylenediamine and organic solvent is 6:3:5, the reaction temperature is 60° C., and the reaction time is 10 h.

[0056] In step 2, G1.0(NH 2 ) 3. The mass ratio of TMPTA to the organic solvent is 0.1:2:0.5, the reaction temperature is 30°C, and the reaction time is 30h.

[0057] In step 3, the mass ratio of G1.5(acrylate)18, ethylenediamine and organic solvent is 0.6:10:1, the reaction temperature is 40° C., and the reaction time is 10 h.

Embodiment 3

[0058] Example 3 The amino-terminated dendrimer with ethylenediamine as the core is G2.0 (NH 2 ) Synthesis of 18

[0059] Prepare G2.0 (NH 2 )18, the difference is:

[0060] In step 1, the mass ratio of TMPTA, ethylenediamine and organic solvent is 2:10:1, the reaction temperature is 30°C, and the reaction time is 15h.

[0061] In step 2, G1.0(NH 2 ) 3. The mass ratio of TMPTA and organic solvent is 0.5:25:2, the reaction temperature is 40°C, and the reaction time is 45h.

[0062] In step 3, the mass ratio of G1.5(acrylate)18, ethylenediamine and organic solvent is 0.3:5:0.6, the reaction temperature is 30°C, and the reaction time is 15h.

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Abstract

The present invention relates to a preparation method of PEGylated dendrimer drug carrier: mixing trimethylolpropane triacrylate and ethylenediamine in an ice-water bath, and reacting alternately in an organic solvent under a protective atmosphere, the reaction temperature is 25-60°C, to obtain amino-terminated dendrimers with ethylenediamine as the core or acrylate-terminated dendrimers with trimethylolpropane triacrylate as the core; PEG, p-nitrophenyl chloride Formate and triethylamine are dissolved in an organic solvent, and then reacted at 20-30°C to obtain PEGylated p-nitrophenyl carbonate after the reaction is complete; The acrylate-terminated dendrimer with trimethylolpropane triacrylate as the core reacts with PEGylated p-nitrophenyl carbonate in an organic solvent at a reaction temperature of 20-30°C. The method of the invention is easy to operate, high in yield and low in cost, and the prepared drug carrier has excellent drug-loading performance for drugs hardly soluble in water.

Description

technical field [0001] The invention relates to the technical field of dendritic macromolecule synthesis technology and drug carrier, in particular to a PEGylated dendritic macromolecule drug carrier and a preparation method thereof. Background technique [0002] In recent years, the use of nano drug delivery systems (NDDSs) to enhance the efficacy of anticancer drugs in vivo has been recognized by more and more researchers, making it a new type of drug delivery system. NDDSs can increase the permeability of biomembrane and the solubility of fat-soluble drugs, which not only has the advantages of good stability, targeted delivery of drugs to tumor sites and slow release, but also reduces the dosage, frequency of administration, and harm to other organs. device damage, broad application prospects. There are various types of NDDSs nanocarriers, including liposomes, polymer nanoparticles, polymer micelles, carbon nanotubes, solid lipid nanoparticles, vesicles, and dendrimers. ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08G81/00A61K47/60
CPCA61K47/60C08G81/00
Inventor 吁诚铭陈燕
Owner 惠州卫生职业技术学院
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