Preparation method of polyethylene glycol modified nano-micelle or vesicle with pH (potential of hydrogen) responsivity and high drug loading capacity

A polyethylene glycol and high drug-loading technology, which is applied in the fields of polymer materials and biomedical engineering, can solve the problems of no targeting effect and large lethality of normal cells, and achieve increased drug loading, improved release, The effect of improving efficiency

Active Publication Date: 2018-05-29
TONGJI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Most of the traditional anti-tumor drugs are non-selective drugs and do not have a targeting effect, so in most cases they have a greater lethality to normal cells

Method used

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  • Preparation method of polyethylene glycol modified nano-micelle or vesicle with pH (potential of hydrogen) responsivity and high drug loading capacity
  • Preparation method of polyethylene glycol modified nano-micelle or vesicle with pH (potential of hydrogen) responsivity and high drug loading capacity
  • Preparation method of polyethylene glycol modified nano-micelle or vesicle with pH (potential of hydrogen) responsivity and high drug loading capacity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Dissolve 0.75 g of polyethylene glycol monomethyl ether with a molecular weight of 750 and 0.12 g of succinic anhydride in 30 ml of tetrahydrofuran, reflux at 75°C for 12 hours, precipitate with ether for 3 times, filter, and vacuum-dry the filter cake to constant weight to obtain carboxyl-terminated Modified polyethylene glycol: 34.0 mg of pentaerythritol, 0.13 g of 4-dimethylaminopyridine and 0.61 g of dicyclohexylcarbodiimide were dissolved in 10 ml of dichloromethane to form a pentaerythritol solution, and the carboxyl-modified polyethylene glycol Dissolve 0.75g of alcohol in 10ml of dichloromethane, add it dropwise to the pentaerythritol solution at a very slow speed, stir thoroughly for 2 days, precipitate with ether for 3 times, filter, and vacuum dry the filter cake to obtain a trihydroxy-modified polyethylene glycol Alcohol; 50 mg of doxorubicin hydrochloride was dissolved in 10 ml of deionized water to form an aqueous solution, 50 mg of cis-aconitic anhydride w...

Embodiment 2

[0028]Dissolve 1.0 g of polyethylene glycol monomethyl ether with a molecular weight of 1000 and 0.16 g of succinic anhydride in 30 ml of tetrahydrofuran, reflux at 75°C for 12 hours, precipitate with methanol for 3 times, filter, and vacuum-dry the filter cake to constant weight to obtain carboxyl-terminated Modified polyethylene glycol: 34.0 mg of pentaerythritol, 0.13 g of 4-dimethylaminopyridine and 0.61 g of dicyclohexylcarbodiimide were dissolved in 10 ml of chloroform to form a pentaerythritol solution, and the carboxyl-modified polyethylene glycol Dissolve 1.0 g of alcohol in 10 ml of chloroform, add it dropwise to the pentaerythritol solution at a very slow speed, stir thoroughly for 2 days, precipitate with ether for 3 times, filter, and vacuum dry the filter cake to obtain a trihydroxy-modified polyethylene glycol alcohol; 50.0 mg of doxorubicin hydrochloride was dissolved in 10 ml deionized water to form an aqueous solution, 50.0 mg of cis-aconitic anhydride was dis...

Embodiment 3

[0031] Dissolve 2.0 g of polyethylene glycol monomethyl ether with a molecular weight of 2000 and 0.16 g of succinic anhydride in 30 ml of tetrahydrofuran, reflux at 75°C for 12 hours, precipitate with n-hexane for 3 times, filter, and vacuum-dry the filter cake to constant weight to obtain terminal Carboxy-modified polyethylene glycol; 34.0 mg of pentaerythritol, 0.13 g of 4-dimethylaminopyridine and 0.61 g of dicyclohexylcarbodiimide are dissolved in 10 ml of dimethylformamide to form a pentaerythritol solution. Dissolve 0.75 g of polyethylene glycol in 10 ml of dimethylformamide, add dropwise to the pentaerythritol solution at a very slow speed, stir thoroughly for 2 days, precipitate with n-hexane for 3 times, filter, and vacuum-dry the filter cake to obtain a constant weight. Hydroxy-modified polyethylene glycol; 50.0 mg of doxorubicin hydrochloride was dissolved in 10 ml of deionized water to make an aqueous solution, 50.0 mg of cis-aconitic anhydride was dissolved in 10 ...

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Abstract

The invention belongs to the field of high polymer materials and biomedical engineering and particularly relates to a preparation method of a polyethylene glycol modified nano-micelle or a vesicle with pH (potential of hydrogen) responsivity and high drug loading capacity. The method comprises the steps of allowing polyethylene glycol and cis-aconitic acid anhydride modified doxorubicin to give areaction to generate an amphipathic segmented copolymer, and obtaining the nano-micelle or the vesicle with the pH responsivity and the high drug loading capacity by taking an anticancer drug, namelydoxorubicin as a hydrophobic chain segment and polyethylene glycol as a hydrophilic chain segment. The nano-micelle or the vesicle takes the anticancer drug as the hydrophobic chain segment, and therefore, has the higher drug loading capacity; at the same time, cis-aconitic acid anhydride is sensitive to acid; and therefore, the prepared nano-micelle or the vesicle has the pH responsivity, is applicable to the field of tumor therapy, can improve chemotherapy efficiency and reduces toxic and side effects of the anticancer drug on normal tissues.

Description

technical field [0001] The invention belongs to the fields of polymer materials and biomedical engineering, and in particular relates to a method for preparing polyethylene glycol-modified nano-micelles or vesicles with pH responsiveness and high drug loading. Background technique [0002] Polyethylene glycol (PEG) is a biocompatible polymer with good water solubility, non-toxic, non-irritating, and low immunogenicity. It can be excreted through the kidneys and will not accumulate in the body. Widely used in the field of biomedicine. [0003] Because polyethylene glycol has good blood compatibility, it is often used in drug release carriers, surface modification of biological materials, tissue engineering materials, etc. When the amphiphilic block copolymer prepared with polyethylene glycol as a raw material is used as a drug carrier, it has no pharmacological effect itself, and the drug can be wrapped into the polymer through self-assembly or linked with a covalent bond to...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K9/127A61K47/60A61K47/54A61K31/704A61P35/00
CPCA61K9/1075A61K9/1273A61K31/704
Inventor 李建波冒诗楠
Owner TONGJI UNIV
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