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Gold nanoparticle-anthracene ring pharmaceutical composition and preparation method thereof

A technology of anthracyclines and conjugates, which is applied in the field of design and construction of gold nano-anthracycline drug conjugates, which can solve the problems of poor water solubility, large toxic and side effects, short half-life and short action time in vivo

Inactive Publication Date: 2015-06-10
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0002] In the past two decades, nano-drug delivery system has become a research hotspot in the field of pharmacy, which can well solve many problems in the clinical application of some drugs, such as poor water solubility, poor stability, low bioavailability, and in vivo half-life. and short action time, poor distribution in the body, and large toxic and side effects

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  • Gold nanoparticle-anthracene ring pharmaceutical composition and preparation method thereof
  • Gold nanoparticle-anthracene ring pharmaceutical composition and preparation method thereof
  • Gold nanoparticle-anthracene ring pharmaceutical composition and preparation method thereof

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preparation example Construction

[0035] The invention relates to the design and construction of a novel gold nano-anthracycline drug conjugate A-D-P, the preparation method of each constituent part of the conjugate, the preparation method of the conjugate, the release characteristics of the drug in vitro, and the drug delivery application. The preparation of the gold nano-anthracycline drug conjugate in the present invention comprises: (1) the preparation of the core of the gold nano-particle; (2) the synthesis of the anthracycline drug sulfhydryl biocompatible ligand; (3) the gold nano-anthracycline Preparation of drug-like conjugates.

[0036] The preparation method of the gold nanometer-anthracycline-hydrophilic polymer conjugate A-D-P uses gold nanometer as the core, dihydrolipoic acid as the connecting arm, doxorubicin as the loaded drug, and monomethoxypolyethylene glycol as the A gold nanometer-doxorubicin-monomethoxypolyethylene glycol conjugate prepared with biocompatible molecules is taken as an exa...

Embodiment 1

[0043] Example 1 Gold Nano-Adriamycin-Monomethoxypolyethylene Glycol Conjugate

[0044] 1. Synthesis of gold nanoparticles (A):

[0045] The glass instruments used were washed successively with aqua regia, distilled water and deionized water, and 50 mL (0.116 mol / L) trisodium citrate aqueous solution was prepared with deionized water, and 50 μL (2.5×10 -6 mol / L) chloroauric acid (HAuCl 4 ) mother liquor was added in the above-mentioned trisodium citrate solution, and under vigorous stirring, 5 mL (1 mg / mL) of frozen sodium borohydride solution was quickly added to the mixture solution, and the reaction solution became orange to purple, and the reaction temperature was kept at 0 °C, continue to stir vigorously for 15-20 minutes until the color no longer changes, then naturally warm up to room temperature, and a solution of gold nanoparticles with a size of 5nm is obtained.

[0046] 2. Synthesis of lipoic acid hydrazide-doxorubicin-monomethoxypolyethylene glycol:

[0047] The...

Embodiment 2

[0054] Example 2 Characterization of Physicochemical Properties of Conjugates

[0055] NMR: take a certain amount of doxorubicin ligand and the lyophilized conjugate and dissolve it in deuterated chloroform, TMS is used as a reference substance, and Bruker (Avace) AV-300AV-500 nuclear magnetic resonance instrument is used to measure and determine the hydrogen nuclear magnetic resonance spectrum;

[0056] Infrared: Take a certain amount of freeze-dried conjugate and disperse it in KBr, press it into tablets, and measure the infrared spectrum with a Bruker TENSOR infrared spectrometer;

[0057] UV: (1) Take freshly prepared sodium citrate-protected gold nanoparticle solution; (2) Precisely weigh a certain amount of lyophilized conjugate and dissolve it in ultrapure water to make a solution, dilute to an appropriate concentration, and use UV- 2401pc uv-vis (Shimadzu, Japan) ultraviolet spectrophotometer scans the ultraviolet absorption from 400 to 800nm;

[0058] Transmission e...

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Abstract

The invention relates to design and construction of a novel gold nanoparticle-anthracene ring pharmaceutical composition. The gold nanoparticle-anthracene ring pharmaceutical composition consists of gold nanoparticles serving as the core, dihydrolipoic acid serving as a connecting arm, an anthracene ring drug serving as a carried medicine and a hydrophilic polymer serving as a biocompatible molecule. The half-life period of the anthracene ring drug can be prolonged, the concentration of the drug in unit volume is increased, the drug is sensitive to acidic pH value, and the bioavailability and the drug metabolism kinetic properties of the drug are improved. The invention also discloses a method for preparing each component of the gold nanoparticle-anthracene ring pharmaceutical composition, a method for preparing the composition, in-vitro release characteristics of the drug and a drug delivery application.

Description

technical field [0001] The invention belongs to the fields of biomedical technology and nanotechnology, and specifically relates to the design and construction of a novel gold nano-anthracycline drug conjugate. The gold nanoanthracycline drug conjugate is composed of gold nanometers as the core, dihydrolipoic acid as the linking arm, anthracyclines as the loaded drug, and a hydrophilic polymer as a biocompatible molecule, which can improve the anthracene The half-life of cyclic drugs increases the concentration of drugs per unit volume, is sensitive to acidic pH, improves the bioavailability and pharmacokinetic properties of drugs, and can be used for intravenous injection of tumor diagnosis and treatment research. Background technique [0002] In the past two decades, nano-drug delivery system has become a research hotspot in the field of pharmacy, which can well solve many problems in the clinical application of some drugs, such as poor water solubility, poor stability, lo...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/704A61P35/00
Inventor 丁娅张灿张文婕耿冬冬梁娟娟
Owner CHINA PHARM UNIV
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