Application of carbon dots as antitumor drug carriers

An anti-tumor drug and carbon dot technology, applied in the field of nanomedicine, can solve the problems of protein non-specific adsorption, poor stability of drug loading, increase drug side effects, etc., achieve high drug loading rate, good water solubility, and high quantum yield Effect

Active Publication Date: 2017-09-19
SOUTHEAST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the method of loading doxorubicin on carbon dots based on physical adsorption (Lee H.U., Park S.Y. and Park E.S. et al., Sci. Rep. 2014, 4, 4665.) has the disadvantage of poor drug loading stability, which may It will cause the drug molecules to be released before reaching the target, which will increase the side effects of the drug and reduce the curative effect
The strategy of directly linking doxorubicin molecules to carbon dots in a covalent manner (Mewada A., Pandey S. and Thakur M. et al., J. Mater. Chem. B, 2014, 2, 698.), due to the The poor solubility of mycin itself will cause the instability of the final product and the non-specific adsorption of proteins

Method used

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  • Application of carbon dots as antitumor drug carriers
  • Application of carbon dots as antitumor drug carriers
  • Application of carbon dots as antitumor drug carriers

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] The preparation of thiolated doxorubicin comprises the following steps:

[0038] (1) Dissolve doxorubicin in a solution (pH=8.0) of dimethyl sulfoxide (DMSO) and phosphate buffer (PBS), and add Traut in the amount of 3 times the substance of doxorubicin ’ s reagent;

[0039] (2) React at room temperature for 1 hour to obtain thiolated doxorubicin.

Embodiment 2

[0041] Preparation of AEEA carbon dots, see figure 1 , including the following steps:

[0042] (1) Into the glycerol, feed nitrogen for 5 minutes to remove the oxygen in the glycerol;

[0043] (2) Add 3-[2-(2-aminoethylamino)ethylamino]propyltrimethoxysilane (AEEA) to glycerol to make its volume fraction 9.1% (5-30%), in a closed state Stir for more than 5 minutes to form a carbon dot precursor solution;

[0044] (3) React in a microwave reactor at 160°C for 15 minutes;

[0045] (4) Centrifuge to remove the precipitate generated, and leave the supernatant;

[0046] (5) Use a dialysis bag with a molecular weight of 1000 to dialyze the supernatant in ultrapure water for more than 48 hours (change the water every 6 hours) to obtain a pure carbon dot solution.

Embodiment 3

[0048] The preparation of aminated carbon dots is similar to that of Example 2, except that in step (3) the microwave reactor was reacted at 180°C for 5 minutes, and the 3-[2-(2-aminoethylamino)ethylamino]propane The volume fraction of trimethoxysilane (AEEA) is 5%.

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Abstract

The invention provides the application of carbon dots as anti-tumor drug carriers, comprising the following steps: preparation of aminated carbon dots: using microwave synthesis method, using amino-containing silane reagents and glycerol as raw materials to prepare aminated carbon dots; carbon dots Surface maleimidation: Aminated carbon dots react with short-chain polyethylene glycol molecules NHS‑EGn‑MAL with N‑hydroxysuccinimide ester at one end and maleimide at the other end to obtain Maleimidated carbon dots; preparation of carbon dot-drug molecule complexes: Maleimidized carbon dots react with drugs with sulfhydryl groups to obtain carbon dot-drug molecule complexes. The aminated carbon dots prepared by this method have high fluorescence quantum yield, good water solubility, low cytotoxicity, a large number of modifiable groups on the surface, and no aggregation and precipitation after modification of short-chain polyethylene glycol segments. A very ideal drug carrier.

Description

technical field [0001] The invention relates to the application of carbon dots as antitumor drug carriers, belonging to the technical field of nanomedicine. Background technique [0002] Carbon is one of the most basic elements that make up organic organisms and is indispensable to all currently known living systems, without which life would not be possible. In recent years, various carbon materials (such as carbon nanotubes, graphene, fullerene, etc.) have been widely used in biological detection, catalysis, energy, electronic devices, and drug loading. Fluorescent carbon nanoparticles, as a new type of zero-dimensional carbon material, have attracted much attention due to their cheap raw materials, good biocompatibility, good photostability and easy surface modification. [0003] Due to the good biocompatibility and easy modification of carbon-based materials, they have been widely used in drug loading in recent years. Early related reports have mentioned graphene oxide a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/60A61K47/51A61K31/704A61P35/00
Inventor 吴富根杨婧婧张晓东王志飞陈战
Owner SOUTHEAST UNIV
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