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A liver cancer-targeted graphene oxide drug-loaded composite material and preparation method thereof

A composite material and graphene technology, applied in the direction of drug combination, pharmaceutical formula, medical preparations of non-active ingredients, etc., can solve the problem of large lethality, achieve high release rate, simple operation, and high drug loading effect

Inactive Publication Date: 2016-11-23
DONGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, DOX will have greater lethality to normal cells in large doses. Therefore, in order to reduce the toxic and side effects of DOX on normal tissues of the human body, it is necessary to use drug carriers to load DOX and control its release.
[0006] A search of domestic and foreign literature and patents on DOX targeted transport shows that: using multifunctional graphene as a carrier material to load doxorubicin through π-π stacking to achieve multiple effects of targeted and pH-sensitive release is still comparative. few

Method used

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  • A liver cancer-targeted graphene oxide drug-loaded composite material and preparation method thereof
  • A liver cancer-targeted graphene oxide drug-loaded composite material and preparation method thereof
  • A liver cancer-targeted graphene oxide drug-loaded composite material and preparation method thereof

Examples

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Effect test

Embodiment 1

[0042] (1) Dissolve 5mg of graphene oxide composite material in 5ml of water, add 5mL of DOX (5mg) aqueous solution dropwise while stirring, adjust the pH to 9.0 with 0.1M sodium hydroxide solution, at room temperature Under stirring for 4h. Finally, the graphene oxide solution containing doxorubicin was put into a dialysis bag (MW=8,000-14,000), and the unattached doxorubicin was removed by dialysis, and dialyzed three times with PBS buffer, 2 L each time. Finally, the product was freeze-dried to obtain GO / DOX.

[0043](2) Weigh 2 mg doxorubicin, prepare respectively 0.002M, 0.004M, 0.008M, 0.016M, 0.032M PBS solution (pH=7.4) and acetic acid solution (pH=5.8), and carry out ultraviolet light on the doxorubicin solution For detection, the absorption wavelength was set to 481nm, and the data were collected and fitted to a standard curve of doxorubicin under two pH conditions.

[0044] (3) Weigh 2mg of the drug-loaded complex in 2ml of phosphate buffer (pH=7.4), dissolve it f...

Embodiment 2

[0047] (1) Dissolve 8mg of graphene oxide composite material in 8ml of water, and add 13mL of DOX (6mg) aqueous solution dropwise while stirring, and adjust the pH to 9.0 with 0.1M sodium hydroxide solution. Under stirring for 4h. Finally, the graphene oxide solution containing doxorubicin was put into a dialysis bag (MW=8,000-14,000), and the unattached doxorubicin was removed by dialysis, and dialyzed three times with PBS buffer, 2 L each time. Finally, the product was freeze-dried to obtain GO / DOX.

[0048] (2) Weigh 3mg doxorubicin, prepare respectively 0.0025M, 0.005M, 0.01M, 0.02M, 0.04M PBS solution (pH=7.4) and acetic acid solution (pH=5.8), and carry out ultraviolet light on the doxorubicin solution For detection, the absorption wavelength was set to 481nm, and the data were collected and fitted to a standard curve of doxorubicin under two pH conditions.

[0049] (3) Weigh 4.5mg of the drug-loaded complex in 4.5ml of phosphate buffer (pH=7.4), fully dissolve it, put...

Embodiment 3

[0052] (1) Dissolve 10mg of graphene oxide composite material in 10ml of water, add 5mL of DOX (10mg) aqueous solution dropwise while stirring, and adjust pH=5.5, 6.5, 7.5, 8.5 and 9.5, stirred at room temperature for 4h. Finally, the graphene oxide solutions containing doxorubicin at different pH values ​​were put into dialysis bags (MW=8,000-14,000), and the unattached doxorubicin was removed by dialysis, and dialyzed three times with PBS buffer, each times 2L. Finally, the product was freeze-dried to obtain GO / DOX.

[0053] (2) Weigh 2 mg doxorubicin, prepare respectively 0.001M, 0.002M, 0.004M, 0.012M, 0.036M PBS solution (pH=7.4) and acetic acid solution (pH=5.8), and carry out ultraviolet light on the doxorubicin solution For detection, the absorption wavelength was set to 481nm, and the data were collected and fitted to a standard curve of doxorubicin under two pH conditions.

[0054] (3) Weigh 0.5 mg of drug-loaded complexes in 1 ml of phosphate buffer (pH=7.4), ful...

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Abstract

The invention relates to a liver cancer-targeted graphene oxide drug-loaded composite material and a preparation method thereof. The composite material is a composite of doxorubicin DOX and lactobionic acid-modified graphene oxide GO-PEI-FI-PEG-LA things. Preparation: synthesis of graphene oxide composite material GO‑PEI‑FI‑PEG‑LA; preparation of doxorubicin standard curves in two pH environments; dissolving graphene oxide composite material in water, adding doxorubicin hydrochloride aqueous solution, And adjust the pH value to neutral alkaline, stir for 4 hours, dialyze, and freeze-dry to obtain the product; the new drug-loaded material of the present invention has the characteristics of pH-sensitive release and liver cancer cell targeting, and can be used for anti-tumor research, and has great advantages. Good practical value.

Description

technical field [0001] The invention belongs to the field of liver cancer targeting nanomaterials and preparation thereof, in particular to a liver cancer targeting graphene oxide drug-loaded composite material and a preparation method thereof. Background technique [0002] The toxic side effects and poor water solubility of anticancer drugs have always been the bottleneck problems in tumor chemotherapy, so the use of drug delivery systems has received extensive attention. With its unique size range (1-100nm), the nano-drug loading system can not only reduce the biological toxicity of drugs, effectively improve the solubility and stability of drugs, but also can and can be modified through the modification of drug carriers, the selection of carrier drugs and loading methods. It is designed to control the sustained release and directional delivery of drugs, so as to achieve the best therapeutic effect. [0003] As a new type of two-dimensional nanomaterial, graphene has uniq...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K31/704A61K47/04A61P35/00
Inventor 朱利民陶磊杨卉卉公晓曹欣乐
Owner DONGHUA UNIV
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