Controlled-release medicine for targeted treatment of colorectal cancer and preparation method thereof

A colorectal cancer, targeted therapy technology, applied in the field of biomedicine, can solve the problem of colorectal cancer without graphene oxide nanocarriers

Active Publication Date: 2020-04-17
AFFILIATED HOSPITAL JIANGNAN UNIV WUXI NO 4 PEOPLES HOSPITAL +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] There are currently no applications of graphene oxide nanocarriers for the treatment of colorectal cancer

Method used

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  • Controlled-release medicine for targeted treatment of colorectal cancer and preparation method thereof
  • Controlled-release medicine for targeted treatment of colorectal cancer and preparation method thereof
  • Controlled-release medicine for targeted treatment of colorectal cancer and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0072] Embodiment 1: the preparation of nano carrier material

[0073] Synthesis of Graphene Oxide Nanosheets:

[0074] Add 0.25g of graphite powder and 0.125g of sodium nitrate into 5.75mL of concentrated sulfuric acid and react for 1.5h. Subsequently, 0.75g KMnO 4 Slowly added to the above mixed solution with continuous stirring. In order to keep the temperature of the solution below 10°C, the mixture was placed in an ice bath for 2 h. Then put it in a constant temperature water bath, react at 38°C for 0.5h, and add 11.5mL of deionized water dropwise. Remove the constant temperature water bath and react in an oil bath at 98° C. for 0.5 h while maintaining magnetic stirring. At this time, the solution turns from purple to brownish yellow. Take it out and put it in a 38°C oil bath, add 35mL of 38°C warm water for further dilution, and then add 3% H 2 o 2 20mL, the solution remained brown-yellow. While hot, use deionized water at 9000rpm, centrifuge and wash three times...

Embodiment 2

[0079] Example 2: Preparation of Drugs for Targeted Treatment of Colorectal Cancer (Nanocomposite Material 5-FU / GO-PEG Loaded with Pentafluorouracil (5-FU))

[0080] Prepare the GO-PEG aqueous suspension, add the chemotherapeutic drug 5-FU at a mass ratio of 1:2, sonicate for 40 minutes, stir at room temperature for 24 hours, and dialyze with deionized water for 48 hours to remove unloaded 5-FU to obtain drug-loaded nanoparticles. Composite 5-FU / GO-PEG. It was measured that the drug loading amount was 25.66% (carrier: 5-FU=3:1), and the encapsulation efficiency was 17.26.

[0081] Determination of the drug loading capacity of drug-loaded nanomaterials 5-FU / GO-PEG: preparation of different concentrations of 5-FU H 2 O solution (0 μg·mL -1 , 2μg·mL -1 , 4μg·mL -1 , 8μg·mL -1, 10μg·mL -1 , 12μg·mL -1 , 14μg·mL -1 , 18μg·mL -1 , 20μg·mL -1 ), using UV-Vis to measure its absorbance at 265nm, and draw a standard curve. Parallel experiments were performed three times. Acc...

Embodiment 3

[0085] Example 3: Synthesis of tumor cell epidermal growth factor peptide (GE11) modified nanocomposite 5-FU / GO-PEG-GE11

[0086] Prepare the aqueous suspension of GO-PEG-5-FU, add 0.3mg 1-ethyl-(3-dimethylaminopropyl) carbodiimide hydrochloride, stir at room temperature for 4h, according to the concentration ratio (1:1 ) by adding an appropriate amount of GE11-FITC targeting peptide, stirring overnight, and dialysis for 12 hours to obtain 5-FU / GO-PEG-GE11 nanosheet material.

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Abstract

The invention discloses a controlled-release medicine for targeted treatment of colorectal cancer and preparation method thereof, belonging to the field of biological medicines. According to the invention, GO modified by polyethylene glycol is used as a carrier for carrying the chemotherapeutic drug pentafluorouracil to form 5-FU/GO-PEG; and the surface of the 5-FU/GO-PEG-GE11 can be modified withtumor cell epidermal growth factor peptide (GE11) to obtain 5-FU/GO-PEG-GE11. The biological safety of the medicine is authenticated and evaluated at a cellular level and in the body of a mouse; in-vitro experiments prove that the nano-carrier realizes drug release under the triggering of an acidic pH value, and it is verified that the nano-carrier has drug delivery capacity and photothermal-chemotherapy synergistic effect; in addition, in-vivo behavior tracing and treatment efficacy evaluation are carried out in a subcutaneous solid tumor mouse model, and the medicine is expected to play a huge role in clinical application.

Description

technical field [0001] The invention belongs to the field of biomedicine, and in particular relates to a targeted and controlled release drug for treating colorectal cancer and a preparation method thereof. Background technique [0002] Colorectal cancer (CRC) is one of the most common malignant tumors. With the improvement of living standards and changes in diet structure in our country, the incidence of colorectal cancer has increased rapidly. There are millions of new cases and hundreds of thousands of deaths every year in the world. It ranks third and second among male and female cancers, respectively. Therefore, improving the therapeutic effect of colorectal cancer is the focus of many scholars' research. Currently, the treatment methods for colorectal cancer are mainly divided into the following four methods: surgery, radiotherapy, chemotherapy and biological therapy. However, simple surgical treatment is now difficult to satisfy the long-term survival desire of canc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K41/00A61K47/60A61K47/64A61K31/513A61P35/00B82Y5/00B82Y30/00
CPCA61K31/513A61K47/64A61K47/60A61K47/6923A61K41/0052A61P35/00B82Y5/00B82Y30/00A61K2300/00
Inventor 华东茆勇尹健胡静仇志超
Owner AFFILIATED HOSPITAL JIANGNAN UNIV WUXI NO 4 PEOPLES HOSPITAL
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