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Preparation method of nanometer targeted drug, and application of nanometer targeted drug for treating gastric carcinoma

A nano-drug, targeting technology, applied in the field of biomedicine, to achieve the effects of good application prospects, high emission quantum yield, and excellent sustained release

Pending Publication Date: 2021-03-16
SHANGHAI JIAO TONG UNIV +4
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The therapeutic agent and targeting ligand are determined, the main issue is the choice of nanocarriers, gold nanoparticles (GNP) and zinc sulfide quantum dots (ZnS QD) are selected as nanocarriers for cancer diseases, not yet in the open literature to report

Method used

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  • Preparation method of nanometer targeted drug, and application of nanometer targeted drug for treating gastric carcinoma
  • Preparation method of nanometer targeted drug, and application of nanometer targeted drug for treating gastric carcinoma
  • Preparation method of nanometer targeted drug, and application of nanometer targeted drug for treating gastric carcinoma

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0111] Embodiment 1, the preparation of nano therapeutic drug

[0112] Two kinds of nano-therapeutic drugs were prepared respectively. Both nanotherapeutics have the same linker: cysteine, the targeting ligand is transferrin, and the chemotherapy drug is doxorubicin, but the nanocarriers are different. Gold nanoparticles (GNPs) were used in the first nanotherapeutic drug due to their unique physical properties, and zinc sulfide quantum dots (ZnS) were selected as the second nanotherapeutic drug nanocarrier.

[0113] The preparation of nano therapeutic drug is as follows:

[0114] 1. The preparation of GNP nano-therapeutic drugs, including the synthesis of GNP, the combination of cysteine ​​and GNP, the combination of doxorubicin and GNP-Cys, and the combination of transferrin and GNP-Cys-Dox.

[0115] GNPs were synthesized using an optimized citric acid reduction method. Different concentrations of gold salts and sodium citrate were used to check the ideal concentration. GNP...

Embodiment 2

[0123] Example 2, Preparation and Characterization of Diagnostic Probes

[0124] Synthetic cysteine-coated GNPs were conjugated to transferrin for diagnostic probing. It is used to examine the efficiency of transferrin as a targeting ligand for cancer and liver cancer cells. Expression of transferrin in induced gastric cancer tissues was also examined.

[0125] Such as figure 1 Shown in (b), is the UV-Vis spectrum analysis of the target diagnostic probe, which is compared with the UV-Vis spectrum of cysteine-coated GNP, as figure 1 (a) shown. The spectrum of cysteine-coated GNPs showed a sharp peak at 520nm, indicating a narrow size distribution with a particle size of less than 20nm. After transferrin binding, as figure 1 As shown in (b), the new spectrum shows a shift of the inorganic peak at 525 nm from the organic peak at 340 nm. The peaks became broader, indicating that conjugation of the protein on the nanoparticles resulted in an increase in the size of the nanoco...

Embodiment 3

[0131] Example 3, Therapeutic Effects of GNP and ZnS QDs

[0132] 1. Nanomedicine for GNP tumor therapy (in vitro)

[0133] Cellular uptake, therapeutic efficacy and cellular targeting of a therapeutic nanomedicine against colon cancer cell (HCT 116-Luc2 and confirmed by different analyses. Techniques used to study cell viability for intracellular nanomedicine tracking include inverted microscopy, fluorescence microscopy, trypan blue assay, neutral red assay (metabolic activity), crystal violet staining assay (cell adhesion studies), and fluorescence intensity measurements. Statistical comparison of all results leads to clear results.

[0134] Human colon cancer cell line: HCT-116 (a male patient-derived cell line) was used to examine the effect of therapeutic nanomedicines in vitro. Involved cell lines specify a mismatch-deficient repair system for p53 wild-type and K-Ras mutants. The morphology of the cells is a spindle-shaped appearance. The reserved vials were remove...

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Abstract

The invention relates to the technical field of biological medicines, in particular to a preparation method of a nanometer targeted drug, and application of the nanometer targeted drug for treating gastric carcinoma. Two types of different nanometer drugs are prepared, and main nano-carriers are gold nanoparticles (GNP) and zinc sulfide quantum dots (ZnS QD), and are coupled with Adriamycin and ligand transferrin to carry out targeting on the protein tumor cell of a transferrin receptor which is in high expression on gastric carcinoma cells or the stomach. The nano-carrier gold nanoparticle (GNP) is a most compatible nanostructure which has better advantages than other metal nanometer composite materials, and the zinc sulfide quantum dot (ZnS QD) is a very important quantum dot nanoparticle, has small toxicity, is friendly to human and has a narrow-band spectrum. The prepared two therapeutic nanometer drugs have good stability, a high drug loading capacity and good slow-release properties, can enhance medicine targeting concentration, enhance a tumor killing treatment effect and lower a non-specific toxic and side effect. The design way of the two therapeutic nanometer drugs can beused for gastric carcinoma diagnosis, gastric carcinoma treatment and gastric carcinoma prognosis, and an application prospect is good.

Description

technical field [0001] The invention relates to the technical field of biomedicine, in particular to a preparation method of a nano-targeted drug and its application in treating gastric cancer. Background technique [0002] Of all the dreadful diseases, cancer is the leading cause of death worldwide and their incidence is increasing worldwide. Among the different types of cancer, gastric cancer is one of the most prevalent cancers with the highest mortality rate, gastric cancer may be caused by diet, organic solvents, insecticides and pesticides, gastric cancer is also directly related to many factors such as high salt in diet Intake or infection with microorganisms such as Helicobacter pylori (H. pylori), which is caused by the infection of the stomach wall by microorganisms such as Helicobacter pylori or caused by certain genetic changes. Currently, various imaging techniques are being used for cancer diagnosis, such as single photon emission tomography, magnetic resonanc...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K31/704A61K47/54A61K47/64A61K47/65A61K49/00A61P35/00B82Y5/00B82Y30/00B82Y40/00B82Y20/00
CPCA61K31/704A61K47/644A61K47/65A61K47/6923A61K47/542A61P35/00B82Y5/00B82Y30/00B82Y40/00B82Y20/00A61K49/0067A61K49/0056
Inventor 魏冬青莫达·沙扎德·洛迪阿里夫·马里克穆罕默德·塔希尔·汗塞拉·阿夫塔布扎胡尔·卡迪尔·萨姆拉王恒王艳菁
Owner SHANGHAI JIAO TONG UNIV
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