Quantum dot and nintedanib compound microsphere and preparation method thereof

A technology of nintedanib and quantum dots, applied in the field of quantum dots and nintedanib complex microspheres and their preparation, can solve the problem of burst release, long chemical half-life, slow release targeting microspheres, in vivo targeting It can solve the problems of cumbersome evaluation and other problems, so as to achieve the effect of targeted detection, simple and easy operation of the reaction, and favorable for targeted evaluation.

Inactive Publication Date: 2021-07-20
JIANGSU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, nintedanib is usually prepared into sustained-release targeted microspheres to improve the efficacy, safety and stability of the drug, but due to its long chemical half-life, high cardiotoxicity, low drug utilization and burst release phenomenon, it is safe The in vivo targeting evaluation of the sustained-release targeting microspheres prepared at the same time is relatively cumbersome and interferes greatly, which limits its clinical application

Method used

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  • Quantum dot and nintedanib compound microsphere and preparation method thereof
  • Quantum dot and nintedanib compound microsphere and preparation method thereof
  • Quantum dot and nintedanib compound microsphere and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] (1) Activation of quantum dots,

[0032] Take 10 µL of 8 µM / mL QDs solution, dilute it four times with BBS with a pH value of 7.4, add 3.08 µL of 5 mg / mL EDC solution and 3.48 µL of 5 mg / mL NHS solution respectively, the solutions of EDC and NHS should be prepared freshly, vortex Spin for 15 min to activate the carboxyl groups on the surface of the quantum dots.

[0033] (2) Preparation of FA-PEG-PLGA composite carrier material:

[0034] Dissolve 0.24g of folic acid in 15ml of dimethyl sulfoxide, add 0.164g of EDC and 0.23g of NHS, and activate it for 12h at room temperature in the dark, then add 1.05g of PEG-PLGA to it, and dropwise add 0.2ml of triethylamine, React at room temperature for 28 hours. After the reaction, dialyze in dimethyl sulfoxide for 36 hours to remove unreacted folic acid, then dialyze with water for 48 hours to remove dimethyl sulfoxide, and then freeze-dry to obtain the composite carrier FA-PEG-PLGA.

[0035] (3) Preparation of quantum dots and ...

Embodiment 2

[0042] (1) Activation of quantum dots:

[0043] Take 10 µL of 8 µM / mL QDs solution, dilute it four times with BBS with a pH value of 7.4, add 3.08 µL of 5 mg / mL EDC solution and 3.48 µL of 5 mg / mL NHS solution respectively, the solutions of EDC and NHS should be prepared freshly, vortex Spin for 15 min to activate the carboxyl groups on the surface of the quantum dots.

[0044] (2) Preparation of FA-PEG-PLGA composite carrier material:

[0045]Dissolve 0.24g of folic acid in 15ml of dimethyl sulfoxide, add 0.164g of EDC and 0.23g of NHS, activate at room temperature for 18h in the dark, then add 1.05g of PEG-PLGA, and dropwise add 0.2ml of triethylamine, React at room temperature for 32 hours. After the reaction, dialyze in dimethyl sulfoxide for 42 hours to remove unreacted folic acid, then dialyze with water for 48 hours to remove dimethyl sulfoxide, and then freeze-dry to obtain the composite carrier FA-PEG-PLGA.

[0046] (3) Preparation of quantum dots and nintedanib com...

Embodiment 3

[0050] (1) Activation of quantum dots:

[0051] Take 10 µL of 8 µM / mL QDs solution, dilute it four times with BBS with a pH value of 7.4, add 3.08 µL of 5 mg / mL EDC solution and 3.48 µL of 5 mg / mL NHS solution respectively, the solutions of EDC and NHS should be prepared freshly, vortex Spin for 15 min to activate the carboxyl groups on the surface of the quantum dots.

[0052] (2) Preparation of FA-PEG-PLGA composite carrier material:

[0053] Dissolve 0.24g of folic acid in 15ml of dimethyl sulfoxide, add 0.164g of EDC and 0.23g of NHS, activate at room temperature for 24h in the dark, then add 1.05g of PEG-PLGA, and dropwise add 0.2ml of triethylamine, React at room temperature for 36 hours. After the reaction, dialyze in dimethyl sulfoxide for 48 hours to remove unreacted folic acid, then dialyze with water for 48 hours to remove dimethyl sulfoxide, and then freeze-dry to obtain the composite carrier FA-PEG-PLGA.

[0054] (3) Preparation of quantum dots and nintedanib co...

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Abstract

The invention provides a quantum dot and nintedanib compound microsphere and a preparation method thereof, and belongs to the technical field of medicine preparation. According to the invention, QDs is taken as a tracing material, nintedanib (NDNB) is taken as an anti-tumor model drug, the QDs and the nintedanib are wrapped in polylactic acid-glycolic acid (PLGA) which takes folic acid as an active targeting ligand and is combined with a carrier material by using a physical embedding technology, and an electrostatic spinning technology is used for a targeting microsphere drug delivery system, so that high activity and high stability of the nintedanib are kept; and meanwhile, the fluorescent quantum dots are applied to a drug delivery system, so that targeting detection of drugs is realized, and later targeting evaluation is facilitated.

Description

technical field [0001] The invention belongs to the technical field of medicine preparation, and in particular relates to a composite microsphere of quantum dots and nintedanib and a preparation method thereof. Background technique [0002] Nintedanib (Nintedanib) is a potent oral small molecule tyrosine kinase inhibitor, and also a triple kinase inhibitor, which mainly acts on three channels involved in angiogenesis, and is effective for idiopathic pulmonary fibrosis (IPF ) shows a strong anti-fibrotic effect, and can also be used in the treatment of idiopathic pulmonary fibrosis (IPF) and in combination with docetaxel for the treatment of patients with advanced adenocarcinoma after first-line chemotherapy. Small molecule targeting and drugs that have effects on interstitial pneumonia. [0003] At present, nintedanib is usually prepared into sustained-release targeted microspheres to improve the efficacy, safety and stability of the drug, but due to its long chemical half-...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/496A61K47/54A61K47/34A61K49/00A61P35/00
CPCA61K49/0067A61K49/0091A61K49/0054A61K49/0052A61K47/545A61K9/1647A61K9/1694A61K31/496A61P35/00
Inventor 刘宏飞王芬邹谊张强
Owner JIANGSU UNIV
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