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Receptor-mediated quantum dot tracing targeted drug delivery system, preparation method thereof and application

A technology of targeted drug delivery and quantum dots, which is applied in the field of receptor-mediated quantum dot tracer targeted drug delivery system and its preparation, can solve the problems of fast degradation, limited application, short residence time, etc., and achieve good stealth resistance, good reversal of drug resistance, and good stealth effect

Inactive Publication Date: 2012-10-24
WUHAN UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, HA is easily soluble in water, easily absorbed, has a short residence time in tissues, and has a fast degradation rate, which limits its application in the medical field.

Method used

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  • Receptor-mediated quantum dot tracing targeted drug delivery system, preparation method thereof and application
  • Receptor-mediated quantum dot tracing targeted drug delivery system, preparation method thereof and application
  • Receptor-mediated quantum dot tracing targeted drug delivery system, preparation method thereof and application

Examples

Experimental program
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Effect test

Embodiment 1

[0039] 1. Preparation of PEG-HA-QDs-MEL components

[0040] (1) Synthesis and purification of carboxyl-terminated polyethylene glycol

[0041] Put 10g (5mmol) PEG-1500 in a 250mL three-necked flask with a condenser, stirrer and thermometer, add 100mL chloroform (CaH 2 After the dissolution, add 2.5g (25mmol) succinic anhydride, heat to dissolve, add 2mL dry pyridine at the same time, stir and reflux for 6 hours, stop the reaction and cool to room temperature, and the reaction mixture is evaporated under reduced pressure Add a large amount of anhydrous ether to the residue until it becomes viscous, and a white precipitate product is precipitated, and the filter cake is obtained by suction filtration. The filter cake is dissolved in 30 mL of dichloromethane, and the insoluble matter is filtered off, and anhydrous ether is added for precipitation, and a white precipitate is precipitated. The product was obtained by suction filtration to obtain a filter cake, and then the produc...

Embodiment 2

[0061] 1. Preparation of PEG-HA-QDs-MEL components

[0062] (1) Synthesis and purification of carboxyl-terminated polyethylene glycol

[0063]Put 40g (5mmol) PEG-1500 in a 500mL three-neck flask with a condenser, a stirrer and a thermometer, add 200mL chloroform (CaH 2 After the dissolution, add 5.0g (25mmol) succinic anhydride, heat to dissolve, add 8mL dry pyridine at the same time, reflux reaction for 6 hours under stirring, cool to room temperature after stopping the reaction, and evaporate the reaction mixture under reduced pressure Add a large amount of anhydrous diethyl ether to the residue to precipitate a white precipitate, filter it with suction, dissolve the product with 120mL of dichloromethane, filter off the insoluble matter, then add anhydrous diethyl ether to precipitate a white precipitate, filter it with suction, Repeat the above operation 3 times, vacuum-dry to constant weight after suction filtration to obtain carboxyl-terminated polyethylene glycol (PEG-...

Embodiment 3

[0084] 1. Preparation of PEG-HA-QDs-MEL components

[0085] (1) Synthesis and purification of carboxyl-terminated polyethylene glycol

[0086] Put 20g (5mmol) PEG-1500 in a 250mL three-necked flask with a condenser, a stirrer and a thermometer, add 100mL chloroform (CaH 2 After the dissolution, add 5.0g (25mmol) succinic anhydride, heat to dissolve, add 4mL of dry pyridine at the same time, stir and reflux for 6 hours, stop the reaction and cool to room temperature, the reaction mixture is decompressed Evaporate until it becomes viscous, add a large amount of anhydrous ether to the residue, precipitate a white precipitate, filter it with suction, dissolve the product with 60mL of dichloromethane, filter off the insoluble matter, add anhydrous ether to precipitate, precipitate a white precipitate, and filter it with suction , repeat the above operation 3 times, vacuum-dry to constant weight after suction filtration, obtain carboxyl-terminated polyethylene glycol (PEG-SA-NHS),...

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Abstract

Disclosed are a receptor-mediated quantum dot tracing targeted drug delivery system, a preparation method thereof and application. The targeted drug delivery system comprises polyethylene glycol, hyaluronic acid, quantum dots and melphalan complex which are abbreviated as PEG-HA-QDs-MEL. The PEG is connected with HA amide in a dewatered and condensed manner, the water-soluble CdTe / CdS quantum dots are connected into the HA, and finally, the PEG, the HA and the QDs are prepared with the MEL complex to obtain the targeted drug delivery system. The component content of the PEG-HA-QDs-MEL includes, by weight, 30-100 parts of the MEL, 600-1500 parts of the PEG, 200-500 parts of the HA, 5-50 parts of the CdTe / CdS quantum dots, 20-50 parts of DCC (dicyclohexylcarbodiimide), 1-10 parts of DMAP (dimethylamino-pyridine), 100-500 parts of succinic anhydride, 20-50 parts of NHS, 20-50 parts of EDC (carbodiimide) and 10-100 parts of sodium bisulfite. The targeted drug delivery system is applied to preparing antitumor drugs.

Description

technical field [0001] The invention relates to the field of medicines, in particular to a receptor-mediated quantum dot tracer targeted drug delivery system and its preparation method and application. Background technique [0002] Malignant tumors have become one of the most important diseases that threaten human health and life. At present, the combination of surgery and chemotherapy is mainly used for the comprehensive treatment of malignant tumors. Chemotherapy is the necessary treatment method. Because of its powerful drug, it can quickly kill or kill tumor cells, and it plays an important role in clinical treatment. However, chemotherapy drugs generally have poor cell selectivity, large toxic and side effects, severe adverse reactions, and are prone to serious adverse reactions and multi-drug resistance (MDR), resulting in unsatisfactory chemotherapy effects. Therefore, how to improve the tissue or cell selectivity of drugs, how to accurately deliver drugs to tumor ti...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/196A61K49/00A61K39/44A61K45/00A61K48/00A61P35/00A61K47/34A61K47/36
Inventor 许沛虎张喻徐海星徐金巧黄志军刘慧王玲李映萱王玉杨昭
Owner WUHAN UNIV OF TECH
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