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Hepatoma-targeted nano medicine delivery system and preparation method and application thereof

A technology targeting nanoparticles and liver cancer, applied in the field of pharmacy, can solve the problems of non-target tissue-tropic drugs that are difficult to reach and poor stability, and achieve good stability and long circulation, and the effect of simple preparation process

Inactive Publication Date: 2019-03-22
YICHUN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Objective: In order to overcome the deficiencies in the prior art, the present invention provides an anti-hepatocarcinoid anti-hepatic cancer drug for the problems of hydrophobicity, poor stability, non-target tissue tropism and other outstanding difficulties in the treatment of liver cancer. A nano-drug delivery system targeting liver cancer, specifically a liver cancer-targeted nano-drug delivery system composed of a copolymer carrier with galactose, polyethylene glycol and PLGA fragments loaded with anti-liver cancer drugs. Liver cancer drug targeted delivery to liver tumor cells and effectively kills liver tumor cells

Method used

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  • Hepatoma-targeted nano medicine delivery system and preparation method and application thereof
  • Hepatoma-targeted nano medicine delivery system and preparation method and application thereof
  • Hepatoma-targeted nano medicine delivery system and preparation method and application thereof

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Embodiment 1

[0034] Materials Synthesis of Gal-PEG-PLGA. Weigh an appropriate amount of galactobionic acid, dissolve it in anhydrous dimethyl sulfoxide, add DCC and NHS in sequence, stir and react for 12 hours under nitrogen protection to activate the carboxyl group; then add amino-terminated PEG at both ends, and react for 12 hours to generate Gal-PEG. Weigh an appropriate amount of PLGA, dissolve in anhydrous DMSO, add DCC and NHS in sequence (the molar ratio of the two to PLGA is 1.2:1), protect with nitrogen, stir at room temperature for 12 hours to activate the carboxyl group; then transfer the reaction solution to the Gal-PEG reaction solution , the reaction was stirred at room temperature for 12 h to generate Gal-PEG-PLGA. After the reaction is completed, remove the precipitate by filtration with a microporous membrane, put the filtrate in a dialysis bag (Mw8000-14000), and dialyze with DMSO and distilled water in sequence to remove unreacted substances and solvents. Freeze-dry aft...

Embodiment 2

[0037] Preparation of nanoparticles:

[0038] Gal-PEG-PLGA-loaded camptothecin / 10-hydroxycamptothecin nanoparticles: Weigh 100 mg of Gal-PEG-PLGA polymer material in proportion and dissolve it in 5 mL of organic solvent, and weigh another anti-liver cancer drug camptothecin or 10 - Dissolve 10-100 mg of hydroxycamptothecin in 5-10 mL of organic solvent, and mix the two evenly. One of the preparation methods is to slowly add the mixed solution into a solution containing 1% polyvinyl alcohol under stirring, and continue to stir for a certain period of time in the dark to obtain nanoparticle suspension. Another preparation method is to transfer the mixed solution into a dialysis bag (MW 1500Da), dialyze to remove the organic solvent, freeze-dry the dialysate to obtain nanoparticles, dry and store at low temperature, and redissolve when needed.

[0039]In this embodiment, the materials used for polymer synthesis include galactobionic acid, polyethylene glycol (molecular weight: 2...

Embodiment 3

[0041] Characterization of Camptothecin / 10-Hydroxycamptothecin Nanoparticles Loaded on Gal-PEG-PLGA

[0042] The size and surface charge of the nanoparticles were determined using dynamic light scattering. Take an appropriate amount of nanoparticle suspension, dilute it appropriately with distilled water, and use NanoBrook 90Plus Zeta to measure the particle size and Zeta potential of nanoparticles. Such as figure 2 As shown, the particle size of the nanoparticles is about 140nm, and the Zeta potential is about -20mV.

[0043] The encapsulation efficiency and drug loading of Gal-PEG-PLGA-loaded camptothecin / 10-hydroxycamptothecin nanoparticles were determined by reverse dialysis. The encapsulation efficiency of the nanoparticles prepared by the above method is about 70%-85%, and the drug loading is about 15%-40%.

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Abstract

The invention discloses a hepatoma-targeted nano medicine delivery system and a preparation method and application thereof, and particularly relates to preparation and application of hepatoma-targetednano particles formed by a copolymer material-loaded anti-hepatoma medicine (camptothecin / 10-hydroxycamptothecine) prepared from galactose, polyethylene glycol and PLGA. The medicine delivery systemis prepared from a polymer material Gal-PEG-PLGA and the anti-hepatoma medicine (camptothecin / 10-hydroxycamptothecine) through a coprecipitation method or a dialysis method. The prepared material Gal-PEG-PLGA has hepatoma targeting, biocompatibility and biodegradability, the preparation technology of the nano particles is simple, and in vitro and vivo targeting and activity assessment proves thatthe medicine delivery system can deliver the camptothecin / 10-hydroxycamptothecine to hepatoma cells targetedly and effectively kill the hepatoma cells.

Description

technical field [0001] The invention relates to a liver cancer-targeted nanometer drug delivery system and its preparation method and application, belonging to the technical field of pharmacy. Background technique [0002] Liver cancer has an insidious onset, high invasiveness, and rapid growth. Most patients are at an advanced stage when they see a doctor and are not suitable for surgery. Choosing anti-liver cancer drugs to treat liver cancer is one of the common and important methods. Camptothecin (CPT) and 10-hydroxycamptothecin (10-HCPT) are inhibitors of topoisomerase I, which have been clinically shown to have good curative effects on various malignant tumors such as liver cancer, gastric cancer, and colon cancer . However, due to the strong hydrophobicity, poor stability and low bioavailability of camptothecin and 10-hydroxycamptothecin itself, problems such as large doses, strong toxic and side effects, and no accumulation at target sites during clinical use have se...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G81/00A61K9/51A61K31/4745A61K47/34A61P1/16A61P35/00
CPCA61K9/5146A61K31/4745A61P1/16A61P35/00C08G81/00
Inventor 张兵锋李家敏
Owner YICHUN UNIVERSITY
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