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A pH-sensitive chitosan drug-loaded micelle with both targeting and fluorescence properties and its preparation method

A technology of fluorescent, drug-loaded micelles, which can be used in pharmaceutical formulations, medical formulations with inactive ingredients, and medical formulations containing active ingredients, etc., can solve tissue and organ damage, affect the healing effect and quality of life of cancer patients, Normal organ cell damage and other problems, to achieve the effect of reducing toxic side effects and good pH-sensitive drug release performance

Active Publication Date: 2019-07-16
TIANJIN CHENGJIAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, while anticancer drugs kill cancer cells, they also cause serious damage to some normal organ cells in the body, and also cause damage to certain tissues and organs such as liver, kidney, heart, lung, etc., seriously affecting cancer cells. Patient outcomes and quality of life

Method used

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  • A pH-sensitive chitosan drug-loaded micelle with both targeting and fluorescence properties and its preparation method
  • A pH-sensitive chitosan drug-loaded micelle with both targeting and fluorescence properties and its preparation method
  • A pH-sensitive chitosan drug-loaded micelle with both targeting and fluorescence properties and its preparation method

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preparation example Construction

[0030] The idea of ​​constructing the pH-sensitive chitosan drug-loaded micelles with both targeting and fluorescence of the present invention is to use pH-sensitive amphiphilic N-octyl-N'-(2-carboxycyclohexanoyl ) Chitosan (OCCC) is a drug-loaded micelle, and polyethylene glycol is used as the linking arm, and folic acid and the fluorescent dye thiazole orange are grafted on both ends of the micelle, thereby constructing a targeted, pH sensitive, Multifunctional chitosan drug-loaded micelles with invisibility and fluorescence tracing in one. In the preparation process of the chitosan drug-loaded micelles, firstly, chitosan was used as the main body, and hydrophobic octyl chains were grafted on it through reductive amination reaction. Hydrophilic carboxycyclohexyl carboxyl group to construct an amphiphilic chitosan with pH-sensitive properties; then, at the terminal amino polyethylene glycol (H 2 N-PEG-NH 2 ) FA-PEG-NH is prepared by grafting folic acid (FA) and fluorescent dye...

Embodiment 1

[0043] Take the chitosan drug-loaded micelle FA-PEG-(OCCC-1)-PEG-TO prepared with the preparation of OC-1 as the main body of chitosan and the holding time of 5h during the preparation of OC as an example

[0044] Weigh 4g of chitosan (CTS) and place it in anhydrous methanol (MeOH), swell at 30°C under mechanical agitation; then slowly add 10 mL of octyl aldehyde dropwise to the reaction solution and keep it warm for 5h Then, add sodium borohydride 2gNaBH in six batches 4 , Continue to reduce at room temperature for 12 hours, adjust the pH of the reaction solution to 6-8 after the reduction reaction is complete; the reaction solution is suction filtered, and the filter cake is washed alternately with methanol and deionized water, and then the filter cake is vacuum dried to obtain a light yellow N- Octyl chitosan (OC); Weigh 1g of the aforementioned N-octyl chitosan (OC) and place it in a reaction flask, swell with anhydrous dimethyl sulfoxide (DMSO), and at room temperature 1g of...

Embodiment 2

[0049] Take the chitosan drug-loaded micelle FA-PEG-(OCCC-2)-PEG-TO prepared with the preparation of OC-2 as the main body of chitosan and the holding time of 8h during the preparation of OC as an example

[0050] Weigh 4g of chitosan (CTS) and place it in anhydrous methanol (MeOH), swell it at 30°C under mechanical agitation; then slowly add 11.5mL of octyl aldehyde dropwise to the reaction solution, and heat the reaction After 8h, add sodium borohydride 2gNaBH in six batches 4 , Continue to reduce at room temperature for 20 hours, adjust the pH of the reaction solution to 6-8 after the reduction reaction is completed; the reaction solution is suction filtered, and the filter cake is washed alternately with methanol and deionized water, and then the filter cake is vacuum dried to obtain a light yellow N- Octyl chitosan (OC); Weigh 1g of the aforementioned N-octyl chitosan (OC) and place it in a reaction flask, swell with anhydrous dimethyl sulfoxide (DMSO), and at room temperatur...

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Abstract

The invention discloses PH-sensitive chitosan drug-carrying micelle with targeting and fluorescent characteristics and a preparation method thereof; the multifunctional chitosan drug-carrying micelle with targeting property, PH sensitivity, invisibility and fluorescent tracing combined in a whole is constructed by using PH-sensitive amphiphilic chitosan as drug-carrying micelle and polyethylene glycol as a link arm, and grafting folic acid and fluorescent dye thiazole orange to two ends of the micelle; the chitosan drug-carrying micelle of the invention has good fluorescent properties, and has good drug-carrying property for anticancer drug 5-fluorouracil, with drug-carrying efficiency up to 42.76%; under physiological environmental PH (PH=7.4), accumulative drug release within 8 h is only 2%, accumulative drug release within 26 h is less than 8%, and toxic and side effects of the chitosan drug-carrying micelle for normal tissue cells during transport of the anticancer drug 5-fluorouracil can be decreased; in addition, under tumor cell lysosome PH value (PH=4.5), good PH-sensitive drug release property is exhibited, and 5-fluorouracil release within 4 h is up to 95%.

Description

Technical field [0001] The present invention belongs to the cross-field of chemistry and biomedicine of the present invention, and specifically relates to a pH-sensitive chitosan drug-loaded micelle with both targeting and fluorescence characteristics and a preparation method thereof. Background technique [0002] Cancer is a major disease that seriously endangers human health and has attracted widespread attention from domestic and foreign researchers. In cancer treatment methods, chemotherapy with anticancer drugs is one of the most effective methods to completely kill cancer cells in the body after surgery for cancer patients. But while anticancer drugs kill cancer cells, they also cause serious damage to certain normal organ cells in the body, and also cause damage to certain tissues and organs such as liver, kidney, heart, lungs, etc., seriously affecting cancer. The patient's healing effect and quality of life. Based on this, how to improve the targeting of anticancer dru...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K47/36A61K47/22A61K47/10A61K31/513A61P35/00C08G81/00
CPCA61K9/1075A61K31/513A61K47/10A61K47/22A61K47/36C08G81/00
Inventor 费学宁李书蓓曹凌云张宝莲于妙卓
Owner TIANJIN CHENGJIAN UNIV
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