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A nano-drug delivery system for time-sequential release of curcumin and chemotherapeutic drugs and its application

A nano-drug delivery system and a technology for chemotherapeutic drugs, applied in the field of biomedicine, can solve problems such as nano-drug delivery systems of curcumin and chemotherapeutic drugs, etc.

Active Publication Date: 2021-05-28
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, there are no relevant reports on nano drug delivery systems that release curcumin and chemotherapeutic drugs sequentially

Method used

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  • A nano-drug delivery system for time-sequential release of curcumin and chemotherapeutic drugs and its application
  • A nano-drug delivery system for time-sequential release of curcumin and chemotherapeutic drugs and its application
  • A nano-drug delivery system for time-sequential release of curcumin and chemotherapeutic drugs and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Example 1 Biotin-modified time-sequential release of curcumin and paclitaxel nano drug delivery system

[0042] Taking the biotin-modified time-sequential release curcumin and paclitaxel nano-delivery system as an example to illustrate its construction process, time-sequential release effect evaluation and anti-MCF-7 / ADR drug-resistant tumor effect:

[0043] 1. Construction of nano drug delivery system

[0044] Take 10 mM PEG (molecular weight about 2000) with Biotin at one end and carboxyl group at the other end, dissolve it in 50 mL of anhydrous dichloromethane, then add 10 mM paclitaxel (PTX), 11 mM N,N'-dicyclohexylcarbodi imine (DCC) and 1.1 mM 4-dimethylaminopyridine (DMAP), stirred at room temperature for three days, filtered, added anhydrous ether to precipitate, and dried in vacuum to obtain Biotin-modified PEGylated paclitaxel (Biotin-PEG- PTX). Dissolve 5 mM Biotin-PEG-PTX and 1 mM curcumin (Cur) in 20 mL of dichloromethane, evaporate the methylene chloride...

Embodiment 2

[0054] Example 2 Neuropeptide analog (PNBL-NPY) modified nano drug delivery system with tumor targeting and time-sequential release of curcumin and docetaxel

[0055] Taking the neuropeptide analog (PNBL-NPY) modified nano drug delivery system with tumor targeting and time sequence release of curcumin and docetaxel as an example to illustrate its construction process, time sequence release effect evaluation and anti-MCF-7 / ADR resistance The effect of medicine on tumor:

[0056] 1. Construction of nano drug delivery system

[0057] Take 10 mM PEG (molecular weight about 2000) with a maleimide group at one end and a carboxyl group at the other end, dissolve it in 60 mL of anhydrous dichloromethane, then add 10 mM docetaxel (DTX), 11 mM MDCC and 1.1 mM DMAP, stirred and reacted at room temperature for three days, filtered, added anhydrous ether to precipitate, and dried in vacuum to obtain docetaxel (Mal-PEG-DTX) with one end PEGylated with a maleimide group. Dissolve 5 mMMal-P...

Embodiment 3

[0067] Example 3 Acid-activated membrane-penetrating peptide (pHLIP) modified nano drug delivery system with tumor targeting and time-sequential release of curcumin and paclitaxel

[0068] Taking acid-activated membrane-penetrating peptide (pHLIP) modified nano-drug delivery system with tumor targeting and time-sequential release of curcumin and paclitaxel as an example to illustrate its construction process, evaluation of time-sequential release effect and anti-MCF-7 / ADR drug-resistant tumor effect :

[0069] 1. Construction of nano drug delivery system

[0070] Take 10 mM PEG (molecular weight about 1000) with a maleimide group at one end and a carboxyl group at the other end, dissolve it in 60 mL of anhydrous dichloromethane, then add 10 mM paclitaxel (PTX), 11 mM DCC and 1.1 mM DMAP was reacted with stirring at room temperature for three days, filtered, precipitated by adding anhydrous ether, and vacuum-dried to obtain paclitaxel (Mal-PEG-PTX) with maleimide-based PEGylat...

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Abstract

The invention discloses a nano drug delivery system with time sequence release of curcumin and chemotherapeutic drugs and its application in anti-tumor. The present invention uses PEG to modify chemotherapy drugs to form amphiphilic conjugates, and then wraps curcumin to form a nano drug delivery system. The nano drug delivery system has the function of releasing drugs in time sequence, and can release curcumin and chemotherapy drugs in chronological order. , the timing release nano drug delivery system can be further modified with tumor cell-specific target molecules to obtain the functions of passive targeting, active targeting, and timing release of drugs. It has excellent characteristics such as anti-drug resistant tumors, and has Good prospects for clinical application.

Description

technical field [0001] The invention belongs to the technical field of biomedicine. More specifically, it relates to a nano drug delivery system and its application for sequentially releasing curcumin and chemotherapeutic drugs. Background technique [0002] Tumor drug resistance, also known as tumor drug resistance, refers to the tolerance of tumor cells to the effects of chemotherapeutic drugs. Once drug resistance occurs, the chemotherapeutic effect of the drug will decrease significantly, or even have no effect. Tumor drug resistance is the biggest obstacle to clinical tumor chemotherapy, and it is also one of the main reasons for the failure of chemotherapy. The emergence of tumor drug resistance has greatly reduced the number of chemotherapy drugs that can be selected clinically. Therefore, how to overcome and reverse the drug resistance of tumor cells The drug resistance of related chemotherapeutic drugs has become an urgent clinical problem to be solved. [0003] C...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/60A61K31/12A61K45/00A61K47/10A61K9/51A61K9/127A61K9/107A61P35/00
CPCA61K9/1075A61K9/1271A61K9/5146A61K31/12A61K45/00A61K47/10A61K2300/00
Inventor 吕立李国成伍俊妍邱凯锋石永辉
Owner SUN YAT SEN UNIV
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