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Mitochondrion-targeting nano-drug delivery system and preparation method and application thereof

A nano-drug and delivery system technology, applied in drug combinations, pharmaceutical formulations, medical preparations with non-active ingredients, etc., can solve problems such as few researches, and achieve good biocompatibility, good stability, and uniform particle size. Effect

Active Publication Date: 2016-08-10
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For example, pH-sensitive, reduction-sensitive, temperature-sensitive, enzyme-sensitive, and light-sensitive, etc., but drug release in response to ROS has rarely been studied

Method used

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  • Mitochondrion-targeting nano-drug delivery system and preparation method and application thereof
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  • Mitochondrion-targeting nano-drug delivery system and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] 1. The steps for synthesizing ROS-sensitive thioketal linker (TL) are as follows:

[0057] Anhydrous 3-mercaptopropionic acid (5.2g, 49.1mmol) and anhydrous acetone (5.8g, 98.2mmol) were saturated with dry HCl gas and reacted at room temperature for 4h. The reaction product was crystallized, filtered, washed with hexane and cold water, and vacuum freeze-dried with thiol linker to obtain the product.

[0058] 2. The experimental steps of synthesizing TL-CPT are as follows:

[0059] TL (252.1mg, 1.0mmol) was dissolved in anhydrous 10mL DMF, followed by adding triethylamine (TEA, 3.0mmol), 2,4,6-trichlorobenzoyl chloride (241.9mg, 1.0mmol), dimethyl Aminopyridine (DMAP, 24.4 mg, 0.2 mmol), stirred for 10 min. Camptothecin (CPT, 174.1 mg, 0.5 mmol) dissolved in 10 mL of DMF was then added, and the reaction was stirred at room temperature for 24 h. Quench the reaction with water and CH 2 Cl 2 Extract 5 times. The crude product was passed through a silica gel column to ...

Embodiment 2

[0076] 1. The synthesis steps of the ROS-sensitive thioketal linker (TL) are the same as in Example 1, and will not be repeated here.

[0077] 2. The experimental steps of synthesizing TL-DOX are as follows:

[0078] TL (252.1mg, 1.0mmol) was dissolved in anhydrous 10mL DMF, followed by adding triethylamine (TEA, 303.6mg, 3.0mmol), 2,4,6-trichlorobenzoyl chloride (241.9mg, 1.0mmol) , Dimethylaminopyridine (DMAP, 24.4 mg, 0.2 mmol), stirred for 10 min. Doxorubicin (DOX, 271.76mg, 0.5mmol) dissolved in 10mL of DMF was added, and the reaction was stirred at room temperature for 24h. The reaction was quenched with water, and the crude product was passed through a silica gel column to obtain pure product.

[0079] 3. The steps for connecting TL-DOX to the amino group at one end of polyethylene glycol are the same as those in Example 1, and will not be repeated here.

[0080] 4. The modification steps of triphenylphosphine are the same as those in Example 1, and will not be repea...

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Abstract

The invention discloses a mitochondrion-targeting nano-drug delivery system, comprising polyethylene glycol connected with TPP and thioketal linker connected with a chemotherapeutic drug, the polyethylene glycol and the thioketal linker are connected with each other through amino and carboxyl condensation. This system also comprises DSPE-PEG and a photosensitizer; the chemotherapeutic drug forms a hydrophobic core inside, a hydrophilic shell layer is formed in the center of the polyethylene glycol, a mitochondrion-targeting crown is formed outside the TPP, and the photosensitizer is of hydrophobic structure distributed inside the core and / or around the core. TPP is selectively positioned to mitochondrion. This system is ROS responsive, the photosensitizer is laser excited to release ROS, and ROS cuts the thioketal linker to release the chemotherapeutic drug and can carry out photodynamic therapy at the same time, thus enabling synergic therapy of mitochondrion-targeting photodynamic therapy and chemotherapy. The invention also discloses a preparation method and application of the mitochondrion-targeting nano-drug delivery system.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a mitochondria-targeted nano drug delivery system and its preparation method and application. Background technique [0002] Mitochondria are the main place for cells to carry out aerobic respiration. They are called "power houses" and their diameters are about 0.5 to 1.0 microns. Mitochondria also play an important role in cell apoptosis. Mitochondrial dysfunction has an important relationship with the occurrence and development of tumors. Photodynamic therapy is the conversion of light energy into chemical energy by photosensitizers—reactive oxygen radicals (abbreviated as ROS). singlet oxygen ( 1 O2), as a kind of ROS, is most commonly used in photodynamic therapy, but its residence time in the living body is very short (<0.1ms), and its diffusion radius is small (<20nm). Therefore, in photodynamic therapy, the photosensitizer must be close enough to the tre...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K45/06A61K41/00A61P35/00A61K31/4745A61K31/704A61K31/337
CPCA61K31/337A61K31/4745A61K31/704A61K41/0071A61K45/06
Inventor 崔大祥岳彩霞杨宇明
Owner SHANGHAI JIAO TONG UNIV
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