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Albumin-bound hypoxia-oxidation dual-responsive composite nanoparticles, preparation method and use

A technology of albumin-binding and nanoparticle, applied in the field of pharmaceutical preparations, can solve problems such as accelerating blood clearance and reducing long-term circulation effects, and achieve the effects of reducing toxicity, uniform particle size, and improving circulation time

Active Publication Date: 2022-06-24
CHINA PHARM UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the main strategy to increase the half-life of drugs in the blood is to use polyethylene glycol (PEG) and its derivatives to modify the drug delivery system, but long-term use of PEG will produce PEG antibodies, resulting in accelerated blood clearance (Accelerated Blood Clearance, ABC) phenomenon, reducing its long-cycle effect

Method used

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  • Albumin-bound hypoxia-oxidation dual-responsive composite nanoparticles, preparation method and use
  • Albumin-bound hypoxia-oxidation dual-responsive composite nanoparticles, preparation method and use
  • Albumin-bound hypoxia-oxidation dual-responsive composite nanoparticles, preparation method and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] Synthesis of Dihydroartemisinin Dimer Linked by Monosulfide Bond (DHA-S-DHA)

[0061] Weigh dihydroartemisinin (227.48 mg, 0.80 mmol) and dimethylaminopyridine (9.77 mg, 0.08 mmol) and dissolve them in anhydrous dichloromethane. Glycolic anhydride (126.85 mg, 0.96 mmol) was added dropwise to the above solution and the reaction was terminated after 4 h. The above reaction product was directly put into the next step, and 1-hydroxybenzotriazole (181.60 mg, 1.34 mmol) and N,N-diisopropylethylamine (352.02 μL, 2.13 mmol) were added, and stirred for 30 min under ice bath. , 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (204.16 mg, 1.06 mmol) was added to it, and stirring was continued for 1 h under ice bath. Subsequently, dihydroartemisinin (154.68 mg, 0.54 mmol) was dissolved in dichloromethane, added dropwise, reacted under an ice bath for 1 h, and then transferred to room temperature to continue the reaction overnight. After the reaction, it was washed thre...

Embodiment 2

[0064] Synthesis of Carbon Single Bonded Dihydroartemisinin Dimers (DHA-C-DHA)

[0065] Weigh dihydroartemisinin (227.48 mg, 0.80 mmol) and dimethylaminopyridine (9.77 mg, 0.08 mmol) and dissolve them in anhydrous dichloromethane. Acid anhydride (109.54 mg, 0.96 mmol) was added dropwise to the above solution, and the reaction was terminated after 4 h. The above reaction product was directly put into the next step, and 1-hydroxybenzotriazole (181.60 mg, 1.34 mmol) and N,N-diisopropylethylamine (352.02 μL, 2.13 mmol) were added, and stirred for 30 min under ice bath. , 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (204.16 mg, 1.06 mmol) was added to it, and stirring was continued for 1 h under ice bath. Subsequently, dihydroartemisinin (154.68 mg, 0.54 mmol) was dissolved in dichloromethane, added dropwise, reacted under an ice bath for 1 h, and then transferred to room temperature to continue the reaction overnight. After the reaction, it was washed three times ...

Embodiment 3

[0068] Synthesis of Polymer CMCTS-MAL&NI with Carboxymethyl Chitosan as Core

[0069] 2-Nitroimidazole (0.50 g, 4.43 mmol), ethyl 6-bromohexanoate (1.04 g, 4.65 mmol) and potassium carbonate (4.90 g, 35.40 mmol)) were dissolved in acetonitrile and heated at 60°C for 6 days. After the reaction is over, by adding an appropriate amount of K 2 CO 3 The pH of the resulting solution was adjusted to 7-8. The solvent was then evaporated to dryness in vacuo, appropriate amounts of ethyl acetate and water were added, and the two phases were separated by extraction. The organic phase was washed three times with water, dried over anhydrous sodium sulfate, filtered and evaporated to dryness to obtain ethyl-(2-nitroimidazolyl)hexanoic acid ethyl ester. Then, ethyl-(2-nitroimidazolyl)hexanoic acid ethyl ester (1.13 g, 4.43 mmol) was placed in concentrated hydrochloric acid and stirred vigorously at room temperature overnight. The solvent was evaporated to dryness in vacuo the next day to...

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Abstract

The present invention relates to an albumin-binding hypoxia-oxidation double-responsive composite nanoparticle, a preparation method and an application thereof. The composite nanoparticle is formed by self-assembling a dimer prodrug molecule and carrying a photosensitizer, and the dimer prodrug molecule The drug molecule is composed of two drug molecules with anti-tumor effect linked by ROS-sensitive bonds. The nanoparticles are simultaneously loaded with antitumor drugs and photosensitizers to achieve a synergistic therapeutic effect. The drug-loaded nanoparticles provide a new design idea for nano-drug delivery systems related to tumor treatment.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and particularly relates to an albumin-binding hypoxia-oxidative dual-responsive composite nanoparticle, a preparation method and an application. Background technique [0002] At present, the main treatment methods for lung cancer include surgery, chemotherapy and radiotherapy. Chemotherapy can effectively inhibit the development of tumors, and can improve the quality of life and prolong the survival period of patients of all stages. However, traditional chemotherapy drugs are highly cytotoxic. , low selectivity, while exerting anti-tumor efficacy, it will also damage some normal tissues, often accompanied by side effects such as bone marrow suppression and liver and kidney function damage. Photodynamic therapy (PDT), as a promising tumor treatment modality, is non-invasive, efficient and controllable, and produces relatively less pain and bleeding tendency. The current clinical applic...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/52A61K47/36A61K47/22A61K41/00A61K31/357A61P35/00
CPCA61K9/5161A61K9/5123A61K9/5192A61K41/0071A61K31/357A61P35/00A61K2300/00
Inventor 柳文媛冯锋骆仁杰曲玮张仲涛薛真
Owner CHINA PHARM UNIV
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