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IR820 and atorvaquone carrier-free self-assembled nanoparticles and preparation method and application thereof

A technology of IR820 and atovaquone, which is applied in the field of medicine, can solve the problems of low bioavailability and easy removal of hydrophilic drug IR820, and achieve good biocompatibility, improved photothermal treatment effect, and uniform particle size

Active Publication Date: 2021-06-11
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The present invention co-assembles the hydrophilic drug IR820 and the hydrophobic drug atovaquone, thereby solving the problems of poor water solubility of atovaquone and low bioavailability and easy removal of the hydrophilic drug IR820 in vivo, and at the same time solving the problem of IR820 in photothermal therapy Therapeutic resistance due to elevated heat shock proteins enables more efficient photothermal anti-tumor therapy

Method used

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  • IR820 and atorvaquone carrier-free self-assembled nanoparticles and preparation method and application thereof
  • IR820 and atorvaquone carrier-free self-assembled nanoparticles and preparation method and application thereof
  • IR820 and atorvaquone carrier-free self-assembled nanoparticles and preparation method and application thereof

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preparation example Construction

[0034] In yet another specific embodiment of the present invention, the preparation method of the above-mentioned nanoparticles is provided, the preparation method comprising: dissolving IR820 in water, dissolving atovaquone in an organic solvent, adding the atovaquone organic solvent solution into the IR820 aqueous solution , stirred, dialyzed, passed through a membrane, and obtained.

[0035] Wherein, the organic solvent can be selected from one or more of dimethyl sulfoxide, methanol, ethanol, dichloromethane, acetonitrile, ethyl acetate, etc., and the inventors have found that only dimethyl sulfoxide Sulfone can achieve good solubility of atovaquone, so the solvent is finally preferably dimethyl sulfoxide.

[0036] In the above preparation process, IR820, atovaquone dissolved in a solvent, and the mixing of the two solutions must be carried out under dark conditions.

[0037] In yet another specific embodiment of the present invention, the concentration of IR820 in the IR...

Embodiment 1

[0052] Example 1 Preparation of IR820 / ATO nanoparticles

[0053] Precisely weigh a certain amount of atovaquone with an analytical balance and disperse it in dimethyl sulfoxide (DMSO) to make a 10 mg / mL solution, and take a certain amount of IR820 and disperse it in water to make a 0.5 mg / mL solution. Slowly drop the DMSO solution of atovaquone into the aqueous solution of IR820 under rapid stirring conditions, and stir for 20 minutes to obtain a green solution. The mass ratio of atovaquone:IR820 is 2:1. After the reaction, dialyze with distilled water for 3 hours to remove unbound free drug and organic solvent, and pass through a 0.8 μm filter membrane. The UV spectrum of the nanoparticles is as figure 1 As shown, the particle size of nanoparticles is ~110nm, and its appearance and aggregation state are as follows figure 2 shown.

Embodiment 2

[0054] Example 2 Composition ratio of IR820 / ATO nanoparticles detected by ultraviolet spectrophotometry (UV)

[0055] Precisely measure 1 volume of IR820 / ATO nanoparticle solution, add 10 volumes of dimethyl sulfoxide, and sonicate in an ice bath for 5 minutes to fully disintegrate the nanoparticle structure, dilute with distilled water: dimethyl sulfoxide = 1:10 solvent solution, dilute the above solution by an appropriate multiple. Using the solvent of distilled water: dimethyl sulfoxide = 1:10 as a blank reference, the absorbance was obtained by ultraviolet scanning. The results are as follows: figure 1 As shown, by calculating the absorbance values ​​of the diluent at 278nm and 833nm, it can be seen that the mass ratio of IR820:ATO drug in the newly prepared IR820 / ATO nanoparticles is close to 1:2, and the average encapsulation efficiency of the two drugs can reach More than 70%. By UV spectrum ( figure 1 ) can confirm the successful preparation of IR820 / ATO nanoparti...

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Abstract

The invention provides IR820 and atorvaquone carrier-free self-assembled nanoparticles and a preparation method and application thereof, and belongs to the technical field of medicines. According to the nanoparticle, IR820 and atorvaquone are taken as active ingredients, the nanoparticle not only solves the problems that IR820 is extremely easy to remove and poor in stability, but also solves the problems that atorvaquone is extremely poor in water solubility and low in bioavailability, and treatment resistance of IR820 is caused by rising of heat shock protein in photo-thermal therapy. The nanoparticle is high in drug loading capacity, uniform in particle size, high in stability and good in biocompatibility, provides more efficient photothermal therapy, can be used for treating or relieving benign tumors or malignant tumors, and therefore has good practical application value.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a carrier-free self-assembled nanoparticle of IR820 and atovaquone and its preparation method and application. Background technique [0002] The information disclosed in this background section is only intended to increase the understanding of the general background of the present invention, and is not necessarily taken as an acknowledgment or any form of suggestion that the information constitutes the prior art already known to those skilled in the art. [0003] Breast cancer is a malignant tumor that occurs in the glandular epithelial tissue of the mammary gland. In the advanced stage, cancer cells may metastasize to multiple organs and cause multiple organ lesions, which directly threaten the life of the patient. At present, chemotherapy, radiotherapy and surgery are the most commonly used cancer treatment methods in clinical practice, but these three methods have...

Claims

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Application Information

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IPC IPC(8): A61K41/00A61K31/122A61K9/14A61P35/00B82Y5/00B82Y40/00
CPCA61K41/0052A61K31/122A61K9/14A61P35/00B82Y5/00B82Y40/00A61K2300/00Y02A50/30
Inventor 栾玉霞杜倩姜悦
Owner SHANDONG UNIV
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