Nano-drug as well as preparation method and application thereof

A technology of nano-drugs and derivatives, applied in the direction of nano-drugs, nanotechnology, nanotechnology, etc., can solve the problems of low degree of drug response, limited effect of drug molecule fixed-point controlled release, etc., to achieve improved bioavailability, good hydrogen peroxide Response ability and acidic environment response ability, effect of increasing accumulation concentration

Active Publication Date: 2021-04-16
SICHUAN PROVINCIAL PEOPLES HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] The purpose of this application is to provide a nano-medicine, which aims to solve the problems of ...

Method used

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  • Nano-drug as well as preparation method and application thereof
  • Nano-drug as well as preparation method and application thereof
  • Nano-drug as well as preparation method and application thereof

Examples

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preparation example Construction

[0046] The embodiment of the present application also provides a preparation method of the above-mentioned nano-medicine, the preparation method of the nano-medicine comprises the following steps:

[0047] S01. Provide a cyclodextrin derivative and a polyhydroxy compound, the surface of the cyclodextrin derivative is modified with boronic acid groups, and the polyhydroxy compound contains at least two hydroxyl groups that are ortho or meta to each other;

[0048] S02, reacting the cyclodextrin derivative and the polyhydroxy compound, so that the hydroxyl group is connected to the boronic acid group to obtain a reaction product;

[0049] S03, dispersing the reaction product in an aqueous solution to assemble to form a nano drug.

[0050] Wherein, the types and properties of the cyclodextrin derivatives and polyols in step S01 refer to the cyclodextrin derivatives and polyols mentioned above, and will not be repeated here to save space.

[0051] Specifically, in step S02, the c...

Embodiment 1

[0064]In this example, a nanomedicine was prepared using 4-hydroxymethylphenylboronic acid-modified hydroxypropyl-β-cyclodextrin as a drug carrier and baicalein as a drug molecule. The preparation method includes the following steps:

[0065] 1. Preparation of 4-hydroxymethylphenylboronic acid-modified hydroxypropyl-β-cyclodextrin (cPBA)

[0066] Dissolve 199 mg of 4-hydroxymethylphenylboronic acid (PBA) and 213 mg of N,N'-carbonyldiimidazole (CDI) in anhydrous dichloromethane (DCM), stir for 1 hour and add 20 mL of dichloromethane and 30 mL of Deionized water was used for extraction, the organic phase was washed with saturated sodium chloride and dried with anhydrous sodium sulfate, and the organic phase was removed by rotary evaporation to obtain a CDI-activated PBA derivative (PBA-CDI). Then, under nitrogen protection, 725 mg of injection-grade hydroxypropyl-β-cyclodextrin (HP-β-CD) and 347 mg of PBA-CDI were dissolved in anhydrous dimethylformamide (DMF), and 250 μL of Af...

Embodiment 2

[0070] In this example, hydroxypropyl-β-cyclodextrin modified with 4-hydroxymethylphenylboronic acid is used as the drug carrier, and quercetin is used as the drug molecule to prepare a nano drug. The difference between the preparation method and Example 1 It mainly lies in the preparation steps of nanomedicine, including:

[0071] Dissolve 163mg of quercetin and 200mg of cPBA in 4mL of anhydrous DMSO containing molecular sieves to react overnight, slowly add the reaction solution into PBS buffer, then place the mixture in a dialysis bag, dialyze in deionized water, and then carry out Freeze dried.

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Abstract

The invention relates to the technical field of pharmaceutical preparations, and provides a nano-drug as well as a preparation method and application thereof. The nano-drug provided by the invention is mainly composed of a cyclodextrin derivative and a polyhydroxy compound, the surface of the cyclodextrin derivative is modified with a boric acid group, the polyhydroxy compound contains at least two hydroxyl groups which are in an ortho-position or in a meta-position of each other, wherein the hydroxyl groups are connected with the boric acid group through chemical bonds. The nano-drug has both hydrogen peroxide response capability and acid environment response capability, and can respond to an inflammatory microenvironment to rapidly release drug molecules after being transferred to a target site, so that the drug molecules are prevented from being released too early in an in-vivo delivery process. The nano-drug can be used as an injection medicine for preventing and treating inflammation-related diseases such as liver injury, asthma, myocardial infarction and atherosclerosis.

Description

technical field [0001] The application belongs to the technical field of pharmaceutical preparations, and in particular relates to a nano-medicine, a preparation method thereof, and an application of the nano-medicine. Background technique [0002] In recent years, nanomedicines including micelles, polymer nanoparticles, liposomes, nanocrystals, etc. have been widely used in the prevention, diagnosis, and treatment of various diseases. In particular, stimuli-responsive nanoparticles not only have the advantages of maintaining long-acting drugs, specific site targeting, and reducing drug side effects, but also have the ability to respond to physical and chemical changes in the surrounding environment (such as redox, pH, enzymes, Glucose, ion concentration, temperature, magnetic field, electric field, light, etc.) respond quickly to control the timing, fixed point, and quantitative release of drugs, so as to achieve long-acting, high efficiency, and low side effects. Therefore...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K47/54A61K45/00A61P1/16A61P9/10A61P11/06A61P29/00B82Y5/00B82Y30/00B82Y40/00
Inventor 张齐雄童荣生李姗姗郭坤
Owner SICHUAN PROVINCIAL PEOPLES HOSPITAL
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