Natural small molecule co-assembled nano-drug delivery system as well as preparation method and application thereof

A nano-drug and delivery system technology, applied in the field of nano-drug delivery system and its preparation, can solve the problems of limited natural small molecules, achieve good biocompatibility, slow systemic toxicity, and high tumor targeting effect

Pending Publication Date: 2020-09-08
HARBIN INST OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, so far, the natural small molecules that can be used for drug loading are very limited, because not all natural small molecules can self-assemble into drug carriers with specific shapes and sizes, and not all natural small molecules with self-assembly properties Has excellent pharmacological activity

Method used

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  • Natural small molecule co-assembled nano-drug delivery system as well as preparation method and application thereof
  • Natural small molecule co-assembled nano-drug delivery system as well as preparation method and application thereof
  • Natural small molecule co-assembled nano-drug delivery system as well as preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0056] This embodiment provides a natural small molecule co-assembled nanoparticle (NPs), the co-assembled nanoparticle is mainly prepared from Passepartout Acid (BTA) and paclitaxel (PTX). In this embodiment, the emulsified solvent volatilization method is used to prepare Passepartout acid-paclitaxel (BTA-PTX) nanoparticles, and the specific steps are as follows:

[0057] Dissolve 5 mg of Passepartout acid and 1.75 mg of paclitaxel in 1.0 mL of dichloromethane (if they cannot be completely dissolved, add a small amount of methanol as a co-solvent), and then add 3.0 mL of 2.5% polyvinyl alcohol (PVA ) aqueous solution (w / v), vortexed for 60 s, and immediately transferred the vortex liquid to a probe-type ultrasonic instrument to perform ultrasonic treatment on the mixture for 60 s. Then, the formed emulsion was added dropwise into 30 mL of 0.3% PVA aqueous solution (w / v) at a magnetic stirring speed of 400 rpm. The solution was stirred at room temperature for 6-8 hours to rem...

Embodiment 2

[0060] This example provides a natural small molecule co-assembled nanoparticle (NPs), which is mainly prepared from oleanolic acid (OA) and glycyrrhetinic acid (GA). In this embodiment, oleanolic acid-glycyrrhetinic acid (OA-GA) nanoparticles are prepared by emulsifying solvent evaporation method, and the specific steps are as follows:

[0061] Dissolve 2.5mg of oleanolic acid and 2.5mg of glycyrrhetinic acid in 1.0mL of dichloromethane (if they cannot be completely dissolved, add a small amount of methanol as a co-solvent), and then add them to 3.0mL of 2.5% polyethylene Alcohol (PVA) aqueous solution (w / v), vortexed for 60 s, and immediately transferred the vortex solution to a probe-type ultrasonic instrument for 60 s of ultrasonic treatment of the mixture. Then, the formed emulsion was added dropwise into 30 mL of 0.3% PVA aqueous solution (w / v) at a magnetic stirring speed of 400 rpm. The solution was stirred at room temperature for 6-8 hours to remove the organic solve...

Embodiment 3

[0064] This example provides a natural small molecule co-assembled nanoparticle (NPs), which is mainly prepared from betulin (Bet) and glycyrrhetinic acid (GA). In this embodiment, betulin-glycyrrhetinic acid (Bet-GA) nanoparticles are prepared by emulsifying solvent evaporation method, and the specific steps are as follows:

[0065] Dissolve 2.5 mg of betulin and 2.5 mg of glycyrrhetinic acid in 1.0 mL of dichloromethane (if they cannot be completely dissolved, a small amount of methanol can be added as a co-solvent), and then added to 3.0 mL of 2.5% polyvinyl alcohol ( PVA) aqueous solution (w / v), vortexed for 60 s, and immediately transferred the vortex liquid to a probe-type ultrasonic instrument to perform ultrasonic treatment on the mixture for 60 s. Then, the formed emulsion was added dropwise into 30 mL of 0.3% PVA aqueous solution (w / v) at a magnetic stirring speed of 400 rpm. The solution was stirred at room temperature for 6-8 hours to remove the organic solvent. ...

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Abstract

The invention discloses a natural small molecule co-assembled nano-drug delivery system as well as a preparation method and application thereof. The natural small molecule co-assembled nano-drug delivery system is a nano-particle formed by co-assembling two or more than two of oleanolic acid, ursolic acid, glycyrrhetinic acid, betulinic acid, betulin, liquidambaric acid, lupeol, paclitaxel, rheinic acid and catechinic. The original self-assembly morphology of a compound can be changed, nanoparticles with different morphologies and sizes are prepared, and the problem that the morphology of compounds is not suitable for intravenous injection is solved. The nano-drug delivery system disclosed by the invention has one or more pharmacological activities, the compounds forming the nano-drug delivery system play a synergistic anti-tumor role through different mechanisms, and the system has health-care functions and can be used for improving the oxidation resistance of an organism.

Description

technical field [0001] The invention belongs to the field of nanomedicine, and relates to a nanomedicine delivery system and its preparation method and application, in particular to a nanomedicine delivery system prepared by a co-assembly method with natural small molecules as a unit, as well as its preparation method and application. Background technique [0002] Cancer is a malignant disease that seriously threatens human health today. Traditional chemotherapy is still an indispensable treatment for most cancer patients, while most anticancer drugs have poor solubility, multidrug resistance and toxicity. The limitation of large side effects. The application of nanotechnology in medicine has been widely recognized, and the design and synthesis of efficient drug delivery systems are crucial for cancer treatment. At present, a series of nano drug delivery systems such as polymer micelles, nanoparticles, nanotubes, and nanogels have been established. However, the preparation...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/51A61K47/28A61K47/12A61K47/22A61K31/56A61K31/337A61K31/192A61K31/353A61P35/00A61P39/06A61P1/16A61P9/00A61P13/12
CPCA61K9/145A61K9/5123A61K31/192A61K31/337A61K31/353A61K31/56A61P1/16A61P9/00A61P13/12A61P35/00A61P39/06A61K2300/00
Inventor 杨鑫王嘉成乔文姝
Owner HARBIN INST OF TECH
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