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Folate receptor-mediated paclitaxel-hydroxycamptothecin superparamagnetic iron oxide nanoparticle as well as preparation method and application thereof

A technology of superparamagnetic iron oxide and hydroxycamptothecin, which is applied in the field of medicine, can solve the problems of grafting and the common occurrence of two antitumor drugs, and achieve the effect of enhancing cytotoxicity

Active Publication Date: 2021-08-17
GUILIN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the current nanoparticles can only be grafted with a single drug, and there has been no report on the co-grafting of two anti-tumor drugs at the same time

Method used

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  • Folate receptor-mediated paclitaxel-hydroxycamptothecin superparamagnetic iron oxide nanoparticle as well as preparation method and application thereof
  • Folate receptor-mediated paclitaxel-hydroxycamptothecin superparamagnetic iron oxide nanoparticle as well as preparation method and application thereof
  • Folate receptor-mediated paclitaxel-hydroxycamptothecin superparamagnetic iron oxide nanoparticle as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] The folic acid receptor mediating paclitaxel and hydroxycamptothecin superparamagnetic iron oxide nanoparticles of the present invention comprises the following steps:

[0062] A. Graft FA on the surface of PEG / PEI-SPIONs nanoparticles to obtain FA@PEG / PEI-SPIONs:

[0063] Mix PEG-1000 and PEI-1800 evenly, and raise the temperature to 78°C within 8 minutes to obtain a mixed solution; Fe(acac) 3 Add it to the mixture, continue stirring at 78°C for 8 minutes, heat to 250°C, keep warm for 0.5h, stop heating, cool to 50°C to obtain a mixture containing PEG / PEI-SPIONs; add PEG / PEI-SPIONs Add toluene to the nanoparticle mixture for ultrasonic dispersion, and use a magnet to adsorb at the bottom of the beaker. When the black magnetic substance is basically absorbed to the bottom of the beaker, discard the supernatant and repeat the cleaning process once. The black precipitate is reused. Wash with acetone once to obtain PEG / PEI-SPIONs nanoparticles; the PEG-1000, PEI-1800, Fe(...

Embodiment 2

[0073] The folic acid receptor mediating paclitaxel and hydroxycamptothecin superparamagnetic iron oxide nanoparticles of the present invention comprises the following steps:

[0074] A. Graft FA on the surface of PEG / PEI-SPIONs nanoparticles to obtain FA@PEG / PEI-SPIONs:

[0075] Mix PEG-1000 and PEI-1800 evenly, and raise the temperature to 82°C within 12 minutes to obtain a mixed solution; Fe(acac) 3 Add to the mixture, continue to stir at 82°C for 12min, heat to 270°C, keep warm for 1.5h, stop heating, cool to 70°C to obtain a mixture containing PEG / PEI-SPIONs; add PEG / PEI-SPIONs Add toluene to the nanoparticle mixture for ultrasonic dispersion, and use a magnet to adsorb at the bottom of the beaker. When the black magnetic substance is basically absorbed to the bottom of the beaker, discard the supernatant and repeat the cleaning process for 3 times. The black precipitate is reused. Acetone was washed 3 times to obtain PEG / PEI-SPIONs nanoparticles; the PEG-1000, PEI-1800,...

Embodiment 3

[0085] The folic acid receptor mediating paclitaxel and hydroxycamptothecin superparamagnetic iron oxide nanoparticles of the present invention comprises the following steps:

[0086] A. Graft FA on the surface of PEG / PEI-SPIONs nanoparticles to obtain FA@PEG / PEI-SPIONs:

[0087] Mix PEG-1000 and PEI-1800 evenly, and heat up to 80°C within 10 minutes to obtain a mixed solution; Fe(acac) 3Add it into the mixture, continue stirring at 80°C for 10 minutes, heat to 260°C, stop heating after 1 hour of heat preservation, and cool to 60°C to obtain a mixture containing PEG / PEI-SPIONs; add PEG / PEI-SPIONs to nano Add toluene to the mixture of granules for ultrasonic dispersion, and use a magnet to adsorb at the bottom of the beaker. When the black magnetic substance is basically absorbed to the bottom of the beaker, discard the supernatant and repeat the cleaning process twice. Wash 2 times to obtain PEG / PEI-SPIONs nanoparticles; the PEG-1000, PEI-1800, Fe(acac) 3 The mass ratio is 1...

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Abstract

The invention discloses a folate receptor-mediated paclitaxel-hydroxycamptothecin superparamagnetic iron oxide nanoparticle and a preparation method thereof. The nanoparticle is p-PS / FA@PEG / PEI-SPIONs@PTX + HCPT . A drug-loaded nanoparticle system disclosed by the invention has a synergistic effect, can enhance anti-tumor effect, has small toxic and side effects, and is a nanoparticle preparation with a great development value for treating tumors.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a folic acid receptor-mediated paclitaxel and hydroxycamptothecin superparamagnetic iron oxide nanoparticle and a preparation method thereof. Background technique [0002] One of the biggest killers that threaten human life and health is tumor. Chemical drugs are an indispensable means of treating nasopharyngeal carcinoma. However, chemical drugs are non-specific to cancerous cells and normal human cells, so that they not only kill cancerous cells during treatment, but also It also kills normal cells, causing serious toxic and side effects throughout the body. In recent years, searching for safe and effective targeted drugs has become a hotspot in the treatment of tumors. [0003] The nano drug delivery system can realize the control of drug delivery and release at the molecular level, and the passive or active targeting of the drug at the tumor site can be achieved ...

Claims

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Application Information

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IPC IPC(8): A61K47/60A61K47/54A61K47/52A61K47/69A61K31/4745A61K31/337A61P35/00A61P11/02A61P11/04B82Y5/00B82Y40/00
CPCA61K47/60A61K47/545A61K47/52A61K47/6935A61K47/6929A61K31/4745A61K31/337A61P35/00A61P11/02A61P11/04B82Y5/00B82Y40/00A61K2300/00
Inventor 徐勤贵刚范子琪张宝林
Owner GUILIN MEDICAL UNIVERSITY
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