Preparation of nanoparticles with targeting or photo-thermal function based on polytannic acid modification technology

A polytannic acid and nanoparticle technology, applied in the field of medicine, can solve problems such as poor water solubility, lack of specific selectivity, and clinical application constraints, and achieve the effects of stable performance, simple operation, and safe and non-toxic raw materials

Pending Publication Date: 2022-02-22
BEIJING UNIV OF CHINESE MEDICINE
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Chemotherapy is one of the traditional treatment methods for tumor treatment at present, but most chemotherapeutic drugs, such as paclitaxel

Method used

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  • Preparation of nanoparticles with targeting or photo-thermal function based on polytannic acid modification technology
  • Preparation of nanoparticles with targeting or photo-thermal function based on polytannic acid modification technology
  • Preparation of nanoparticles with targeting or photo-thermal function based on polytannic acid modification technology

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0032] Example 1 Preparation of Nanoparticles with Photothermal Function Based on Polytannic Acid Modification Technology

[0033] 1) Preparation of PNCs

[0034]First, add 3 mL of dichloromethane to 6 mg of paclitaxel and 24 mg of surfactant poloxamer (F127), dissolve them completely, and transfer them to an eggplant-shaped flask. The solvent was removed by rotary evaporation to obtain a thin film of paclitaxel and F127 mixture. Then add 6 mL of deionized water for 3 hours of hydration. After paclitaxel was precipitated in the form of crystals, ultrasonic crushing was performed using an ultrasonic cell disruptor in an ice-water bath (power: 150W; frequency: 2s on, 2s off; duration: 15min) to obtain nano-scale paclitaxel nanosuspension. Finally, the precipitate was collected by centrifugation (14000rpm, 15min) to obtain purified PNC.

[0035] 2) Preparation of PNC-pTA

[0036] The purified PNC prepared in 1) was dispersed into 1.5 mL of N-biglycine buffer solution (10 mM, ...

Example Embodiment

[0037] Example 2 Preparation of nanoparticles with tumor targeting function based on polytannic acid modification technology

[0038] 1) Preparation of PNCs

[0039] First, add 3 mL of dichloromethane to 6 mg of paclitaxel and 24 mg of surfactant poloxamer (F127), dissolve them completely, and transfer them to an eggplant-shaped flask. The solvent was removed by rotary evaporation to obtain a thin film of paclitaxel and F127 mixture. Then add 6 mL of deionized water for 3 hours of hydration. After paclitaxel was precipitated in the form of crystals, ultrasonic crushing was performed using an ultrasonic cell disruptor in an ice-water bath (power: 150W; frequency: 2s on, 2s off; duration: 15min) to obtain nano-scale paclitaxel nanosuspension. Finally, the precipitate was collected by centrifugation (14000rpm, 15min) to obtain purified PNC.

[0040] 2) Preparation of PNC-pTA

[0041] The purified PNC prepared in 1) was dispersed into 1.5 mL of N-biglycine buffer solution (10 ...

Example Embodiment

[0044] Example 3 Zeta potential characterization of nanoparticles

[0045] In this example, the PNC and PNC-pTA prepared in Example 1 and the PNC-pTA-cRGD prepared in Example 2 were morphologically characterized as follows:

[0046] Disperse 1-2 drops of PNC, PNC-pTA and PNC-pTA-cRGD suspensions in 1mL phosphate buffer solution (10mM, pH=7.4), and use the Malvern laser particle size analyzer to investigate the Zeta potential of each nanoparticle . Measured in parallel three times. The surface potential of PNC is -1.66±0.27mV, which is close to electrical neutrality. After coating pTA, the potential drops to -26.23±0.59mV, which proves that pTA has been coated. The specific results are shown in Table 1.

[0047] Table 1 Zeta potential measurement results of different samples (n=3)

[0048]

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Abstract

The invention belongs to the technical field of medicines, and relates to a preparation method of nanoparticles with a targeting or photo-thermal function based on a tannic acid modification technology and application of the nanoparticles in tumor targeting and photo-thermal therapy. Firstly, paclitaxel nanocrystals (PNC) are prepared. The tannic acid can quickly form a poly-tannic acid molecular layer (pTA) on the surface of the nanocrystal under the action of ferric iron, and the paclitaxel nanocrystal (PNC-pTA) with a photo-thermal therapy effect is obtained. The paclitaxel nanocrystal PNC-pTA-cRGD with a tumor targeting effect can be obtained by further stably modifying a targeting ligand with an amino group or a sulfydryl group, such as cRGD, on the surface of the nanoparticle by utilizing pTA. The pTA-based nanoparticle surface modification method provided by the invention is simple and reliable, the obtained product is stable in performance, the raw materials are safe, and the pTA-based nanoparticle surface modification method is an innovation in the aspects of photothermal and chemotherapy combined therapy and drug tumor targeted delivery, and has huge economic and social benefits.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a preparation method of nanoparticles based on tannic acid modification technology and its application in tumor targeting and photothermal therapy. Background technique [0002] According to reports, due to aging and population growth, the number of new cancer cases in the world will increase from 18.1 million in 2018 to 29.4 million in 2040. Cancer has become a major threat to human health. [0003] Tannic acid (TA) is a polyphenol with a large number of hydroxyl groups in its structure, and it can form a polytannic acid molecular layer (pTA) to coat the surface of nanoparticles with the participation of Fe3+. The molecular layer can chemically modify the targeting groups containing amino or sulfhydryl groups on the surface of nanoparticles through Michael addition or Schiff base reaction, and can be physically connected by electrostatic force, hydrogen bond and hyd...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K47/64A61K41/00A61K31/337A61P35/00
CPCA61K47/6935A61K47/64A61K41/0052A61K31/337A61P35/00A61K2300/00
Inventor 韩宁黄星月
Owner BEIJING UNIV OF CHINESE MEDICINE
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