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Aptamer-modified targeted drug delivery nanoparticles as well as preparation method and application thereof

A drug-loaded nano-aptamer technology, which is applied in the direction of pharmaceutical formulations, medical preparations containing active ingredients, and medical preparations containing active ingredients, can solve the problem of insufficient specificity of photodynamic therapy and targeted delivery carriers poor specificity

Active Publication Date: 2018-03-06
FUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The present invention has obvious advantages over single drug therapy for the combination therapy of tumor chemotherapy and photodynamic therapy. Drug-loaded nanoparticles, which can exert the combined curative effect of chemotherapy / photodynamic therapy, and have the specific recognition ability of nucleic acid aptamers, can increase the targeted recognition ability of the drug delivery carrier for tumor cells, so as to realize the anti-cancer effect of tumor cells. Accurate dosing, accurate release of photosensitizer effect

Method used

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  • Aptamer-modified targeted drug delivery nanoparticles as well as preparation method and application thereof
  • Aptamer-modified targeted drug delivery nanoparticles as well as preparation method and application thereof
  • Aptamer-modified targeted drug delivery nanoparticles as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Take 1.0 g of cetylmethyltrimethylammonium bromide (CTAB), dissolve it in 480 mL of ultrapure water, stir continuously at 80 °C, then slowly add 3.5 mL of NaOH solution (2M) dropwise, and then add 5 mL TEOS (addition time should be longer than 10 min), continue to react at 80°C for 2 h; after the reaction, wait for the reaction solution to cool to room temperature, filter to obtain a white precipitate, wash with secondary water and methanol for 3 times, and disperse the precipitate in Heat and reflux in acidic ethanol (concentrated hydrochloric acid: ethanol = 5:1, v / v) for 24 hours, centrifuge after the reflux to remove the unreacted template agent CTAB, and freeze-dry the resulting solid to obtain white solid MSN-OH .

Embodiment 2

[0034] Take 1.0 g of MSN-OH obtained in Example 1, dissolve it in 30 mL of anhydrous toluene, stir continuously at 130 °C, then add 0.6 mL of 3-aminopropyltriethoxysilane (APTES) dropwise, and After the reaction, the reaction solution was cooled to room temperature, filtered, and the obtained solid was washed 3 times with toluene, and then the obtained solid material was dried to obtain MSN-NH 2 .

Embodiment 3

[0036] Add 7 mmoL carboxy-modified nucleic acid aptamer E-APt targeting EGFR, 8 mg EDC, and 8 mg NHS to 5 mL of ultrapure water, stir for 15 min, then add 10 mg of the MSN obtained in Example 2 -NH 2 , and continued stirring for 12 h; then the reaction mixture was centrifuged at 15,000 rpm for 10 min, the supernatant was removed, and dried to obtain E-MSN.

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Abstract

The invention discloses aptamer-modified targeted drug delivery nanoparticles as well as a preparation method and application thereof. The targeted drug delivery nanoparticles are nucleic acid aptamerin which by taking mesoporous silica nanoparticles as a vector, an anticancer drug and a photosensitizer are entrapped in channels of the mesoporous silica nanoparticles, and specific proteins whichcan recognize cancer cell surfaces are modified on the surfaces of the mesoporous silica nanoparticles. The targeted drug delivery nanoparticles can recognize tumor cells in a targeted manner, exertscombined curative effect of chemotherapy / photodynamic therapy and can be used for preparing an antitumor drug.

Description

technical field [0001] The invention belongs to the field of biomedicine, in particular to a nucleic acid aptamer-modified mesoporous silica drug-loaded nanoparticle loaded with anticancer drug doxorubicin (DOX) and photosensitizer hematoporphyrin (Hp) and its preparation methods and applications. Background technique [0002] Cancer is a disease that threatens global public health and is still incurable. The effect of single-drug chemotherapy for tumors often fails to achieve the ideal tumor treatment effect, and it is easy to lead to drug resistance. Therefore, the combination therapy of tumor drug chemotherapy and other anti-tumor treatment methods, such as photothermal therapy and photodynamic therapy, has obvious advantages. At the same time, there are many specific proteins on the surface of tumor cells, such as EGFR, EpCAM, HER2, etc., but these proteins are not expressed or expressed at a very low level in normal cells. Therefore, it can be used as a target for th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K41/00A61K31/704A61K47/54A61K47/69A61P35/00
CPCA61K31/704A61K41/0071A61K2300/00
Inventor 高瑜林晓文柯玲洁张英英雷桂财李冬梅方胤瑾陈海军
Owner FUZHOU UNIV
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