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Tumor-targeting nano-composite Apt-PAMAM/ERL/SUV and preparation and application thereof

A nano-composite, tumor-targeting technology, applied in the preparation of aptamer-modified drug-gene co-delivery nanoparticles, in the field of EGFR mutant lung cancer, to improve targeting, increase targeting, and enhance resistance. The effect of tumor effect

Inactive Publication Date: 2018-05-08
FUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Retrieval of relevant literature and patents at home and abroad shows that there is no report on the Apt-PAMAM / ERL / SUV nanocomposite with tumor targeting and its preparation method

Method used

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  • Tumor-targeting nano-composite Apt-PAMAM/ERL/SUV and preparation and application thereof
  • Tumor-targeting nano-composite Apt-PAMAM/ERL/SUV and preparation and application thereof
  • Tumor-targeting nano-composite Apt-PAMAM/ERL/SUV and preparation and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0034] Weigh 50 μL of an aqueous solution of Anti-EGFR aptamer (10 μM), add 10 μg of N-hydroxysuccinimide (NHS) and 2 μg of 1-(3-dimethylaminopropyl)-3-ethylcarbon Diimine hydrochloride (EDC) aqueous solution was stirred at room temperature for 3 h at low speed. Add 6 mg of the fourth-generation PAMAM (10 mg / mL) aqueous solution, stir overnight at room temperature at low speed, put it into a dialysis bag for dialysis for 2 days, and freeze-dry to obtain the Apt-PAMAM polymer (Apt-G4). Weigh 100 mg of Apt-G4 and 20 mg of erlotinib and dissolve them in 40 mL of anhydrous methanol, put them into a round bottom flask, seal and stir for 4 h. Methanol was removed by rotary evaporation, the sticky substance was dissolved in pure water, the precipitate was removed by centrifugation, and the supernatant was freeze-dried to obtain Apt-G4 / ERL nanomedicine. Weigh 100 μL of Apt-G4 / ERL nanomedicine (350 μg / mL) and add dropwise to 100 μL of Survivin shRNA (400 μg / mL) aqueous solution vortex...

Embodiment 2

[0036] Weigh 50 μL of an aqueous solution of Anti-EGFR aptamer (10 μM), add 10 μg of N-hydroxysuccinimide (NHS) and 2 μg of 1-(3-dimethylaminopropyl)-3-ethylcarbon Diimine hydrochloride (EDC) aqueous solution was stirred at room temperature for 3 h at low speed. Add 6 mg of the fifth-generation PAMAM (10 mg / mL) aqueous solution, stir overnight at room temperature at low speed, put it into a dialysis bag for dialysis for 2 days, and freeze-dry to obtain the Apt-PAMAM polymer (Apt-G5). Weigh 100 mg of Apt-G5 and 20 mg of erlotinib and dissolve them in 40 mL of anhydrous methanol, put them into a round bottom flask, seal and stir for 6 h. Methanol was removed by rotary evaporation, the sticky substance was dissolved in pure water, the precipitate was removed by centrifugation, and the supernatant was freeze-dried to obtain Apt-G5 / ERL nanomedicine. Weigh 100 μL Apt-G5 / ERL nanomedicine (350 μg / mL) and add dropwise to 100 μL Survivin shRNA (400 μg / mL) aqueous solution which is vort...

Embodiment 3

[0038] Weigh 100 μL of an aqueous solution of Anti-EGFR aptamer (10 μM), add 10 μg of N-hydroxysuccinimide (NHS) and 2 μg of 1-(3-dimethylaminopropyl)-3-ethylcarbon Diimine hydrochloride (EDC) aqueous solution was stirred at room temperature for 3 h at low speed. Add 6 mg of the sixth-generation PAMAM (10 mg / mL) aqueous solution, stir overnight at room temperature at low speed, put it into a dialysis bag for 2 days of dialysis, and freeze-dry to obtain the Apt-PAMAM polymer (Apt-G6). Weigh 100 mg of Apt-G6 and 20 mg of erlotinib and dissolve them in 40 mL of anhydrous methanol, put them into a round bottom flask, seal and stir for 6 h. Methanol was removed by rotary evaporation, the sticky substance was dissolved in pure water, the precipitate was removed by centrifugation, and the supernatant was freeze-dried to obtain Apt-G6 / ERL nanomedicine. Weigh 100 μL of Apt-G6 / ERL nanomedicine (350 μg / mL) and add dropwise to 100 μL of Survivin shRNA (400 μg / mL) aqueous solution vortexe...

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Abstract

The invention discloses a preparation method of tumor-targeting aptamer-modified drug gene co-transport nanoparticles and application of the nanoparticles in preparation of EGFR-mutation-resistant drugs for lung cancer. The preparation method comprises the specific steps that firstly, Apt carboxyl is activated first and then reacted with amino on the surface of PAMAM, an Apt-PAMAM carrier is synthesized, the drug ERL is encapsulated to form an Apt-PAMAM / ERL nano-drug, and the Apt-PAMAM / ERL nano-drug is compounded with SUV to form a tumor-targeting nano-composite. By means of the composite, thedefect that the ERL is poor in water solubility is overcome, and meanwhile, the surface-modified Apt and ERL dual-targeting EGFR mutation tumor cells are utilized so as to increase targeting of tumortissue; through compounding with the SUV, expression of anti-apoptosis genes is silenced, the drug resistance of the cells to the ERL is reversed, therefore, the bioavailability of the drug is effectively improved, and the clinical application value of the drug is improved.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and relates to a preparation method of an aptamer-modified drug-gene co-transport nanoparticle with tumor targeting and its effect on EGFR mutant lung cancer. Background technique [0002] Lung cancer is one of the malignant tumors with the fastest increasing morbidity and mortality and the greatest threat to the health and life of the population. Lung cancer is divided into small cell lung cancer (SCLC) and non-small cell lung cancer (NSCLC), of which NSCLC accounts for about 85% of all lung cancers, and the epidermal growth factor receptor (EGFR) mutation rate is as high as 40% (Ettinger DS, Bepler G, Bueno R, Chang A, Chang JY, Chirieac LR, et al. Non-small cell lung cancer clinical practice guidelines in oncology. Journal of the National Comprehensive Cancer Network: JNCCN. 2006;4:548-82). With the continuous progress of molecular genetics research, a variety of molecular targeted drugs ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K47/34A61K47/26A61K31/517A61K31/713A61K48/00A61P35/00
CPCA61K48/005A61K9/145A61K9/146A61K31/517A61K31/713A61K2300/00
Inventor 高瑜吕婷婷李子颖文一博张涛陈海军
Owner FUZHOU UNIV
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