Hydrophobic drug nanometer capsule of pH response of near-infrared fluorescent trace and preparation method of hydrophobic drug nanometer capsule

A technology of hydrophobic drugs and nanocapsules, which is applied in the preparation of in vivo experiments, drug combinations, microcapsules, etc., can solve the problems of difficult penetration of animal tissues and long time for data collection, and achieve novel and simple preparation methods. The effect of strong fluorescent signal

Active Publication Date: 2015-06-24
BEIJING UNIV OF CHEM TECH
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  • Abstract
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  • Claims
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Problems solved by technology

However, the real-time tracking of drugs in the internal circulation process is often limited by the spatial or temporal resolution of the analysis method. For example, the general fluorescent probes used in fluorescence i

Method used

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  • Hydrophobic drug nanometer capsule of pH response of near-infrared fluorescent trace and preparation method of hydrophobic drug nanometer capsule
  • Hydrophobic drug nanometer capsule of pH response of near-infrared fluorescent trace and preparation method of hydrophobic drug nanometer capsule
  • Hydrophobic drug nanometer capsule of pH response of near-infrared fluorescent trace and preparation method of hydrophobic drug nanometer capsule

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Embodiment 1

[0021] A. the preparation method of oleylamine grafted polysuccinimide:

[0022] Add 1.6g polysuccinimide (PSI) into 32mL N,N-dimethylformamide and heat to 80°C for 1 hour until dissolved; then add 2.1mL oleylamine and maintain 100°C for 4 hours; finally add methanol to dissolve It is precipitated, centrifuged, and then dispersed in 8 mL of chloroform to obtain a chloroform solution of oleylamine grafted polysuccinimide;

[0023] b. Use oleylamine grafted polysuccinimide to encapsulate hydrophobic anticancer drugs and near-infrared fluorescent tracer materials into nanocapsules:

[0024] 5mg poly(ethylene-ethylene glycol), 50μL 0.05mmol / L surface chelated Ag of oleic acid 2 S nanoparticles in chloroform solution, 200 μL oleylamine grafted polysuccinimide in chloroform solution, 1.0 mg paclitaxel, 600 μL chloroform, 10 mL deionized water and 50 μL 0.1 mmol / L NaOH aqueous solution were mixed; 300W power Under ultrasonication for 6 minutes, the obtained emulsion was stirred at ...

Embodiment 2

[0029] A. the preparation method of oleylamine grafted polysuccinimide:

[0030] Add 1.6g polysuccinimide (PSI) into 32mL N,N-dimethylformamide and heat to 80°C for 1 hour until dissolved; then add 2.1mL oleylamine and maintain 100°C for 4 hours; finally add methanol to dissolve It is precipitated, centrifuged, and then dispersed in 8 mL of chloroform to obtain a chloroform solution of oleylamine grafted polysuccinimide;

[0031] b. Encapsulate hydrophobic anticancer drugs into nanocapsules by grafting polysuccinimide with oleylamine:

[0032] 5mg poly(ethylene-ethylene glycol), 50 μL 0.05mmol / L surface chelated Ag of dodecanethiol 2 S nanoparticles in chloroform, 200 μL 200 mg / mL oleylamine-grafted polysuccinimide in chloroform, 1.0 mg camptothecin, 600 μL chloroform, 10 mL deionized water and 50 μL 0.1 mmol / L NaOH Mix the aqueous solution; ultrasonicate for 6 minutes at 300W power, and stir the obtained emulsion at 55°C for 2 hours to evaporate chloroform; after the reacti...

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Abstract

The invention discloses a hydrophobic drug nanometer capsule of pH response of near-infrared fluorescent trace and a preparation method of the hydrophobic drug nanometer capsule and belongs to the technical field of preparation of nanometer materials. The hydrophobic drug nanometer capsule is applied to research of in-vivo imaging, cancer treatment and drug trace. The hydrophobic drug nanometer capsule of pH response of near-infrared fluorescent trace, which is wrapped with hydrophobic anticancer drugs and Ag2s nanometer particles, responds to pH (degraded in the acidic environment) and is in the diameter of 70-150 nm, has stable dispersibility in water phase, emits stable and strong near-infrared second-district fluorescent light under excitation of 808 nm, and can be used for tracing drug in real time in the blood circulation and the tumor position. The preparation method of the hydrophobic drug nanometer capsule is novel and simple, a drug carrier has cancer cell target and pH response characteristics as compared with a reported drug transport carrier and can emit near-infrared second-district fluorescent light, fluorescent signals are strong and can be used for tracing drug in real and identifying curative effect.

Description

technical field [0001] The invention belongs to the technical field of nanomaterial preparation, and in particular relates to the drug release of a pH-responsive hydrophobic drug nanocapsule and the biomedical application of near-infrared fluorescence tracking drug distribution in vivo. technical background [0002] Drug tracking is especially important for pharmacokinetic studies. However, the real-time tracking of drugs in the internal circulation process is often limited by the spatial or temporal resolution of the analysis method. For example, the general fluorescent probes used in fluorescence imaging emit visible light, which is difficult to penetrate animal tissues, while nuclear magnetic resonance imaging, CT, B-ultrasound and other imaging methods take a long time to collect data and are not real-time imaging. The near-infrared fluorescent probe Ag used in the near-infrared fluorescence imaging method 2 S nanoparticles emit near-infrared second region (1100-1400nm...

Claims

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Application Information

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IPC IPC(8): A61K49/00A61K9/51A61K47/34A61K47/42A61K31/337A61K31/4745A61P35/00
Inventor 汪乐余何倩黄盛
Owner BEIJING UNIV OF CHEM TECH
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