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Nanoparticles containing anti-cancer drugs and preparation method and application thereof

A nanoparticle and anticancer drug technology is applied to the nanoparticle containing anticancer drug, and the preparation field thereof can solve the problems of low drug loading and low bioavailability of the nano drug-carrying system, and achieve uniform morphology and cycle time. Long, good therapeutic effect

Inactive Publication Date: 2014-03-12
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In order to overcome the problems of low bioavailability of anti-tumor hydrophobic drug molecules and low drug loading capacity of nano drug-loading systems, the present invention provides a nanoparticle containing anticancer drugs and a preparation method thereof. The nanoparticle has bioavailability High and high drug loading; the method is simple to operate, has a wide range of applications and strong universality, and the obtained nanoparticles have high stability and controllable morphology

Method used

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  • Nanoparticles containing anti-cancer drugs and preparation method and application thereof
  • Nanoparticles containing anti-cancer drugs and preparation method and application thereof
  • Nanoparticles containing anti-cancer drugs and preparation method and application thereof

Examples

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Effect test

Embodiment 1

[0038] Example 1: Preparation of nanoparticles comprising paclitaxel

[0039] Paclitaxel was dissolved in absolute ethanol to make a solution with a concentration of 50 mM, and 200 μL of the prepared paclitaxel absolute ethanol solution was added to 20 mL of deionized water, stirred magnetically at 25 °C for 5 min and then left to stand to obtain a precursor nanoparticle suspoemulsion.

[0040] Distearoylphosphatidylethanolamine-polyethylene glycol was formulated as a 5mg / mL aqueous solution.

[0041] Add 300 μL of 5 mg / mL distearoylphosphatidylethanolamine-polyethylene glycol aqueous solution into the precursor nanoparticle suspoemulsion, ultrasonically disperse for 5 minutes under the condition of ultrasonic power of 100%, and let it stand for 6 hours to prepare water Phase-dispersed nanoparticles comprising paclitaxel.

Embodiment 2

[0042] Example 2: Preparation of nanoparticles comprising docetaxel

[0043] Docetaxel was dissolved in tetrahydrofuran to prepare a solution with a concentration of 500 mM, and 50 μL of the prepared docetaxel tetrahydrofuran solution was added to 10 mL of deionized water, stirred magnetically at 25 °C for 30 min and then left to stand to obtain a precursor nanoparticle suspoemulsion.

[0044] Polylactic acid-polyethylene glycol was formulated into a 0.5 mg / mL aqueous solution.

[0045] Add 1mL of 0.5mg / mL polylactic acid-polyethylene glycol aqueous solution into the precursor nanoparticle suspoemulsion, ultrasonically disperse for 30min under the condition of ultrasonic power of 100%, and let it stand for 6h to prepare the aqueous phase dispersion containing Nanoparticles of docetaxel.

Embodiment 3

[0046] Example 3: Preparation of nanoparticles comprising 10-hydroxycamptothecin

[0047] Dissolve 10-hydroxycamptothecin in N,N-dimethylformamide to make a solution with a concentration of 1mM, take 500μL of the prepared 10-hydroxycamptothecin N,N-dimethylformamide solution and add it to 10mL In deionized water, stir magnetically at 20° C. for 1 min and then let stand to obtain precursor nanoparticle suspoemulsion.

[0048] Distearoylphosphatidylethanolamine-polyethylene glycol was formulated as a 10mg / mL aqueous solution.

[0049] Add 100 μL of 10 mg / mL distearoylphosphatidylethanolamine-polyethylene glycol aqueous solution into the precursor nanoparticle suspoemulsion, ultrasonically disperse for 1 min under the condition of ultrasonic power of 100%, and let it stand for 6 h to prepare water Phase-dispersed nanoparticles comprising 10-hydroxycamptothecin.

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Abstract

The invention relates to nanoparticles containing anti-cancer drugs and a preparation method and application thereof. The nanoparticles are rod-shaped and are prepared by the following process steps: preparing hydrophobic anti-cancer drug molecules into precursor nanoparticle suspension through a solvent exchange method, adding an aqueous solution of an amphiphilic surfactant into the precursor nanoparticle suspension, and performing ultrasonic treatment to obtain the nanoparticles coated with the amphiphilic surfactant. The nanoparticles has the characteristics of high bioavailability and high drug loading capacity; the method for preparing the nanoparticles is easy to operate, wide in application range and high in universality, and the nanoparticles are high in stability and controllable in appearance.

Description

technical field [0001] The invention relates to the technical field of nanoparticle pharmaceutical preparations, in particular to a nanoparticle containing anticancer drugs, its preparation method and application. Background technique [0002] The biological fluid environment is a hydrophilic environment, but hydrophobic and insoluble organic drug small molecules play a pivotal role in tumor therapy. Its insoluble problem leads to a series of problems such as the decrease of drug bioavailability, which greatly hinders its clinical application. [0003] In recent years, the use of micro-nanocarriers to disperse poorly water-soluble anticancer drugs has improved the bioavailability to a certain extent. Currently commonly used nanocarriers mainly include nanoparticles (Nanoparticles, NP), nanospheres (Nanospheres, NS), nanocapsules (Nanocapsules, NC), nanomicelles (Nanomicelle, NM), nanoliposomes (Nano-liposomes, NL ) and nanoemulsion (Nano-emulsion, NE), etc. These nano-car...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K45/00A61K47/34A61P35/00
Inventor 梁兴杰柳娟张晓宏李亚楠曹伟鹏
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA