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评估纳米颗粒的药物释放:通过使用新型光学技术和数学模型克服透析的缺点。

Assessing the drug release from nanoparticles: Overcoming the shortcomings of dialysis by using novel optical techniques and a mathematical model.

机构信息

Institute of Biophysics, Goethe University, Max-von-Laue-Str. 1, 60438 Frankfurt (Main), Germany.

Institute of Pharmaceutical Technology, Goethe University, Max-von-Laue-Str. 9, 60438 Frankfurt (Main), Germany.

出版信息

Int J Pharm. 2015 Jul 5;488(1-2):108-19. doi: 10.1016/j.ijpharm.2015.03.080. Epub 2015 Apr 4.

Abstract

The aim of the present investigation was to develop a reliable method which can be applied to the measurement of in vitro drug release from nanocarriers. Since the limited membrane transport is one major obstacle to the assessment of drug release with dialysis techniques, the determination of this parameter was our objective. Therefore, a novel drug release automatic monitoring system (DREAMS) was designed to conduct continuous measurements during the dialysis process. Moreover, a mathematical model was used for evaluation of the experimental data. This combination of mathematical and analytical tools enabled the quantification of the total amount of free drug in the system. Eudragit(®) RS 100 nanoparticles loaded with the model compound 5,10,15,20-tetrakis(m-hydroxypheny)chlorin (mTHPC) were investigated and the drug release was continuously monitored by using a fluorescence spectrometer that is part of the setup. Free drug and drug-loaded nanoparticles were tested to discriminate between the two formulations. In addition, two types of membranes composed of different materials were evaluated and the kinetics of membrane transport was determined. The data obtained from the apparatus were further treated by a mathematical model, which yielded distinguishable release profiles between samples of different compositions. The method offers a promising option for release testing of nanoparticles.

摘要

本研究旨在开发一种可靠的方法,可用于测量纳米载体中药物的体外释放。由于有限的膜转运是评估透析技术中药物释放的主要障碍之一,因此我们的目标是确定这个参数。因此,设计了一种新型药物释放自动监测系统(DREAMS),以在透析过程中进行连续测量。此外,还使用了数学模型来评估实验数据。这种数学和分析工具的结合能够定量系统中游离药物的总量。研究了载有模型化合物 5,10,15,20-四(间-羟苯基)氯(卟啉 mTHPC)的 Eudragit(®) RS 100 纳米粒子,并使用荧光光谱仪连续监测药物释放,该荧光光谱仪是该装置的一部分。测试了游离药物和载药纳米粒子,以区分两种制剂。此外,还评估了由不同材料组成的两种类型的膜,并确定了膜转运的动力学。通过数学模型进一步处理从仪器获得的数据,该模型在不同组成的样品之间产生了可区分的释放曲线。该方法为纳米粒子的释放测试提供了一种有前途的选择。

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