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纳米载体药物负载量和释放动力学定量的通用方法。

General method for the quantification of drug loading and release kinetics of nanocarriers.

作者信息

Schwarzl Richard, Du Fang, Haag Rainer, Netz Roland R

机构信息

Freie Universität Berlin, Fachbereich Physik, 14195 Berlin, Germany.

Freie Universität Berlin, Institut für Chemie und Biochemie, 14195 Berlin, Germany.

出版信息

Eur J Pharm Biopharm. 2017 Jul;116:131-137. doi: 10.1016/j.ejpb.2016.12.015. Epub 2016 Dec 23.

Abstract

Macromolecular nanostructures that are used as drug carriers are characterized by their loading and release kinetics. Release studies commonly employ the dialysis method, in which a cellulose membrane separates the solution of released drug from the nanocarrier solution. We demonstrate that it is necessary to take the effect of the dialysis membrane on the release kinetics into account. Using a two-step approach, consisting of a calibration experiment of drug diffusion through the dialysis membrane in the absence of nanocarriers, and an experiment in the presence of nanocarriers, we are able to determine all kinetic rates and in particular to disentangle kinetic dialysis membrane properties from kinetic nanocarrier properties. We apply our general approach to experimental dexamethasone release data from core-multishell nanocarriers and demonstrate that our method yields a consistent description of the nanocarrier release kinetics.

摘要

用作药物载体的大分子纳米结构的特征在于其负载和释放动力学。释放研究通常采用透析法,其中纤维素膜将释放药物的溶液与纳米载体溶液分开。我们证明有必要考虑透析膜对释放动力学的影响。采用两步法,包括在不存在纳米载体的情况下药物通过透析膜扩散的校准实验以及在存在纳米载体的情况下的实验,我们能够确定所有动力学速率,特别是能够将动力学透析膜性质与动力学纳米载体性质区分开来。我们将我们的通用方法应用于来自核-多壳纳米载体的地塞米松实验释放数据,并证明我们的方法对纳米载体释放动力学给出了一致的描述。

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