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用于研究用于皮肤应用的纳米载体的不同体外释放方法的比较。

Comparison of different in vitro release methods used to investigate nanocarriers intended for dermal application.

作者信息

Balzus Benjamin, Colombo Miriam, Sahle Fitsum Feleke, Zoubari Gaith, Staufenbiel Sven, Bodmeier Roland

机构信息

College of Pharmacy, Freie Universität Berlin, Kelchstr. 31, 12169 Berlin, Germany.

College of Pharmacy, Freie Universität Berlin, Kelchstr. 31, 12169 Berlin, Germany.

出版信息

Int J Pharm. 2016 Nov 20;513(1-2):247-254. doi: 10.1016/j.ijpharm.2016.09.033. Epub 2016 Sep 11.

Abstract

In vitro drug release measurement is one of the most important methods used to assess the quality of a nanocarrier and estimate it́s in vivo performance. Different in vitro drug release methods have been used to investigate the drug release from nanocarriers, however, little information is available with regard to a comparison of these methods (e.g. discriminative power, reproducibility). Thus, drug release from four nanocarriers (nanocrystals, lipid nanoparticles, Eudragit RS and ethyl cellulose nanoparticles) was investigated under sink and non-sink conditions with three drug release methods: an in situ method using Sirius inForm and two in vitro methods using dialysis bags and Franz diffusion cells. Dexamethasone was used as the model drug. The in situ measurement was a simple and fast method but not adequately discriminating because of a too rapid drug dissolution/release. Franz diffusion cells and dialysis bags were in most cases discriminative for the different nanocarriers with the drug dissolution/release being in the order of nanocrystals>Eudragit RS nanoparticles>lipid nanoparticles>ethyl cellulose nanoparticles. Drug release experiments with Franz diffusion cells had the highest reproducibility. The Franz diffusion cells could also be easily used with semisolid dosage forms.

摘要

体外药物释放测定是评估纳米载体质量和估计其体内性能的最重要方法之一。已使用不同的体外药物释放方法来研究纳米载体的药物释放,然而,关于这些方法的比较(例如鉴别力、重现性)的信息很少。因此,采用三种药物释放方法,在漏槽和非漏槽条件下研究了四种纳米载体(纳米晶体、脂质纳米粒、Eudragit RS和乙基纤维素纳米粒)的药物释放:一种使用Sirius inForm的原位方法和两种使用透析袋和Franz扩散池的体外方法。地塞米松用作模型药物。原位测量是一种简单快速的方法,但由于药物溶解/释放过快而鉴别力不足。在大多数情况下,Franz扩散池和透析袋对不同的纳米载体具有鉴别力,药物溶解/释放顺序为纳米晶体>Eudragit RS纳米粒>脂质纳米粒>乙基纤维素纳米粒。使用Franz扩散池进行的药物释放实验具有最高的重现性。Franz扩散池也可轻松用于半固体制剂。

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