Development and Evaluation of a Novel Mucus Diffusion Test System Approved by Self-Nanoemulsifying Drug Delivery Systems

作者：Friedl Heike; Duennhaupt Sarah; Hintzen Fabian; Waldner Claudia; Parikh Shruti; Pearson Jeffrey P; Wilcox Matthew D; Bernkop Schnuerch Andreas^*

来源：Journal of Pharmaceutical Sciences, 2013, 102(12): 4406-4413.

DOI：10.1002/jps.23757

• diffusion
• nanoparticles
• particle size
• self-emulsifying
• solubility
• surfactants

The aim of this study was the development of a novel mucus diffusion model and the approval thereof by self-nanoemulsifying drug delivery systems (SNEDDSs). For diffusion experiments, various SNEDD formulations were developed, spiked with fluorescein diacetate, and evaluated for their mucus diffusion behavior through an intestinal mucus layer within the novel setup. In brief, SNEDD formulations resulting in particle sizes of 12.0nm produced 70.3% of diffused model drug through the mucus layer. In comparison, SNEDDSs with particle sizes of 455.5nm led to a permeation of 8.3% only. Apart from this size dependence, two SNEDDS excipients namely Cremophor RH40 and triacetin were identified to strongly affect the permeation through mucus. Hence, it could be demonstrated that particle size and single excipients can positively influence mucus diffusion of SNEDDSs. Furthermore, it could be shown that the developed mucus diffusion model is a promising tool for pharmaceutical research in comparison with already established systems as it allows an easy handling coupled with the possibility to test different kinds of mucus in parallel within one setup.

• 出版日期2013-12