Department of Health Technology, Technical University of Denmark, Ørsteds Plads 345C, 2800 Kgs. Lyngby, Denmark.
Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, 2100 Copenhagen, Denmark.
Int J Pharm. 2019 Oct 30;570:118658. doi: 10.1016/j.ijpharm.2019.118658. Epub 2019 Sep 3.
Micro fabricated delivery systems have shown promise in increasing oral bioavailability of drugs. Micrometer-sized polymeric devices (microcontainers) have the potential to facilitate unidirectional drug release directly into the intestinal mucosa whereby, drug absorption can be enhanced. The aim of this study was to develop an ex vivo model to investigate mucosal adhesion and orientation of microcontainers. Furthermore, to investigate how microcontainers with varying height, shape and material behave in regards to mucoadhesion and orientation. Microcontainers were placed at the top of an inclined piece of porcine small intestine. The tissue was perfused with biorelevant medium followed by microscopic examination to observe the orientation and amount of microcontainers on the tissue. The mucoadhesion of the microcontainers were evaluated based on the observed position on the tissue after being exposed to flow. When comparing the varying types of microcontainers, good adhesion was in general observed since most of the microcontainers were located in the beginning of the intestine. Microcontainers fabricated from the epoxy-based photoresist SU-8 had a slightly better adherence than those fabricated from poly-ɛ-caprolactone (PCL). The orientation of the microcontainers appeare to be dictated mainly by the height. In general, the model showed promising results in evaluating mucoadhesion and orientation.
微制造的给药系统在提高药物的口服生物利用度方面显示出了前景。微米级的聚合物装置（微容器）有可能促进药物单向释放到肠黏膜中，从而增强药物吸收。本研究的目的是开发一种体外模型来研究微容器的黏膜黏附性和定向性。此外，还研究了不同高度、形状和材料的微容器在黏附性和定向性方面的表现。微容器被放置在猪小肠的倾斜部分的顶部。组织用生物相关介质灌注，然后进行显微镜检查，以观察组织上微容器的定向和数量。微容器的黏附性是根据暴露于流动后的组织上的观察位置来评估的。在比较不同类型的微容器时，由于大多数微容器位于肠的起始端，因此通常观察到良好的黏附性。由环氧树脂基光致抗蚀剂 SU-8 制成的微容器的黏附性略优于由聚己内酯（PCL）制成的微容器。微容器的定向似乎主要由高度决定。总的来说，该模型在评估黏附性和定向性方面显示出了有前途的结果。
