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From concept to in vivo testing: Microcontainers for oral drug delivery
Journal of Controlled Release ( IF 10.8 ) Pub Date : 2017-10-18 , DOI: 10.1016/j.jconrel.2017.10.013
Chiara Mazzoni , Fabio Tentor , Sophie Andersen Strindberg , Line Hagner Nielsen , Stephan Sylvest Keller , Tommy Sonne Alstrøm , Carsten Gundlach , Anette Müllertz , Paolo Marizza , Anja Boisen

This work explores the potential of polymeric micrometer sized devices (microcontainers) as oral drug delivery systems (DDS). Arrays of detachable microcontainers (D-MCs) were fabricated on a sacrificial layer to improve the handling and facilitate the collection of individual D-MCs. A model drug, ketoprofen, was loaded into the microcontainers using supercritical CO2 impregnation, followed by deposition of an enteric coating to protect the drug from the harsh gastric environment and to provide a fast release in the intestine. In vitro, in vivo and ex vivo studies were performed to assess the viability of the D-MCs as oral DDS. D-MCs improved the relative oral bioavailability by 180% within 4 h, and increased the absorption rate by 2.4 times compared to the control. This work represents a significant step forward in the translation of these devices from laboratory to clinic.



中文翻译:

从概念到体内测试:口服药物微容器

这项工作探索了聚合物微米级装置(微容器)作为口服药物输送系统(DDS)的潜力。在牺牲层上制造了可拆卸微容器(D-MC)的阵列,以改善处理能力并促进单个D-MC的收集。使用超临界CO 2浸渍将模型药物酮洛芬装入微容器中,然后沉积肠溶衣以保护药物免受恶劣的胃环境影响并在肠道内快速释放。体外体内离体进行了研究以评估D-MC作为口服DDS的生存能力。与对照组相比,D-MC在4小时内使相对口服生物利用度提高了180%,吸收率提高了2.4倍。这项工作代表了这些设备从实验室到临床的翻译迈出的重要一步。

更新日期:2017-10-18
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