Mosgaard Mette D, Sassene Philip J, Mu Huiling, Rades Thomas, Müllertz Anette
Department of Pharmacy, University of Copenhagen, Universitetsparken 2, Copenhagen 2100, Denmark.
Department of Pharmacy, University of Copenhagen, Universitetsparken 2, Copenhagen 2100, Denmark.
J Pharm Sci. 2017 Apr;106(4):1183-1186. doi: 10.1016/j.xphs.2016.12.026. Epub 2017 Jan 3.
The high-throughput in vitro intestinal lipolysis model (HTP) applicable for rapid and low-scale screening of lipid-based drug delivery systems (LbDDSs) was optimized and adjusted as to be conducted in 96-well plates (HTP-96). Three different LbDDSs (I-III) loaded with danazol or cinnarizine were used as model systems. The distributions of cinnarizine and danazol in the aqueous and precipitated digestion phases generated during lipolysis in HTP-96 were compared with previously published data obtained from HTP. The final HTP-96 setup resulted in the same rank order as the original HTP model with regard to solubilization in the aqueous phase during digestion: LbDDS III > LbDDS II > LbDDS I for danazol and LbDDS III ≈ LbDDS II ≈ LbDDS I for cinnarizine. HTP-96 is a useful model for fast performance assessment of LbDDS in a small scale.
适用于基于脂质的药物递送系统（LbDDS）快速小规模筛选的高通量体外肠道脂解模型（HTP）进行了优化和调整，以便在96孔板中进行（HTP-96）。使用三种载有达那唑或桂利嗪的不同LbDDS（I-III）作为模型系统。将HTP-96脂解过程中产生的水相和沉淀消化阶段中桂利嗪和达那唑的分布与先前从HTP获得的已发表数据进行比较。最终的HTP-96设置在消化过程中在水相中的增溶方面产生了与原始HTP模型相同的排名顺序：对于达那唑，LbDDS III>LbDDS II>LbDDS I；对于桂利嗪，LbDDS III≈LbDDS II≈LbDDS I。HTP-96是一种用于小规模快速评估LbDDS性能的有用模型。
