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| Caco-2 细胞渗透性测定× | 溶出度f1/f2相似因子× | 脂质体药物递送× | |
|---|---|---|---|
| 领域 | 药理学 | 药理学 | 药理学 |
| 方法族 | Process / pipeline | Process / pipeline | Process / pipeline |
| 起源年份≠ | 1989 | 1996 | 1965 |
| 提出者≠ | Ingrid Hidalgo | James Moore and Hector Flanner | Alec Bangham |
| 类型≠ | absorption screening | similarity testing | formulation technology |
| 开创性文献≠ | Hidalgo, I. J., Raub, T. J., & Borchardt, R. T. (1989). Characterization of the human colon carcinoma cell line (Caco-2) as a model system for intestinal epithelial permeability. Gastroenterology, 96(3), 736-749. DOI ↗ | Moore, J. W., & Flanner, H. H. (1996). Mathematical comparison of dissolution profiles. Pharmaceutical Technology, 20(6), 64-74. link ↗ | Bangham, A. D., Standish, M. M., & Watkins, J. C. (1965). Diffusion of univalent ions across the lamellae of swollen phospholipid films and the determination of membrane potential. Journal of Molecular Biology, 13(1), 238-252. DOI ↗ |
| 别名 | Caco-2 assay, intestinal permeability, ADME screening | f1, f2, similarity factor | liposomal formulation, vesicular delivery, lipid nanoparticles |
| 相关 | 3 | 3 | 3 |
| 摘要≠ | The Caco-2 assay is an in vitro model system using human colon carcinoma cell monolayers to screen drug intestinal permeability. Developed by Hidalgo and colleagues in 1989, Caco-2 cells differentiate into an epithelial barrier resembling intestinal mucosa, enabling rapid assessment of drug absorption potential and identification of transporter-mediated transport. | The f1 and f2 factors are dimensionless statistical measures developed by Moore and Flanner to quantify the similarity between two dissolution profiles. Adopted by regulatory agencies (FDA, EMA) as the gold standard for comparing dissolution curves, these factors enable rapid assessment of whether formulation changes significantly impact drug release. | Liposomal encapsulation is a formulation technique using lipid bilayer vesicles (liposomes) to enclose drugs, improving bioavailability, reducing toxicity, and enabling targeted delivery. Developed by Alec Bangham in 1965, liposomes are now standard in pharmaceutical development, with several FDA-approved liposomal drugs on the market. |
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