کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
9918783 | 1557557 | 2005 | 7 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Validation of the 96 well Caco-2 cell culture model for high throughput permeability assessment of discovery compounds
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کلمات کلیدی
BMSTrans Epithelial Electrical Resistanceabsorption, distribution, metabolism, eliminationP-gpTEERHBSSNCEPAMPAADMELSCHEPESN-2-hydroxyethylpiperazine-N′-2-ethanesulfonic acid - N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acidP-glycoprotein - P-گلیکوپروتئینParallel artificial membrane permeability assay - تست نفوذپذیری غشایی موازیAbsorption - جذبTransport - حمل و نقل یا ترابریBCs - روند BCsCaco-2 cells - سلول های Caco-2biopharmaceutics classification system - سیستم طبقه بندی بیولوژیکی داروLiquid scintillation counter - ضد شمعدان مایعPermeability coefficient - ضریب نفوذپذیریhigh throughput screening - غربالگری بالاImmobilized artificial membrane - غشای مصنوعی ImmobilizedHank's balanced salt solution - محلول نمک متعادل هانکIAM - من هستمnew chemical entity - موجودی شیمیایی جدیدPermeability - نفوذپذیریDrug discovery - کشف مواد مخدر
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
علوم دارویی
پیش نمایش صفحه اول مقاله

چکیده انگلیسی
The use of Caco-2 cells for permeability screening of discovery compounds is quite well established and serves as the “method-of-choice” across the pharmaceutical industries worldwide. The typical permeability-screening model involves growing cells on a 12 well or 24 well transwell format. In this manuscript, we report the use of Caco-2 cells grown on 96 well transwell plates for screening of discovery compounds to assess their permeability characteristics. A set of standard compounds (marketed compounds) belonging to the various class of Biopharmaceutics Classification System (BCS) were used to assess the utility of the 96 well Caco-2 cells. Extensive validations were also performed with â¼160 Bristol-Myers Squibb (BMS) discovery compounds by comparing the permeability values in the 96 well Caco-2 cells with the in-house 24 well Caco-2 cells. Functional Caco-2 cells with intact monolayers could be established in the 96 well format using optimized seeding and culturing conditions. The permeability of BCS compounds in the 96 well format was found to be comparable to the permeability in 24 well format. Similarly, there was very good correlation (R2Â =Â 0.93) between the two formats for the extensive validation performed with in-house discovery compounds. The validated 96 well Caco-2 cell system presents a very attractive permeability screening tool that can perform much more efficiently than the conventional 12 well or 24 well systems while providing the same high quality permeability screening data.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: International Journal of Pharmaceutics - Volume 297, Issues 1â2, 13 June 2005, Pages 235-241
Journal: International Journal of Pharmaceutics - Volume 297, Issues 1â2, 13 June 2005, Pages 235-241
نویسندگان
Anthony M. Marino, Melissa Yarde, Hetal Patel, Saeho Chong, Praveen V. Balimane,