Discrimination between drug candidates using models for evaluation of intestinal absorption
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Multidimensional analysis of human intestinal fluid composition
2020, European Journal of Pharmaceutics and BiopharmaceuticsCitation Excerpt :Drug solubility in the gastrointestinal environment is therefore a key factor controlling bioavailability and has been incorporated into theoretical and practical biopharmaceutical concepts for example the Absorption Potential (AP) [2], Maximum Absorbable Dose (MAD) [3], Biopharmaceutical Classification System (BCS) [4] and Developability Classification System (DCS) [5,6]. This has led to a focus on gastrointestinal drug solubility during development [7–9] and a recognition that determination of the value either by computation or experimentation is a key stage. However, the current experimental methods available to determine solubility are not adequate [10] to permit in vivo prediction of average solubility and its variability from in vitro measurement and further development is warranted.
Nanostructured therapeutic systems with bioadhesive and thermoresponsive properties
2017, Nanostructures for Novel Therapy: Synthesis, Characterization and ApplicationsGastrointestinal behavior and ADME phenomena: I. In vitro simulation
2016, Journal of Drug Delivery Science and TechnologyEvaluation in vitro and in vivo of curcumin-loaded mPEG-PLA/TPGS mixed micelles for oral administration
2016, Colloids and Surfaces B: BiointerfacesThe physiological performance of a three-dimensional model that mimics the microenvironment of the small intestine
2011, BiomaterialsCitation Excerpt :Due to the intestinal absorption process complexity, to date, there have been various models established that take the variability of test parameters into consideration; however, no universal model that combines all necessary properties has been developed [7]. The currently used 2D intestinal in vitro test systems are predominantly based on the use of cell lines that were derived from mammalian colon cancer [4,8]. One of the most routinely utilized cell lines for the establishment of intestinal test systems, and therefore for the prediction of oral absorption of drug candidates in early drug discovery programs, is the Caco-2 cell line, which was originally established from human epithelial colorectal adenocarcinoma cells [9–15].