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Evaluation Models for Drug Transport Across the Blood–Brain Barrier
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
Caco-2 cells are epithelial cells derived from human colon adenoma cell line having distinct morphological characteristics are mainly used in BBB permeability studies (Lundquist and Renftel, 2002). Caco-2 cells are a poor model for permeability studies (Lundquist, 2002; Lohmann et al., 2002).
Polymeric Colloidal Carriers for Natural Polyphenolic Compounds
Published in Madhu Gupta, Durgesh Nandini Chauhan, Vikas Sharma, Nagendra Singh Chauhan, Novel Drug Delivery Systems for Phytoconstituents, 2020
Maria Rosaria Lauro, Teresa Musumeci, Francesca Sansone, Giovanni Puglisi, Rosario Pignatello
An interesting work was published by Iannone et al. (2017) on flavan-3-ols-rich grape seed extracts (GSE), known for its pro-apoptotic and anti-proliferative properties. In this investigation, different amounts of GSE (12.5, 25.0, and 37.5 mg/100 mg of polymer) were encapsulated in chitosan microsystems by spray-drying to create a GSE biocompatible matrix, able to modulate its biopharmaceutical parameters. The smallest microparticles were obtained with 12.5% and 25% of GSE that provided also a greater encapsulation efficiency (EE) value (80%) with respect to the sample prepared with 37.5% of GSE (EE of 60%). The authors justified this phenomenon with the saturation of the inner compartments that made the microsystems unable to load more extract. They also supposed that the formulation with 25% possessed the parameters for the evaluation of the in vitro antitumor activity. A549 and CaCo-2 cells were used as models of human lung cancer and human colon carcinoma, respectively, because they are suitable for local treatment. Due to the chitosan ability to bio-adhere to the cell membranes, the formulation selected was capable to enhance the anticancer ability on A549 and CaCo-2 cells (Figure 13.4). Less than 100 μg/mL of GSE gave high amount of cell survival rates. Instead, 100 μg/mL of GSE decreased the cell viability. At 50 μg/mL of loaded GSE, the better antitumor effect was obtained on the CaCo-2 cells.
Growth Factor Expression and Response in Human Colon Carcinoma Cells
Published in Leonard H. Augenlicht, Cell and Molecular Biology of Colon Cancer, 2019
Kathleen M. Mulder, Michael G. Brattain
Induction of a terminally differentiated phenotype in a colon tumor cell line, which would provide a model system with characteristics approaching a normal colon epithelial cell, has not yet been achieved. A biochemical marker indicative of terminal differentiation of colon tumor cells, such as that used to identify terminal differentiation of certain hematopoietic cell lines,84 does not exist. However, biochemical markers of enterocytic differentiation have been utilized with the HT-29 cell line.64,85 This cell line was originated from a well-differentiated human colon adenocarcinoma but, when cultured in serum-containing medium, grows as a monolayer of undifferentiated epithelial cells. HT-29 cells grown in glucose-free-medium express several brush border-specific enzymes at post-confluency.85 The Caco-2 cell line spontaneously expresses these enzymatic activities at post-confluency.86,87 More recently, the expression of such enzymatic activities has been demonstrated in the EB cell line from the prototypic bank when the cells are cultured in glucose-free medium.54 Although some of these brush border hydrolases (alkaline phosphatase and aminopeptidase) are present in normal colon88 and are expressed at higher levels in more differentiated cells,83 they are also expressed during the embryonic development of colon cells,88 thereby making their use as markers of terminal differentiation difficult.
Methylprednisolone 100 mg tablet formulation with pea protein: experimental approaches over intestinal permeability and cytotoxicity
Published in Drug Development and Industrial Pharmacy, 2023
Erhan Koc, Fatih Ciftci, Hilal Calik, Seval Korkmaz, Rabia Cakir Koc
A human colorectal carcinoma cell line, Caco-2 [15], has been used to predict the intestinal absorption of various drugs for a couple of decades. ICH M9 scientific guideline was published at the end of 2020 based on bio-waivers for BCS (Biopharmaceutical Classification System) Class I [5,16] and III drugs (Anonymous 1) [17]. Recently, Caco-2 has been used for several purposes, including intestinal permeability characteristics of orally applicated solid drugs. This study was undertaken to elucidate the permeation of methylprednisolone and different formulated tablets across Caco-2 cell monolayers to estimate it’s in vivo intestinal permeability profiles [18,19]. Caco-2 cell permeability is often used as a screening tool for assessing oral drug absorption during the early stages of drug development. Despite some differences in transporter gene expression, Caco-2 cells possess many structural and functional similarities to normal human enterocytes, and Caco-2 permeability has generally correlated well with Fa for many drugs in humans. Hence, many scientists use Caco-2 permeability as a surrogate for the human intestinal permeability [20].
Improved uptake and bioavailability of cinnamaldehyde via solid lipid nanoparticles for oral delivery
Published in Pharmaceutical Development and Technology, 2022
Long Wu, Yun Meng, Yuhang Xu, Xiaoqin Chu
After oral administration, the small intestine is the main organ for the absorption of drugs. Under in vitro growth circumstances, Caco-2 cells, which are derived from a cell line of a human colon adenocarcinoma, can differentiate into dense monolayers of epithelial cells that resemble the form and function of normally differentiated human small intestine epithelial cells (Sambuy et al. 2005; Xu et al. 2018). In addition, Caco-2 cells express several active transport systems and marker enzymes, so much so that the permeability coefficient of drugs in the monolayer of Caco-2 cells correlates well with drug absorption in humans (van Breemen and Li 2005; Zhou et al. 2018). The Caco-2 cell model has become the most commonly used in vitro model for studying intestinal absorption, with Caco-2 cell monolayers being the accepted classical cell model for studying nanodrug transport through intestinal epithelial cells. Therefore, we chose the Caco-2 cell line to study the absorption and transport mechanisms of CA and CA-SLNs.
Do differences in cell lines and methods used for calculation of IC50 values influence categorisation of drugs as P-glycoprotein substrates and inhibitors?
Published in Xenobiotica, 2022
Donna A. Volpe, Abhay Joshi, Vikram Arya
The cell line factor was selected as the expression of efflux transporters can vary between cells (Shirasaka et al. 2008; Bentz et al. 2013) and this can lead to different efflux ratios of a substrate drug (Tang et al. 2002; Siissalo et al. 2007; Patil et al. 2011) and IC50 values of an inhibitor drug (Tang et al. 2002). The human epithelial colorectal adenocarcinoma (Caco-2) and Madin-Darby canine kidney (MDCK) cells are two cell lines that are most commonly used to assess whether a new drug is a substrate and/or inhibitor of the P-gp efflux transporter in bidirectional cell assays (Volpe 2011, 2016). Given the canine origin of MDCK cells and low expression of transporter proteins, they are often transfected with human transporter proteins such as P-gp (MDR1-MDCK cells) for use in transport assays (Tang et al. 2002; Volpe 2011). Additionally, Lilly Laboratories cell-porcine kidney 1 (LLC-PK1) cells are transfected with MDR1 for use in P-gp assays (Sugimoto et al. 2011).