Biological, Pharmaceutical, and Analytical Considerations with Respect to the Transport Media Used in the Absorption Screening System, Caco-2

Journal of Pharmaceutical Sciences - Tập 92 - Trang 1545-1558 - 2003
Françoise M. Ingels1, Patrick F. Augustijns2
1Biopharmaceutics and Drug Delivery, Lilly Development Centre, 11 rue Granbonpré, 1348 Mont-Saint-Guibert, Belgium
2Laboratory for Pharmacotechnology and Biopharmacy, Katholieke Universiteit Leuven, O&N Gasthuisberg, 3000 Leuven, Belgium

Tài liệu tham khảo

Martin, 1981, A practitioner's perspective of the role of quantitative structure–activity analysis in medicinal chemistry, J Med Chem, 24, 229, 10.1021/jm00135a001 Palm, 1996, Correlation of drug absorption with molecular surface properties, J Pharm Sci, 85, 32, 10.1021/js950285r Palm, 1998, Evaluation of dynamic polar molecular surface area as predictor of drug absorption: Comparison wtih other computational and experimental predictors, J Med Chem, 41, 5382, 10.1021/jm980313t Conradi, 1991, The influence of peptide structure on transport across Caco-2 cells, Pharm Res, 8, 1453, 10.1023/A:1015825912542 Stenberg, 1999, Prediction of membrane permeability to peptides from calculated dynamic molecular surface properties, Pharm Res, 16, 205, 10.1023/A:1018816122458 Stenberg, 1999, Prediction of the intestinal absorption of endothelin receptor antagonists using three theoretical methods of increasing complexity, Pharm Res, 16, 1520, 10.1023/A:1015092201811 Wright, 1992, Role of desolvatation energy in the nonfacilitated membrane permeability of didoxyribose analogs of thymidine, Mol Pharmacol, 41, 957 Veber, 2002, Molecular properties that influence the oral bioavailability of drug candidates, J Med Chem, 45, 2615, 10.1021/jm020017n Egan, 2000, Prediction of drug absorption using multivariate statistics, J Med Chem, 43, 3867, 10.1021/jm000292e Lipinski, 2001, Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings, Adv Drug Del Rev, 46, 3, 10.1016/S0169-409X(00)00129-0 Goodwin, 1996, Relationships between physiochemical properties for a series of peptides and membrane permeability in Caco-2 cells, Pharm Res, 13, S243, 10.1023/A:1016043114998 Stenberg, 2000, Virtual screening of intestinal drug permeability, J Controlled Release, 65, 231, 10.1016/S0168-3659(99)00239-4 Kansy, 1998, Physicochemical high throughput screening: Parallel artificial membrane permeation assay in the description of passive absortpion process, J Med Chem, 41, 1007, 10.1021/jm970530e Avdeef, 2001, Drug absorption in vitro model: Filter-immobilized artifical membranes 2. Studies of the permeability properties of lactones in Piper methysticum Forst, Eur J Pharm Sci, 14, 271, 10.1016/S0928-0987(01)00191-9 Lundahl, 1997, Immobilized liposome chromatography of drugs for model analysis of drug–membrane interactions, Adv Drug Del Ref, 23, 221, 10.1016/S0169-409X(96)00437-1 Yang, 1997, Immobilized artificial membranes—Screens for drug membrane interactions, Adv Drug Del Rev, 23, 229, 10.1016/S0169-409X(96)00438-3 Kim, 1993, A correlation between the permeability characteristics of a series of peptides using an in vitro cell culture model (Caco-2) and those using an in situ perfused rat ileum model of the intestinal mucosa, Pharm Res, 10, 1710, 10.1023/A:1018969713547 Ginski, 1999, Prediction of dissolution–absorption relationships from a dissolution/Caco-2 system, Int J Pharm, 177, 117, 10.1016/S0378-5173(98)00330-5 Van der Bijl, 2002, Permeability of human intestinal mucosa using a continuous flow-through perfusion system, Int J Pharm, 235, 71, 10.1016/S0378-5173(01)00977-2 Hidalgo, 1989, Characterization of human colon carcinoma cell line (Caco-2) as a model system for intestinal epithelial permeability, Gastroenterology, 96, 736, 10.1016/S0016-5085(89)80072-1 Hilgers, 1990, Caco-2 cell monolayers as a model for drug transport across the intestinal mucosa, Pharm Res, 7, 902, 10.1023/A:1015937605100 Gan, 1997, Applications of the Caco-2 model in the design and development of orally active drugs: Elucidation of biochemical and physical barriers posed by the intestinal epithelium, Adv Drug Del Rev, 23, 77, 10.1016/S0169-409X(96)00427-9 Artursson, 1991, Correlation between oral drug absorption in humans and apparent drug permeability coefficients in human intestinal epithelial (Caco-2) cells, Biochem Biophys Res Commun, 175, 880, 10.1016/0006-291X(91)91647-U Artursson, 2001, Caco-2 monolayers in experimental and theortical predictions of drug transport, Adv Drug Del Rev, 56, 27, 10.1016/S0169-409X(00)00128-9 Wikman Larherd, 1998, The influence of intestinal mucus components on the diffusion of drugs, Pharm Res, 15, 166 Hidalgo, 1996, Cultured intestinal epithelial cell models, 35 Barthe, 1999, Gastrointestinal absorption of drugs: Methods and studies, Fundam Clin Pharmacol, 13, 154, 10.1111/j.1472-8206.1999.tb00334.x Bohets, 2001, Strategies for absorption screen in drug discovery and development, Curr Top Med Chem, 1, 367, 10.2174/1568026013394886 Wikman, 1993, A drug absorption model based on the mucus layer producing human intestinal goblet cell line HT29-H, Pharm Res, 10, 843, 10.1023/A:1018905109971 Hilgendorf, 2000, Caco-2 versus Caco-2/HT29-MTX co-cultured cell lines: Permeabilities via diffusion, inside- and outside-directed carrier-mediated transport, J Pharm Sci, 89, 63, 10.1002/(SICI)1520-6017(200001)89:1<63::AID-JPS7>3.0.CO;2-6 Cummins, 2001, Characterizing the expression of CYP3A4 and efflux transporters (P-gp, MRP2, and MRP2) in CYP3A4-transfected Caco-2 cells after induction with sodium buytrate and the phorbol ester 12-O-tetradecanocylphorbol-13-acetate, Pharm Res, 18, 1102, 10.1023/A:1010914624111 Crespi, 1996, Development of Caco-2 cells expressing high levels of cDNA-derived cytochrome P4503A4, Pharm Res, 13, 1635, 10.1023/A:1016428304366 Schmiedlin-Ren, 1997, Expression of enzymatically active TYP3A4 by Caco-2 cells grown on extracellular matrix-coated permeable supports in the presence of aα,25-dihydroxy-vitamin-D3, Mol Pharmacol, 51, 741, 10.1124/mol.51.5.741 Hochman, 2000, Influence of P-glycoprotein on the transport and metabolism of indinavir in Caco-2 cells expressing cytochrome P-450 3A4, J Pharmacol Exp Ther, 292, 310 Fisher, 1999, Midazolarn metabolism by modified Caco-2 monolayers: Effects of extracellular protein binding, J Pharmacol Exp Ther, 289, 1143 Hu, 1999, Transport and metabolic characterizaiton of Caco-2 cells expressing CYP3A4 and CYP3A4 plus oxidoreductase, Pharm Res, 16, 1352, 10.1023/A:1018986605929 Grass, 1988, In vitro measurement of gastorintestinal tissue permeability using a new diffusion cell, Pharm Res, 5, 372, 10.1023/A:1015911712079 Annaert, 2000, In vitro ex vivo and in situ intestinal absorption characteristics of the antiviral ester prodrug adefovir dipivoxil, J Pharm Sci, 89, 1054, 10.1002/1520-6017(200008)89:8<1054::AID-JPS10>3.0.CO;2-5 Makhey, 1998, Characterization of the regional intestinal kinetics of the drug efflux in rat and human intestine and in Caco-2 cells, Pharm Res, 15:15, 1160, 10.1023/A:1011971303880 Nakayame, 2000, Region-dependent disappearance of vinblastine in rat small intestine and characterization of its P-glycoprotein-mediated efflux system, Eur J Pharm Sci, 11, 317, 10.1016/S0928-0987(00)00113-5 Yu, 2002, Biopharmaceutics classification system: The scientific basis for biowaiver extensions, Pharm Res, 19, 921, 10.1023/A:1016473601633 Braun, 2000, Cell cultures as tools in biopharmacy, Eur J Pharm Sci, 11, S51, 10.1016/S0928-0987(00)00164-0 Mathieu, 1999, Transepithelial transport of bepiridil in the human intestinal cell line, Caco-2, using two media, DMEMc and HBSS, Int J Pharm, 181, 203, 10.1016/S0378-5173(99)00027-7 Walgren, 1999, The influence of plasma binding on absorption/exsorption in the Caco-2 model of human intestinal absorption, J Pharm Pharmacol, 51, 1037, 10.1211/0022357991773366 Chan, 1996, Absorption of Cam-2445, an NK1 neurokinin receptor antagonist: In vivo, in situ, and in vitro evaluations, J Pharm Sci, 85, 253, 10.1021/js9503338 Augustijns, 1993, Evidence of a polarized efflux system in Caco-2 cells capable of modulating cyclosporin A transport, Biochem Biophys Res Commun, 197, 360, 10.1006/bbrc.1993.2487 Krishna, 2001, Permeability of lipophilic compounds in drug discovery using in-vitro human absorption model, Caco-2, Int J Pharm, 222, 77, 10.1016/S0378-5173(01)00698-6 Deferme, 2002, Intestinal absorption characteristics of the low solubility thiocarboxanilide UC-781, Int J Pharm, 234, 113, 10.1016/S0378-5173(01)00952-8 Nerurkar, 1996, The use of surfactants to enhance the permeability of peptides through Caco-2 Cells by inhibition of an apically polarized efflux system, Pharm Res, 13, 528, 10.1023/A:1016033702220 Rege, 2002, Effects of non-ionic surfactants on membrane transporters in Caco-2 cell monolayers, Eur J Pharm Sci, 16, 237, 10.1016/S0928-0987(02)00055-6 Flanagan, 2002, Contributions of saturable active secretion, passive transcellular, and paracellular diffusion to the overall transport of furosemide across adenocarcinoma (Caco-2) cells, J Pharm Sci, 91, 1169, 10.1002/jps.10099 Ginski, 2000, Evaluation of cosolvent systems to facilitate Caco-2 permeability screening of poorly water soluble drug candidates, AAPS Annual Meeting; poster, 3247 Yamashita, 2000, Optimized conditions for prediction of intestinal drug permeability using Caco-2 cells, Eur J Pharm Sci, 10, 195, 10.1016/S0928-0987(00)00076-2 Aungst, 2000, The influence of donor and reservoir additives on Caco-2 permeability and secretory transport of HIB protease inhibitors and other lipophillic compounds, Pharm Res, 17, 1175, 10.1023/A:1026402410783 Saha, 2000, Effect of solubilizing excipients on permeation of poorly water-soluble compounds across Caco-2 cell monolayers, Eur J Pharm Biopharm, 50, 403, 10.1016/S0939-6411(00)00113-2 Yu, 1999, Vitamin E-TPGS increases absorption flux on an HIV protease inhibitor by enhancing in solubility and permeability, Pharm Res, 16, 1813 Aungst, 2000, Intestinal permeation enhancers, J Pharm Sci, 89, 429, 10.1002/(SICI)1520-6017(200004)89:4<429::AID-JPS1>3.0.CO;2-J Batrakova, 1999, Pluronic P85 increases permeability of a broad spectrum of drugs in polarized BBMEC and Caco-2 cell monolayers, Pharm Res, 16, 1366, 10.1023/A:1018990706838 Hugger, 2002, A comparison of commonly used polyethoxylated pharmaceutial excipitents on their ability to inhibit P-glycoprotein activity in vitro, J Pharm Sci, 91, 1991, 10.1002/jps.10176 Hugger, 2002, Effects of poly(ethylene glycol) on efflux transporter activity in Caco-2 cell monolayers, J Pharm Sci, 91, 1980, 10.1002/jps.10175 Dintaman, 1999, Inhibition of P-glycoprotein by D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS), Pharm Res, 16, 1550, 10.1023/A:1015000503629 Dimitrijevic, 2000, Effects of some non-ionic surfactants on transepitherlial permeability in Caco-2 cells, J Pharm Pharmacol, 52, 157, 10.1211/0022357001773805 Rege, 2001, Effects of common excipients on Caco-2 transport of low-permeability drugs, J Pharm Sci, 90, 1776, 10.1002/jps.1127 Taub, 2002, Optimized conditions for MDCK permeability and turbidimetric solubility studies using compounds representative of BCS classes I–IV, Eur J Pharm Sci, 15, 331, 10.1016/S0928-0987(02)00015-5 Mountfield, 2000, Potential inhibitory effects of formulation ingredients on intestinal cytochrome P450, Int J Pharm, 211, 89, 10.1016/S0378-5173(00)00586-X Udata, 2003, Enhanced transport of a novel anti-HIV agent—Cosalane and its congeners across human intestinal epithelial (Caco-2) cell monolayers, Int J Pharm, 250, 157, 10.1016/S0378-5173(02)00523-9 Wiedmann, 2002, Examination of the solubilizaiton of drugs by bile salt micelles, J Pharm Sci, 91, 1743, 10.1002/jps.10158 Gray, 1996, Change of pH requirements for simulated intestinal fluid TS, Pharmacopeial Forum, 22, 1943 Lucas, 1983, Determination of acid surface pH in vivo in rat proximal jejunum, Gut, 24, 734, 10.1136/gut.24.8.734 Tsuji, 1996, Carrier-mediated intestinal transport of drugs, Pharm Res, 13, 963, 10.1023/A:1016086003070 Hidalgo, 1996, Carrier-mediated transport and efflux mechanisms in Caco-2 cells, Adv Drug Del Rev, 22, 53, 10.1016/S0169-409X(96)00414-0 Ogihara, 1999, Structural characterization of substrates for the anion exchange transporter in Caco-2 cells, J Pharm Sci, 88, 1217, 10.1021/js9900093 Putman, 2002, Comparison of bi-directional cephalexin transport across MDCK and Caco-2 cell monolayers: Interactions with peptide transporters, Pharm Res, 19, 27, 10.1023/A:1013647114152 Friedrichsen, 2002, Synthesis of analogs of L-valacyclovir and determination of their substrate activity for the oligopeptide transporter in Caco-2 cells, Eur J Pharm Sci, 16, 1, 10.1016/S0928-0987(02)00047-7 Palm, 1999, Effect of molecular charge on intestinal epithelial drug transport: pH-dependent transpot of cationic drugs, J Pharmacol Exp Ther, 291, 435 Ungell, 2002, Real and false efflux of weak basic drugs across Caco-2 monolayers, APPS Annual Meeting; poster, W5056 Yamashita, 1997, Analysis of drug permeation across Caco-2 monolayer: Implication for predicting in vivo drug absorption, Pharm Res, 14, 486, 10.1023/A:1012103700981 Anderberg, 1992, Epithelial transport of drugs in cell culture. VII: Effects of pharamceutical surfactant excipients and bile acids on transepithelial permeability in monolayers of human intestinal epithelial (Caco-2) cells, J Pharm Sci, 81, 879, 10.1002/jps.2600810908 Lo, 2002, Effects of sodium deoxycholate and sodium caprate on the transport of epirubicin in human intestinal epithelial Caco-2 cell layers and everted gut sacs of rats, Biochem Pharmacol, 59, 665, 10.1016/S0006-2952(99)00377-9 Meaney, 2000, A comparison of the permeation enhancement potential of simple bile salt and mixed bile salt: Fatty acid micellar systems using the Caco-2 cell culture model, Int J Pharm, 207, 21, 10.1016/S0378-5173(00)00526-3 Dressman, 1998, Dissolution testing as a prognostic tool for oral drug absorption: Immediate release dosage forms, Pharm Res, 15, 11, 10.1023/A:1011984216775 Ingels, 2002, Simulated intestinal fluid as transport medium in the Caco-2 cell culture model, Int J Pharm, 232, 183, 10.1016/S0378-5173(01)00897-3 Akita, 2002, Transport activity of human MRP3 expressed in Sf9 cells: Comaprative studies with rat MRP3, Pharm Res, 19, 34, 10.1023/A:1013699130991 Saha, 2002, Effect of bovine serum ablumin on drug permeability estimation across Caco-2 monolayers, Eur J Pharm Biopharm, 54, 319, 10.1016/S0939-6411(02)00089-9 Chung, 2001, Profound effect of plasma protein binding on the polarize transport of flurosemide and verapamil in the Caco-2 model, Pharm Res, 18, 544, 10.1023/A:1011022931368 1998, USP Pharmacopeial forum, US Pharmacopeia, 24, 6015 2000, Waiver of in vivo bioavailability and bioequivalence studies for immediate-release solid oral dosage forms based on a biopharmaceutics classifications sytems, Guidance for industry, 1 Spahn-Langguth, 1998, P-glycoprotein transporters and the gastrointestinal tract: Evaluation of the potential in vivo relevance of in vitro data employing talinolol as model compound, Int J Clin Pharmacol Ther, 36, 16