Drug permeability profiling using cell-free permeation tools: Overview and applications
Tài liệu tham khảo
Adson, 1994, Quantitative approaches to delineate paracellular diffusion in cultured epithelial cell monolayers, J. Pharm. Sci., 83, 1529, 10.1002/jps.2600831103
Artursson, 1993, Selective paracellular permeability in two models of intestinal absorption: cultured monolayers of human intestinal epithelial cells and rat intestinal segments, Pharm. Res., 10, 1123, 10.1023/A:1018903931777
Avdeef, 2005, The rise of PAMPA, Expert Opin. Drug Metab. Toxicol., 1, 325, 10.1517/17425255.1.2.325
Avdeef, 2001, Drug absorption in vitro model: filter-immobilized artificial 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
Avdeef, 2004, PAMPA–a drug absorption in vitro model 11. Matching the in vivo unstirred water layer thickness by individual-well stirring in microtitre plates, Eur. J. Pharm. Sci., 22, 365
Avdeef, 2008, Absorption-excipient-pH classification gradient maps: sparingly soluble drugs and the pH partition hypothesis, Eur. J. Pharm. Sci., 33, 29, 10.1016/j.ejps.2007.09.009
Behrens, 2001, Transport of lipophilic drug molecules in a new mucus-secreting cell culture model based on HT29-MTX cells, Pharm. Res., 18, 1138, 10.1023/A:1010974909998
Beig, 2015, Head-to-head comparison of different solubility-enabling formulations of etoposide and their consequent solubility-permeability interplay, J. Pharm. Sci., 104, 2941, 10.1002/jps.24496
Beig, 2017, Advantageous solubility-permeability interplay when using amorphous solid dispersion (ASD) formulation for the BCS class IV P-gp substrate rifaximin: simultaneous increase of both the solubility and the permeability, AAPS J., 19, 806, 10.1208/s12248-017-0052-1
Beig, 2017, Concomitant solubility-permeability increase: vitamin E TPGS vs. amorphous solid dispersion as oral delivery systems for etoposide, Eur. J. Pharm. Biopharm., 121, 97, 10.1016/j.ejpb.2017.09.012
Bendels, 2006, PAMPA - excipient classification gradient map, Pharm. Res., 23, 2525, 10.1007/s11095-006-9137-8
Berben, 2018, Assessment of passive intestinal permeability using an artificial membrane insert system, J. Pharm. Sci., 107, 250, 10.1016/j.xphs.2017.08.002
Berben, 2018, The artificial membrane insert system as predictive tool for formulation performance evaluation, Int. J. Pharm., 537, 22, 10.1016/j.ijpharm.2017.12.025
Berben, 2017, Gastrointestinal behavior of itraconazole in humans - part 2: the effect of intraluminal dilution on the performance of a cyclodextrin-based solution, Int. J. Pharm., 526, 235, 10.1016/j.ijpharm.2017.04.057
Bermejo, 2004, PAMPA—a drug absorption in vitro model: 7. Comparing rat in situ, Caco-2, and PAMPA permeability of fluoroquinolones, Eur. J. Pharm. Sci., 21, 429, 10.1016/j.ejps.2003.10.009
Bibi, 2015, Permeapad™ for investigation of passive drug permeability: the effect of surfactants, co-solvents and simulated intestinal fluids (FaSSIF and FeSSIF), Int. J. Pharm., 493, 192, 10.1016/j.ijpharm.2015.07.028
Bibi, 2016, Use of Permeapad® for prediction of buccal absorption: a comparison to in vitro, ex vivo and in vivo method, Eur. J. Pharm. Sci., 93, 399, 10.1016/j.ejps.2016.08.041
Bibi, 2017, Simultaneous lipolysis/permeation in vitro model, for the estimation of bioavailability of lipid based drug delivery systems, Eur. J. Pharm. Biopharm., 117, 300, 10.1016/j.ejpb.2017.05.001
Balimane, 2000, Current methodologies used for evaluation of intestinal permeability and absorption, J. Pharmacol. Toxicol. Methods, 44, 301, 10.1016/S1056-8719(00)00113-1
Blanquet, 2004, A dynamic artificial gastrointestinal system for studying the behavior of orally administered drug dosage forms under various physiological conditions, Pharm. Res., 21, 585, 10.1023/B:PHAM.0000022404.70478.4b
Boegh, 2015, Mucus as a barrier to drug delivery – understanding and mimicking the barrier properties, Basic Clin. Pharmacol. Toxicol., 116, 179, 10.1111/bcpt.12342
Bohets, 2001, Strategies for absorption screening in drug discovery and development, Curr. Top. Med. Chem., 1, 367, 10.2174/1568026013394886
Brandl, 2001, Liposomes as drug carriers: a technological approach, Biotechnol. Annu. Rev., 7, 59, 10.1016/S1387-2656(01)07033-8
Buckley, 2012, In vitro models to evaluate the permeability of poorly soluble drug entities: challenges and perspectives, Eur. J. Pharm. Sci., 45, 235, 10.1016/j.ejps.2011.12.007
Buckley, 2013, Biopharmaceutical classification of poorly soluble drugs with respect to “enabling formulations”, Eur. J. Pharm. Sci., 50, 8, 10.1016/j.ejps.2013.04.002
di Cagno, 2015, New biomimetic barrier Permeapad™ for efficient investigation of passive permeability of drugs, Eur. J. Pharm. Sci., 73, 29, 10.1016/j.ejps.2015.03.019
Camenisch, 1996, Review of theoretical passive drug absorption models: historical background, recent developments and limitations, Pharm. Acta Helv., 71, 309, 10.1016/S0031-6865(96)00031-3
Camenisch, 1998, Estimation of permeability by passive diffusion through Caco-2 cell monolayers using the drugs' lipophilicity and molecular weight, Eur. J. Pharm. Sci., 6, 317, 10.1016/S0928-0987(97)10019-7
Chan, 2004, The ABCs of drug transport in intestine and liver: efflux proteins limiting drug absorption and bioavailability, Eur. J. Pharm. Sci., 21, 25, 10.1016/j.ejps.2003.07.003
Chen, 2008, A novel design of artificial membrane for improving the PAMPA model, Pharm. Res., 25, 1511, 10.1007/s11095-007-9517-8
Delvadia, 2012, A biorelevant in vitro release/permeation system for oral transmucosal dosage forms, Int. J. Pharm., 430, 104, 10.1016/j.ijpharm.2012.03.050
Dhiman, 2008, Formulation, characterization, and in vitro evaluation of bioadhesive gels containing 5-fluorouracil, Pharm. Dev. Technol., 13, 15, 10.1080/10837450701702438
Di, 2003, High throughput artificial membrane permeability assay for blood–brain barrier, Eur. J. Med. Chem., 38, 223, 10.1016/S0223-5234(03)00012-6
Ecker, 2014, The therapeutic monoclonal antibody market, MAbs, 7, 9, 10.4161/19420862.2015.989042
Engesland, 2013, New applications of phospholipid vesicle-based permeation assay: permeation model mimicking skin barrier, J. Pharm. Sci., 102, 1588, 10.1002/jps.23509
Engesland, 2015, Phospholipid vesicle-based permeation assay and EpiSkin® in assessment of drug therapies destined for skin administration, J. Pharm. Sci., 104, 1119, 10.1002/jps.24315
Engesland, 2016, In vitro models to estimate drug penetration through the compromised stratum corneum barrier, Drug Dev. Ind. Pharm., 42, 1742, 10.3109/03639045.2016.1171334
Ensign, 2012, Oral drug delivery with polymeric nanoparticles: the gastrointestinal mucus barriers, Adv. Drug Deliv. Rev., 64, 557, 10.1016/j.addr.2011.12.009
Falavigna, 2018, Mucus-PVPA (mucus phospholipid vesicle-based permeation assay): an artificial permeability tool for drug screening and formulation development, Int. J. Pharm., 537, 213, 10.1016/j.ijpharm.2017.12.038
Faller, 2008, Artificial membrane assays to assess permeability, Curr. Drug Metab., 9, 886, 10.2174/138920008786485227
FDA Drug Approvals - nrd.2017.14.pdf
Fischer, 2011, In-vitro permeability of poorly water soluble drugs in the phospholipid vesicle-based permeation assay: the influence of nonionic surfactants, J. Pharm. Pharmacol., 63, 1022, 10.1111/j.2042-7158.2011.01301.x
Fischer, 2012, Application of simulated intestinal fluid on the phospholipid vesicle-based drug permeation assay, Int. J. Pharm., 422, 52, 10.1016/j.ijpharm.2011.10.026
Flaten, 2007
Flaten, 2006, Drug permeability across a phospholipid vesicle-based barrier 2. Characterization of barrier structure, storage stability and stability towards pH changes, Eur. J. Pharm. Sci., 28, 336, 10.1016/j.ejps.2006.03.008
Flaten, 2006, Drug permeability across a phospholipid vesicle based barrier: a novel approach for studying passive diffusion, Eur. J. Pharm. Sci., 27, 80, 10.1016/j.ejps.2005.08.007
Flaten, 2007, Drug permeability across a phospholipid vesicle based barrier: 3. Characterization of drug-membrane interactions and the effect of agitation on the barrier integrity and on the permeability, Eur. J. Pharm. Sci., 30, 324, 10.1016/j.ejps.2006.11.017
Flaten, 2008, Drug permeability across a phospholipid vesicle-based barrier 4. The effect of tensides, co-solvents and pH changes on barrier integrity and on drug permeability, Eur. J. Pharm. Sci., 34, 173, 10.1016/j.ejps.2008.04.001
Flaten, 2015, In vitro skin models as a tool in optimization of drug formulation, Eur. J. Pharm. Sci., 75, 10, 10.1016/j.ejps.2015.02.018
Florence, 2001, Transcytosis of nanoparticle and dendrimer delivery systems: evolving vistas, Adv. Drug Deliv. Rev., 50, S69, 10.1016/S0169-409X(01)00184-3
Fong, 2017, A novel microdialysis-dissolution/permeation system for testing oral dosage forms: a proof-of-concept study, Eur. J. Pharm. Sci., 96, 154, 10.1016/j.ejps.2016.09.018
Galia, 1998, Evaluation of various dissolution media for predicting in vivo performance of class I and II drugs, Pharm. Res., 15, 698, 10.1023/A:1011910801212
Gantzsch, 2014, Characterization and evaluation of a modified PVPA barrier in comparison to Caco-2 cell monolayers for combined dissolution and permeation testing, J. Control. Release, 175, 79, 10.1016/j.jconrel.2013.12.009
Hayeshi, 2008, Comparison of drug transporter gene expression and functionality in Caco-2 cells from 10 different laboratories, Eur. J. Pharm. Sci., 35, 383, 10.1016/j.ejps.2008.08.004
Helander, 2014, Surface area of the digestive tract – revisited, Scand. J. Gastroenterol., 49, 681, 10.3109/00365521.2014.898326
Hens, 2015, Gastrointestinal behavior of nano- and microsized fenofibrate: in vivo evaluation in man and in vitro simulation by assessment of the permeation potential, Eur. J. Pharm. Sci., 77, 40, 10.1016/j.ejps.2015.05.023
Hens, 2016, Supersaturation and precipitation of posaconazole upon entry in the upper small intestine in humans, J. Pharm. Sci., 105, 2677, 10.1002/jps.24690
Hidalgo, 1991, Characterization of the unstirred water layer in Caco-2 cell monolayers using a novel diffusion apparatus, Pharm. Res., 8, 222, 10.1023/A:1015848205447
Ingels, 2004, Effect of simulated intestinal fluid on drug permeability estimation across Caco-2 monolayers, Int. J. Pharm., 274, 221, 10.1016/j.ijpharm.2004.01.014
Kansy, 1998, Physicochemical high throughput screening: parallel artificial membrane permeation assay in the description of passive absorption processes, J. Med. Chem., 41, 1007, 10.1021/jm970530e
Kanzer, 2010, In-vitro permeability screening of melt extrudate formulations containing poorly water-soluble drug compounds using the phospholipid vesicle-based barrier, J. Pharm. Pharmacol., 62, 1591, 10.1111/j.2042-7158.2010.01172.x
Kapitza, 2007, Absorption of poorly water soluble drugs subject to apical efflux using phospholipids as solubilizers in the Caco-2 cell model, Eur. J. Pharm. Biopharm., 66, 146, 10.1016/j.ejpb.2006.08.010
Karadzovska, 2013, Assessing vehicle effects on skin absorption using artificial membrane assays, Eur. J. Pharm. Sci., 50, 569, 10.1016/j.ejps.2013.02.020
Kataoka, 2003, In vitro system to evaluate oral absorption of poorly water-soluble drugs: simultaneous analysis on dissolution and permeation of drugs, Pharm. Res., 20, 1674, 10.1023/A:1026107906191
Khdair, 2013, In vitro artificial membrane-natural mucosa correlation of carvedilol buccal delivery, J. Drug Delivery Sci. Technol., 23, 603, 10.1016/S1773-2247(13)50092-X
Koplin, 2017, Surfactants enhance recovery of poorly soluble drugs during microdialysis sampling: implications for in vitro dissolution-/permeation-studies, J. Pharm. Biomed. Anal., 145, 586, 10.1016/j.jpba.2017.07.022
Könczöl, 2013, Applicability of a blood-brain barrier specific artificial membrane permeability assay at the early stage of natural product-based CNS drug discovery, J. Nat. Prod., 76, 655, 10.1021/np300882f
Lechanteur, 2017, The role of mucus in cell-based models used to screen mucosal drug delivery, Adv. Drug Deliv. Rev., 124, 50, 10.1016/j.addr.2017.07.019
Lee, 2017, Quantitative analysis of lab-to-lab variability in Caco-2 permeability assays, Eur. J. Pharm. Biopharm., 114, 38, 10.1016/j.ejpb.2016.12.027
Lennernäs, 1998, Human intestinal permeability, J. Pharm. Sci., 87, 403, 10.1021/js970332a
Linnankoski, 2008, Passive oral drug absorption can be predicted more reliably by experimental than computational models–fact or myth, Eur. J. Pharm. Sci., 34, 129, 10.1016/j.ejps.2008.03.001
Lipinski, 2000, Drug-like properties and the causes of poor solubility and poor permeability, J. Pharmacol. Toxicol. Methods, 44, 235, 10.1016/S1056-8719(00)00107-6
Lipinski, 2001, Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings, Adv. Drug Deliv. Rev., 46, 3, 10.1016/S0169-409X(00)00129-0
Liu, 2003, In vitro permeability of poorly aqueous soluble compounds using different solubilizers in the PAMPA assay with liquid chromatography/mass spectrometry detection, Pharm. Res., 20, 1820, 10.1023/B:PHAM.0000003380.44755.5a
Loftsson, 2010, Pharmaceutical applications of cyclodextrins: basic science and product development, J. Pharm. Pharmacol., 62, 1607, 10.1111/j.2042-7158.2010.01030.x
Lovering, 1973, Drug permeation through membranes. I. Effect of various substances on amobarbital permeation through polydimethylsiloxane, J. Pharm. Sci., 62, 602, 10.1002/jps.2600620412
Ma, 2017, Development of phospholipid vesicle-based permeation assay models capable of evaluating percutaneous penetration enhancing effect, Drug Dev. Ind. Pharm., 43, 2055, 10.1080/03639045.2017.1371730
Mandagere, 2002, Graphical model for estimating oral bioavailability of drugs in humans and other species from their Caco-2 permeability and in vitro liver enzyme metabolic stability rates, J. Med. Chem., 45, 304, 10.1021/jm010152k
Mann, 2017, Validation of dissolution testing with biorelevant media: an OrBiTo study, Mol. Pharm., 14, 4192, 10.1021/acs.molpharmaceut.7b00198
Markopoulos, 2013, In vitro and ex vivo investigation of the impact of luminal lipid phases on passive permeability of lipophilic small molecules using PAMPA, Pharm. Res., 30, 3145, 10.1007/s11095-013-1141-1
Matsson, 2015, Quantifying the impact of transporters on cellular drug permeability, Trends Pharmacol. Sci., 36, 255, 10.1016/j.tips.2015.02.009
McCartney, 2016, Safety concerns over the use of intestinal permeation enhancers: a mini-review, Tissue Barriers, 4, 10.1080/21688370.2016.1176822
Mensch, 2010, Evaluation of various PAMPA models to identify the most discriminating method for the prediction of BBB permeability, Eur. J. Pharm. Biopharm., 74, 495, 10.1016/j.ejpb.2010.01.003
Mols, 2005, Sulfasalazine transport in in-vitro, ex-vivo and in-vivo absorption models: contribution of efflux carriers and their modulation by co-administration of synthetic nature-identical fruit extracts, J. Pharm. Pharmacol., 57, 1565, 10.1211/jpp.57.12.0006
Mudie, 2012, Mechanistic analysis of solute transport in an in vitro physiological two-phase dissolution apparatus, Biopharm. Drug Dispos., 33, 378, 10.1002/bdd.1803
Müller, 2015, Tuning the predictive capacity of the PAMPA-BBB model, Eur. J. Pharm. Sci., 79, 53, 10.1016/j.ejps.2015.08.019
Naderkhani, 2014, Improved permeability of acyclovir: optimization of mucoadhesive liposomes using the phospholipid vesicle-based permeation assay, J. Pharm. Sci., 103, 661, 10.1002/jps.23845
Naderkhani, 2014, Development of a biomimetic phospholipid vesicle-based permeation assay for the estimation of intestinal drug permeability, J. Pharm. Sci., 103, 1882, 10.1002/jps.23954
Naderkhani, 2015, Biomimetic PVPA in vitro model for estimation of the intestinal drug permeability using fasted and fed state simulated intestinal fluids, Eur. J. Pharm. Sci., 73, 64, 10.1016/j.ejps.2015.03.017
Netsomboon, 2016, Mucoadhesive vs. mucopenetrating particulate drug delivery, Eur. J. Pharm. Biopharm., 98, 76, 10.1016/j.ejpb.2015.11.003
Neuhoff, 2005, pH-Dependent passive and active transport of acidic drugs across Caco-2 cell monolayers, Eur. J. Pharm. Sci., 25, 211, 10.1016/j.ejps.2005.02.009
Nielsen, 2004, PAMPA–a drug absorption in vitro model 8. Apparent filter porosity and the unstirred water layer, Eur. J. Pharm. Sci., 22, 33, 10.1016/j.ejps.2004.02.003
Niess, 2006, Dendritic cells in the recognition of intestinal microbiota, Cell. Microbiol., 8, 558, 10.1111/j.1462-5822.2006.00694.x
Ölander, 2016, The proteome of filter-grown Caco-2 cells with a focus on proteins involved in drug disposition, J. Pharm. Sci., 105, 817, 10.1016/j.xphs.2015.10.030
Ottaviani, 2006, Parallel artificial membrane permeability assay: a new membrane for the fast prediction of passive human skin permeability, J. Med. Chem., 49, 3948, 10.1021/jm060230+
Palac, 2014, Liposomes for (trans)dermal drug delivery: the skin-PVPA as a novel in vitro stratum corneum model in formulation development, J. Liposome Res., 24, 313, 10.3109/08982104.2014.899368
Palm, 1997, Polar molecular surface properties predict the intestinal absorption of drugs in humans, Pharm. Res., 14, 568, 10.1023/A:1012188625088
Patel, 2006, Use of simulated intestinal fluids with Caco-2 cells and rat ileum, Drug Dev. Ind. Pharm., 32, 151, 10.1080/03639040500465991
Pion Inc
Pongjanyakul, 2009, Alginate-magnesium aluminum silicate films for buccal delivery of nicotine, Colloids Surf. B Biointerfaces, 74, 103, 10.1016/j.colsurfb.2009.06.033
Proulx, 1991, Structure-function relationships in intestinal brush border membranes, Biochim. Biophys. Acta, 1071, 255, 10.1016/0304-4157(91)90016-P
Proulx, 1996, Membrane vesicles, Adv. Food Nutr. Res., 40, 197, 10.1016/S1043-4526(08)60029-7
Riethorst, 2016, Characterization of human duodenal fluids in fasted and fed state conditions, J. Pharm. Sci., 105, 673, 10.1002/jps.24603
Rogers, 1987, Intestinal metabolism of ethinyloestradiol and paracetamol in vitro: studies using Ussing chambers, Br. J. Clin. Pharmacol., 23, 727, 10.1111/j.1365-2125.1987.tb03108.x
Shiau, 1985, Mechanisms maintaining a low-pH microclimate in the intestine, Am. J. Phys., 248, G608
Sinkó, 2009, A PAMPA study of the permeability-enhancing effect of new ceramide analogues, Chem. Biodivers., 6, 1867, 10.1002/cbdv.200900149
Sinkó, 2012, Skin-PAMPA: a new method for fast prediction of skin penetration, Eur. J. Pharm. Sci., 45, 698, 10.1016/j.ejps.2012.01.011
Sironi, 2017, Evaluation of a dynamic dissolution/permeation model: mutual influence of dissolution and barrier-flux under non-steady state conditions, Int. J. Pharm., 522, 50, 10.1016/j.ijpharm.2017.03.002
Sironi, 2017, Dynamic dissolution-/permeation-testing of nano- and microparticle formulations of fenofibrate, Eur. J. Pharm. Sci., 96, 20, 10.1016/j.ejps.2016.09.001
Stappaerts, 2015, In situ perfusion in rodents to explore intestinal drug absorption: challenges and opportunities, Int. J. Pharm., 478, 665, 10.1016/j.ijpharm.2014.11.035
Stappaerts, 2017, The effect of 2-hydroxypropyl-β-cyclodextrin on the intestinal permeation through mucus, Eur. J. Pharm. Sci., 114, 238, 10.1016/j.ejps.2017.12.014
Sugano, 2001, Optimized conditions of bio-mimetic artificial membrane permeation assay, Int. J. Pharm., 228, 181, 10.1016/S0378-5173(01)00845-6
Sugano, 2002, Prediction of passive intestinal absorption using bio-mimetic artificial membrane permeation assay and the paracellular pathway model, Int. J. Pharm., 241, 241, 10.1016/S0378-5173(02)00240-5
Sun, 2002, Comparison of human duodenum and Caco-2 gene expression profiles for 12,000 gene sequences tags and correlation with permeability of 26 drugs, Pharm. Res., 19, 1400, 10.1023/A:1020483911355
Tsuji, 1996, Carrier-mediated intestinal transport of drugs, Pharm. Res., 13, 963, 10.1023/A:1016086003070
Ungell, 1998, Membrane transport of drugs in different regions of the intestinal tract of the rat, J. Pharm. Sci., 87, 360, 10.1021/js970218s
Veber, 2002, Molecular properties that influence the oral bioavailability of drug candidates, J. Med. Chem., 45, 2615, 10.1021/jm020017n
Volkova, 2017, Towards the rational design of novel drugs based on solubility, partitioning/distribution, biomimetic permeability and biological activity exemplified by 1,2,4-thiadiazole derivatives, Med. Chem. Commun., 8, 162, 10.1039/C6MD00545D
Wagner, 2012, Predicting the oral absorption of a poorly soluble, poorly permeable weak base using biorelevant dissolution and transfer model tests coupled with a physiologically based pharmacokinetic model, Eur. J. Pharm. Biopharm., 82, 127, 10.1016/j.ejpb.2012.05.008
Wohnsland, 2001, High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes, J. Med. Chem., 44, 923, 10.1021/jm001020e
Wuyts, 2015, Evaluation of fasted state human intestinal fluid as apical solvent system in the Caco-2 absorption model and comparison with FaSSIF, Eur. J. Pharm. Sci., 67, 126, 10.1016/j.ejps.2014.11.010
Wuyts, 2015, Evaluation of fasted and fed state simulated and human intestinal fluids as solvent system in the Ussing chambers model to explore food effects on intestinal permeability, Int. J. Pharm., 478, 736, 10.1016/j.ijpharm.2014.12.021
Zhang, 2017, Characterization of a liposome-based artificial skin membrane for in vitro permeation studies using Franz diffusion cell device, J. Liposome Res., 27, 302, 10.1080/08982104.2016.1231205
Zhu, 2002, A comparative study of artificial membrane permeability assay for high throughput profiling of drug absorption potential, Eur. J. Med. Chem., 37, 399, 10.1016/S0223-5234(02)01360-0
Zhu, 2017, Chapter 11 - oral absorption basics: pathways and physicochemical and biological factors affecting absorption, 297
Zidovetzki, 2007, Use of cyclodextrins to manipulate plasma membrane cholesterol content: evidence, misconceptions and control strategies, Biochim. Biophys. Acta, 1768, 1311, 10.1016/j.bbamem.2007.03.026