Application of simulated intestinal fluid on the phospholipid vesicle-based drug permeation assay

International Journal of Pharmaceutics

Volumn 422, Issue 1-2, 2012, Pages 52-58

  Fischer, Sarah Maud ^a,b   Buckley, Stephen Timothy ^a   Kirchmeyer, Wiebke ^a,b   Fricker, Gert ^b   Brandl, Martin ^a  

^a UNIVERSITY OF SOUTHERN DENMARK   (Denmark)

^b UNIVERSITY OF HEIDELBERG   (Germany)

Author keywords

Fasted state simulated intestinal fluid (FaSSIF); Permeability; Phospholipid vesicle based permeation assay (PVPA); Sodium taurocholate

Indexed keywords

BOVINE SERUM ALBUMIN; CALCEIN; CIMETIDINE; GRISEOFULVIN; KETOPROFEN; NADOLOL; TAUROCHOLIC ACID;

ARTICLE; CELL ENCAPSULATION; CONFOCAL LASER MICROSCOPY; CONTROLLED STUDY; DRUG PENETRATION; ELECTRIC RESISTANCE; IN VITRO STUDY; INTESTINE FLUID; MICELLE; PHOSPHOLIPID VESICLE; PHYSICAL CHEMISTRY; PRIORITY JOURNAL; VISION TEST;

CHEMISTRY, PHARMACEUTICAL; CIMETIDINE; ELECTRIC IMPEDANCE; FLUORESCEINS; GRISEOFULVIN; INTESTINAL SECRETIONS; KETOPROFEN; MICROSCOPY, CONFOCAL; NADOLOL; PERMEABILITY; PHARMACEUTICAL PREPARATIONS; PHOSPHOLIPIDS; SERUM ALBUMIN, BOVINE; TAUROCHOLIC ACID; TECHNOLOGY, PHARMACEUTICAL; TIME FACTORS;

EID: 84655169730     PISSN: 03785173     EISSN: 18733476     Source Type: Journal    
DOI: 10.1016/j.ijpharm.2011.10.026     Document Type: Article

References (40)

1. A. Albalak, M.L. Zeidel, S.D. Zucker, A.A. Jackson, and J.M. Donovan Effects of submicellar bile salt concentrations on biological membrane permeability to low molecular weight non-ionic solutes Biochemistry 35 1996 7936 7945 (Pubitemid 26202534)
2. J. Brouwers, J. Tack, F. Lammert, and P. Augustijns Intraluminal drug and formulation behavior and integration in in vitro permeability estimation: a case study with amprenavir J. Pharm. Sci. 95 2006 372 383 (Pubitemid 43241979)
3. B. de Castro, P. Gameiro, C. Guimaraes, J.L. Lima, and S. Reis Partition coefficients of beta-blockers in bile salt/lecithin micelles as a tool to assess the role of mixed micelles in gastrointestinal absorption Biophys. Chem. 90 2001 31 43 (Pubitemid 32178110)
4. S.M. Fischer, G.E. Flaten, E. Hagesaether, G. Fricker, and M. Brandl In-vitro permeability of poorly water soluble drugs in the phospholipid vesicle-based permeation assay: the influence of nonionic surfactants J. Pharm. Pharmacol. 63 2011 1022 1030
5. G.E. Flaten, A.B. Dhanikula, K. Luthman, and M. Brandl Drug permeability across a phospholipid vesicle based barrier: a novel approach for studying passive diffusion Eur. J. Pharm. Sci. 27 2006 80 90 (Pubitemid 41728258)
6. G.E. Flaten, H. Bunjes, K. Luthman, and M. Brandl 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 2006 336 343 (Pubitemid 44218739)
7. G.E. Flaten, K. Luthman, T. Vasskog, and M. Brandl 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 2008 173 180
8. G.E. Flaten, M. Skar, K. Luthman, and M. Brandl 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 2007 324 332 (Pubitemid 46282449)
9. L. Fossati, R. Dechaume, E. Hardillier, D. Chevillon, C. Prevost, S. Bolze, and N. Maubon Use of simulated intestinal fluid for Caco-2 permeability assay of lipophilic drugs Int. J. Pharm. 360 2008 148 155
10. E. Galia, E. Nicolaides, D. Horter, R. Lobenberg, C. Reppas, and J.B. Dressman Evaluation of various dissolution media for predicting in vivo performance of class I and II drugs Pharm. Res. 15 1998 698 705 (Pubitemid 28275645)
11. H. Grohganz, V. Ziroli, U. Massing, and M. Brandl Quantification of various phosphatidylcholines in liposomes by enzymatic assay AAPS PharmSciTech 4 2003 E63
12. C. Hansch, P.G. Sammes, and J.B. Taylor Comprehensive Medicinal Chemistry: the Rational Design, Mechanistic Study & Therapeutic Application of Chemical Compounds 1st ed. 1990 Pergamon Press, Oxford New York
13. I. Hubatsch, E.G. Ragnarsson, and P. Artursson Determination of drug permeability and prediction of drug absorption in Caco-2 monolayers Nat. Protoc. 2 2007 2111 2119 (Pubitemid 351565848)
14. F. Ingels, B. Beck, M. Oth, and P. Augustijns Effect of simulated intestinal fluid on drug permeability estimation across Caco-2 monolayers Int. J. Pharm. 274 2004 221 232 (Pubitemid 38457021)
15. F. Ingels, S. Deferme, E. Destexhe, M. Oth, G. Van den Mooter, and P. Augustijns Simulated intestinal fluid as transport medium in the Caco-2 cell culture model Int. J. Pharm. 232 2002 183 192 (Pubitemid 34076764)
16. M. Kansy, F. Senner, and K. Gubernator Physicochemical high throughput screening: parallel artificial membrane permeation assay in the description of passive absorption processes J. Med. Chem. 41 1998 1007 1010 (Pubitemid 28207375)
17. J. Kanzer, I. Tho, G.E. Flaten, M. Magerlein, P. Holig, G. Fricker, and M. Brandl In-vitro permeability screening of melt extrudate formulations containing poorly water-soluble drug compounds using the phospholipid vesicle-based barrier J. Pharm. Pharmacol. 62 2010 1591 1598
18. M. Kataoka, Y. Masaoka, Y. Yamazaki, T. Sakane, H. Sezaki, and S. Yamashita In vitro system to evaluate oral absorption of poorly water-soluble drugs: simultaneous analysis on dissolution and permeation of drugs Pharm. Res. 20 2003 1674 1680 (Pubitemid 37268286)
19. T. Kimura, H. Sezaki, and K. Kakemi Effect of bile salts on the gastrointestinal absorption of drugs. IV. Site of intestinal absorption of sodium taurocholate and its consequence on drug absorption in the rat Chem. Pharm. Bull. (Tokyo) 20 1972 1656 1662
20. M. Kirjavainen, A. Urtti, I. Jaaskelainen, T.M. Suhonen, P. Paronen, R. Valjakka-Koskela, J. Kiesvaara, and J. Monkkonen Interaction of liposomes with human skin in vitro - the influence of lipid composition and structure Biochim. Biophys. Acta 1304 1996 179 189 (Pubitemid 26426990)
21. K. Kleberg, F. Jacobsen, D.G. Fatouros, and A. Mullertz Biorelevant media simulating fed state intestinal fluids: colloid phase characterization and impact on solubilization capacity J. Pharm. Sci. 99 2010 3522 3532
22. K. Kleberg, J. Jacobsen, and A. Mullertz Characterising the behaviour of poorly water soluble drugs in the intestine: application of biorelevant media for solubility, dissolution and transport studies J. Pharm. Pharmacol. 62 2010 1656 1668
23. G. Krishna, K. Chen, C. Lin, and A.A. Nomeir Permeability of lipophilic compounds in drug discovery using in-vitro human absorption model, Caco-2 Int. J. Pharm. 222 2001 77 89 (Pubitemid 32525789)
24. M. Lakeram, D.J. Lockley, R. Pendlington, and B. Forbes Optimisation of the caco-2 permeability assay using experimental design methodology Pharm. Res. 25 2008 1544 1551
25. P. Lehto, H. Kortejarvi, A. Liimatainen, K. Ojala, H. Kangas, J. Hirvonen, V.P. Tanninen, and L. Peltonen Use of conventional surfactant media as surrogates for FaSSIF in simulating in vivo dissolution of BCS class II drugs Eur. J. Pharm. Biopharm. 78 2011 531 538
26. M.L. Lind, J. Jacobsen, R. Holm, and A. Mullertz Development of simulated intestinal fluids containing nutrients as transport media in the Caco-2 cell culture model: assessment of cell viability, monolayer integrity and transport of a poorly aqueous soluble drug and a substrate of efflux mechanisms Eur. J. Pharm. Sci. 32 2007 261 270 (Pubitemid 350051889)
27. S. Massari, R. Colonna, and E. Folena Interaction of the fluorescent probe N-(lissamine Rhodamine B sulfonyl)dipalmitoylphosphatidylethanolamine with phosphatidylcholine bilayers Biochim. Biophys. Acta 940 1988 149 157
28. J.M. Miller, A. Beig, B.J. Krieg, R.A. Carr, T. Borchardt, G. Amidon, G.L. Amidon, and A. Dahan The solubility-permeability interplay: mechanistic modeling and predictive application of the impact of micellar solubilization on intestinal permeation Mol. Pharm. 2011
29. S.D. Mithani, V. Bakatselou, C.N. TenHoor, and J.B. Dressman Estimation of the increase in solubility of drugs as a function of bile salt concentration Pharm. Res. 13 1996 163 167 (Pubitemid 26076314)
30. J.W. Nichols Low concentrations of bile salts increase the rate of spontaneous phospholipid transfer between vesicles Biochemistry 25 1986 4596 4601
31. P.B. Nielsen, A. Mullertz, T. Norling, and H.G. Kristensen The effect of alpha-tocopherol on the in vitro solubilisation of lipophilic drugs Int. J. Pharm. 222 2001 217 224 (Pubitemid 32568365)
32. N. Patel, B. Forbes, S. Eskola, and J. Murray Use of simulated intestinal fluids with Caco-2 cells and rat ileum Drug Dev. Ind. Pharm. 32 2006 151 161
33. E.M. Persson, A.S. Gustafsson, A.S. Carlsson, R.G. Nilsson, L. Knutson, P. Forsell, G. Hanisch, H. Lennernas, and B. Abrahamsson The effects of food on the dissolution of poorly soluble drugs in human and in model small intestinal fluids Pharm. Res. 22 2005 2141 2151 (Pubitemid 41821594)
34. R. Schubert, K. Beyer, H. Wolburg, and K.H. Schmidt Structural changes in membranes of large unilamellar vesicles after binding of sodium cholate Biochemistry 25 1986 5263 5269
35. R. Schubert, H. Jaroni, J. Schoelmerich, and K.H. Schmidt Studies on the mechanism of bile salt-induced liposomal membrane damage Digestion 28 1983 181 190 (Pubitemid 14215951)
36. R. Schubert, and K.H. Schmidt Structural changes in vesicle membranes and mixed micelles of various lipid compositions after binding of different bile salts Biochemistry 27 1988 8787 8794 (Pubitemid 19008195)
37. H.J. Schwebel, P. van Hoogevest, M.L. Leigh, and M. Kuentz The apparent solubilizing capacity of simulated intestinal fluids for poorly water-soluble drugs Pharm. Dev. Technol. 16 2011 278 286
38. J.J. Sheng, D.P. McNamara, and G.L. Amidon Toward an in vivo dissolution methodology: a comparison of phosphate and bicarbonate buffers Mol. Pharm. 6 2009 29 39
39. S. Thomas, F. Brightman, H. Gill, S. Lee, and B. Pufong Simulation modelling of human intestinal absorption using Caco-2 permeability and kinetic solubility data for early drug discovery J. Pharm. Sci. 97 2008 4557 4574
40. S. Yamashita, T. Furubayashi, M. Kataoka, T. Sakane, H. Sezaki, and H. Tokuda Optimized conditions for prediction of intestinal drug permeability using Caco-2 cells Eur. J. Pharm. Sci. 10 2000 195 204 (Pubitemid 30190095)