Evidence-based approach to assess passive diffusion and carrier-mediated drug transport

Drug Discovery Today

Volumn 17, Issue 15-16, 2012, Pages 905-912

  Di, Li ^a   Artursson, Per ^b   Avdeef, Alex ^c   Ecker, Gerhard F ^d   Faller, Bernard ^e   Fischer, Holger ^f   Houston, J Brian ^g   Kansy, Manfred ^f   Kerns, Edward H ^h   Krämer, Stefanie D ⁱ   Lennernäs, Hans ^b   Sugano, Kiyohiko ^j,k  

^a PFIZER INC   (United States)

^b UPPSALA UNIVERSITY   (Sweden)

^c In ADME Research   (United States)

^d UNIVERSITY OF VIENNA   (Austria)

^e NOVARTIS PHARMA AG   (Switzerland)

^f F HOFFMANN LA ROCHE LTD   (Switzerland)

^g UNIVERSITY OF MANCHESTER   (United Kingdom)

^h NATIONAL INSTITUTES OF HEALTH   (United States)

ⁱ ETH ZURICH   (Switzerland)

^j PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United Kingdom)

^k Asahi Kasei Pharma Corporation   (Japan)

more..

Author keywords

[No Author keywords available]

Indexed keywords

4 NITROPHENOL; AMINO ACID TRANSPORTER; ATENOLOL; DRUG CARRIER; GABAPENTIN; LEVODOPA; SMALL MOLECULE TRANSPORT AGENT; TERBUTALINE;

ACTIVE TRANSPORT; BLOOD BRAIN BARRIER; CELL LINE; CELL MEMBRANE; CELL STRAIN; CELL STRAIN CACO 2; DIFFUSION; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG DESIGN; DRUG PENETRATION; DRUG TRANSPORT; EVIDENCE BASED PRACTICE; HUMAN; IONIZATION; LIPID MEMBRANE; LIPOPHILICITY; MEMBRANE TRANSPORT; PROCESS OPTIMIZATION; PUBLISHING; REVIEW;

ANIMALS; BIOLOGICAL TRANSPORT; CARRIER PROTEINS; CELL MEMBRANE PERMEABILITY; DIFFUSION; DRUG CARRIERS; HUMANS; MEMBRANES, ARTIFICIAL; PHARMACEUTICAL PREPARATIONS; PHARMACOKINETICS;

EID: 84864612910     PISSN: 13596446     EISSN: 18785832     Source Type: Journal    
DOI: 10.1016/j.drudis.2012.03.015     Document Type: Review

References (56)

1. P.D. Dobson, and D.B. Kell Carrier-mediated cellular uptake of pharmaceutical drugs: an exception or the rule? Nat. Rev. Drug Discov. 7 2008 205 220 (Pubitemid 351321232)
2. K. Sugano Coexistence of passive and carrier-mediated processes in drug transport Nat. Rev. Drug Discov. 9 2010 597 614
3. D.B. Kell Pharmaceutical drug transport: the issues and the implications that it is essentially carrier-mediated only Drug Discov. Today 16 2011 704 714
4. H. Sasabe Carrier-mediated hepatic uptake of quinolone antibiotics in the rat J. Pharmacol. Exp. Ther. 282 1997 162 171 (Pubitemid 27425538)
5. Y. Shirasaka Intestinal absorption of HMG-CoA reductase inhibitor pitavastatin mediated by organic anion transporting polypeptide and P-glycoprotein/multidrug resistance 1 Drug Metab. Pharmacokinet. 26 2011 171 179
6. D. Jappar Effect of dose escalation on the in vivo oral absorption and disposition of glycylsarcosine in wild-type and Pept1 knockout mice Drug Metab. Dispos. 39 2011 2250 2257
7. D. Jappar Significance and regional dependency of peptide transporter (PEPT) 1 in the intestinal permeability of glycysarcosine: in situ single-pass perfusion studies in wild-type and Pept1 knockout mice Drug Metab. Dispos. 38 2010 1740 1746
8. A. Yamazaki Microdose study of a P-glycoprotein substrate, fexofenadine, using a non-radioisotope-labelled drug and LC/MS/MS J. Clin. Pharm. Ther. 35 2010 169 175
9. K. Maeda Identification of the rate-determining process in the hepatic clearance of atorvastatin in a clinical cassette microdosing study Clin. Pharmacol. Ther. 90 2011 575 581
10. K. Maeda Nonlinear pharmacokinetics of oral quinidine and verapamil in healthy subjects: a clinical microdosing study Clin. Pharmacol. Ther. 90 2011 263 270
11. Y. Yabe Kinetic characterization of rat hepatic uptake of 16 actively transported drugs Drug Metab. Dispos. 39 2011 1808 1814
12. R. Christon Modification of fluidity and lipid-protein relationships in pig intestinal brush-border membrane by dietary essential fatty acid deficiency Biochim. Biophys. Acta: Biomembr. 980 1989 77 84 (Pubitemid 19078306)
13. P. Quinn Density of newly synthesized plasma membrane proteins in intracellular membranes. II. Biochemical studies J. Cell Biol. 98 1984 2142 2147 (Pubitemid 14121844)
14. P. Laeuger Relaxation studies of ion transport systems in lipid bilayer membranes Q. Rev. Biophys. 14 1981 513 598
15. H. Leontiadou Molecular dynamics simulations of hydrophilic pores in lipid bilayers Biophys. J. 86 2004 2156 2164 (Pubitemid 38524406)
16. H. Leontiadou Ion transport across transmembrane pores Biophys. J. 92 2007 4209 4215 (Pubitemid 46910537)
17. S. Paula Permeation of halide anions through phospholipid bilayers occurs by the solubility-diffusion mechanism Biophys. J. 74 1998 319 327 (Pubitemid 28041759)
18. O. Sandre Dynamics of transient pores in stretched vesicles Proc. Natl. Acad. Sci. U. S. A. 96 1999 10591 10596 (Pubitemid 29442188)
19. S. Lesieur Evidence of surfactant-induced formation of transient pores in lipid bilayers by using magnetic-fluid-loaded liposomes J. Am. Chem. Soc. 125 2003 5266 5267 (Pubitemid 36582722)
20. S.K. Kandasamy, and R.G. Larson Cation and anion transport through hydrophilic pores in lipid bilayers J. Chem. Phys. 125 2006 074901
21. S.D. Kramer, and H. Wunderli-Allenspach No entry for TAT(44-57) into liposomes and intact MDCK cells: novel approach to study membrane permeation of cell-penetrating peptides Biochim. Biophys. Acta: Biomembr. 1609 2003 161 169 (Pubitemid 36120723)
22. A.V. Thomae Comparing the lipid membrane affinity and permeation of drug-like acids: the intriguing effects of cholesterol and charged lipids Pharm. Res. 24 2007 1457 1472 (Pubitemid 46988212)
23. A.V. Thomae Permeation of aromatic carboxylic acids across lipid bilayers: the pH-partition hypothesis revisited Biophys. J. 89 2005 1802 1811 (Pubitemid 41233535)
24. A.C. Chakrabarti, and D.W. Deamer Permeability of lipid bilayers to amino acids and phosphate Biochim. Biophys. Acta: Biomembr. 1111 1992 171 177
25. M. Romanowski Interaction of enkephalin peptides with anionic model membranes Biochim. Biophys. Acta: Biomembr. 1558 2002 45 53 (Pubitemid 34031953)
26. Y.N. Antonenko, and A.A. Bulychev Measurements of local pH changes near bilayer lipid membrane by means of a pH microelectrode and a protonophore-dependent membrane potential. Comparison of the methods Biochim. Biophys. Acta: Biomembr. 1070 1991 279 282
27. P.T. Mayer Independence of substituent contributions to the transport of small molecule permeants in lipid bilayers AAPS PharmSci. 2 2000 14
28. T.X. Xiang, and B.D. Anderson Influence of a transmembrane protein on the permeability of small molecules across lipid membranes J. Membr. Biol. 173 2000 187 201 (Pubitemid 30100211)
29. H.T. Tien, and A. Ottova-Leitmannova Planar lipid biylayers and spherical liposomes Membrane biophysics as viewed from experimental bilayer lipid membranes Vol. 5 2000 Elsevier 178-265
30. F. Wohnsland, and B. Faller High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes J. Med. Chem. 44 2001 923 930 (Pubitemid 32861617)
31. O. Tsinman Physicochemical selectivity of the BBB microenvironment governing passive diffusion-matching with a porcine brain lipid extract artificial membrane permeability model Pharm. Res. 28 2011 337 363
32. A. Avdeef Caco-2 permeability of weakly basic drugs predicted with the Double-Sink PAMPA pKfluxa method Eur. J. Pharm. Sci. 24 2005 333 349 (Pubitemid 40283516)
33. T. Korjamo The asymmetry of the unstirred water layer in permeability experiments Pharm. Res. 25 2008 1714 1722
34. M. Velicky In situ artificial membrane permeation assay under hydrodynamic control: permeability-pH profiles of warfarin and verapamil Pharm. Res. 27 2010 1644 1658
35. N. Nagahara Contribution of the paracellular route to the pH-dependent epithelial permeability to cationic drugs J. Pharm. Sci. 93 2004 2972 2984 (Pubitemid 39657801)
36. P. Matsson Exploring the role of different drug transport routes in permeability screening J. Med. Chem. 48 2005 604 613 (Pubitemid 40139802)
37. D. Sun 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 2002 1400 1416 (Pubitemid 35266543)
38. A. Avdeef, and K.Y. Tam How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability? J. Med. Chem. 53 2010 3566 3584
39. W.S. Putnam Functional characterization of monocarboxylic acid, large neutral amino acid, bile acid and peptide transporters, and P-glycoprotein in MDCK and Caco-2 cells J. Pharm. Sci. 91 2002 2622 2635 (Pubitemid 35379420)
40. H. Lennernaes Comparison between active and passive drug transport in human intestinal epithelial (Caco-2) cells in vitro and human jejunum in vivo Int. J. Pharm. 127 1996 103 107
41. S.D. Kraemer Lipid-bilayer permeation of drug-like compounds Chem. Biodivers. 6 2009 1900 1916
42. P.D. Dobson Metabolite-likeness as a criterion in the design and selection of pharmaceutical drug libraries Drug Discov. Today 14 2009 31 40
43. C. Yang Prodrug based optimal drug delivery via membrane transporter/receptor Expert Opin Biol. Ther. 1 2001 159 175 (Pubitemid 33770074)
44. S. Majumdar Membrane transporter/receptor-targeted prodrug design: strategies for human and veterinary drug development Adv. Drug Deliv. Rev. 56 2004 1437 1452 (Pubitemid 38748825)
45. B. Pavan Progress in drug delivery to the central nervous system by the prodrug approach Molecules 13 2008 1035 1065
46. M. Gynther Large neutral amino acid transporter enables brain drug delivery via prodrugs J. Med. Chem. 51 2008 932 936 (Pubitemid 351304700)
47. M. Gynther Glucose promoiety enables glucose transporter mediated brain uptake of ketoprofen and indomethacin prodrugs in rats J. Med. Chem. 52 2009 3348 3353
48. E.M. del Amo Pharmacokinetic role of l-type amino acid transporters LAT1 and LAT2 Eur. J. Pharm. Sci. 35 2008 161 174
49. X. Liu, and C. Chen Strategies to optimize brain penetration in drug discovery Curr. Opin. Drug Discov. Dev. 8 2005 505 512 (Pubitemid 40917412)
50. A. Doran The impact of P-glycoprotein on the disposition of drugs targeted for indications of the central nervous system: evaluation using the MDR1A/1B knockout mouse model Drug Metab. Dispos. 33 2005 165 174 (Pubitemid 40023528)
51. M. Hammarlund-Udenaes On the rate and extent of drug delivery to the brain Pharm. Res. 25 2008 1737 1750
52. L. Di Strategies to assess blood-brain barrier penetration Expert Opin Drug Discov. 3 2008 677 687 (Pubitemid 351890679)
53. A. Schlessinger Comparison of human solute carriers Protein Sci. 19 2010 412 428
54. M. Kansy 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)
55. F.T. Huque Permeability through DOPC/dodecane membranes: measurement and LFER modeling Eur. J. Pharm. Sci. 23 2004 223 232 (Pubitemid 39369877)
56. H. Fischer Permeation of permanently positive charged molecules through artificial membranes - influence of physico-chemical properties Eur. J. Pharm. Sci. 31 2007 32 42 (Pubitemid 46601866)