The impact of lymphatic transport on the systemic disposition of lipophilic drugs

Journal of Pharmaceutical Sciences

Volumn 102, Issue 7, 2013, Pages 2395-2408

  Caliph, Suzanne M ^a   Cao, Enyuan ^a   Bulitta, Jürgen B ^a   Hu, Luojuan ^a   Han, Sifei ^a   Porter, Christopher J H ^a   Trevaskis, Natalie L ^a  

^a MONASH UNIVERSITY   (Australia)

Author keywords

Absorption; Clearance; Disposition; Distribution; Intravenous; Lipids; Lipoproteins; Lymphatic transport; Oral absorption; Pharmacokinetics

Indexed keywords

CHLORPHENOTANE; HALOFANTRINE; LIPID; LIPOPROTEIN;

ADIPOSE TISSUE; ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; DRUG ABSORPTION; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG ELIMINATION; DRUG HALF LIFE; DRUG TRANSPORT; INTESTINE; LIPOPHILICITY; LYMPH; LYMPHATIC SYSTEM; NONHUMAN; PLASMA; RAT; TISSUE DISTRIBUTION; VASCULARIZATION;

EID: 84879024116     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.23597     Document Type: Article

References (51)

1. Mansbach CM, Dowell RF, Pritchett D. 1991. Portal transport of absorbed lipids in rats. Am J Physiol 261(3):G530-G538.
2. Nordskog BK, Phan CT, Nutting DF, Tso P. 2001. An examination of the factors affecting intestinal lymphatic transport of dietary lipids. Adv Drug Deliv Rev 50(1-2):21-44.
3. Trevaskis NL, Charman WN, Porter CJ. 2008. Lipid-based delivery systems and intestinal lymphatic drug transport: A mechanistic update. Adv Drug Deliv Rev 60(6):702-716.
4. Williams HD, Trevaskis NL, Charman SA, Shanker RM, Charman WN, Pouton CW, Porter CJ. 2013. Strategies to address low drug solubility in discovery and development. Pharmacol Rev 65(1):315-499.
5. Caliph SM, Charman WN, Porter CJ. 2000. Effect of short-, medium-, and long-chain fatty acid-based vehicles on the absolute oral bioavailability and intestinal lymphatic transport of halofantrine and assessment of mass balance in lymph-cannulated and non-cannulated rats. J Pharm Sci 89(8):1073-1084.
6. Dixon JB. 2010. Mechanisms of chylomicron uptake into lacteals. Ann N Y Acad Sci 1207 Suppl 1:E52-E57.
7. Chaikoff IL, Bloom B, Stevens BP, Reinhardt WO, Dauben WG. 1951. Pentadecanoic acid-5-C14; its absorption and lymphatic transport. J Biol Chem 190(2):431-435.
8. Bloom B, Chaikoff IL, Reinhardt. 1951. Intestinal lymph as pathway for transport of absorbed fatty acids of different chain lengths. Am J Physiol 166(2):451-455.
9. Kiyasu JY, Bloom B, Chaikoff IL. 1952. The portal transport of absorbed fatty acids. J Biol Chem 199(1):415-419.
10. Porter CJ, Charman SA, Charman WN. 1996. Lymphatic transport of halofantrine in the triple-cannulated anesthetized rat model: Effect of lipid vehicle dispersion. J Pharm Sci 85(4):351-356.
11. Charman WN, Stella VJ. 1986. Estimating the maximum potential for intestinal lymphatic transport of lipophilic drug molecules. Int J Pharm 34:175-178.
12. Gershkovich P, Fanous J, Qadri B, Yacovan A, Amselem S, Hoffman A. 2009. The role of molecular physicochemical properties and apolipoproteins in association of drugs with triglyceride-rich lipoproteins: In-silico prediction of uptake by chylomicrons. J Pharm Pharmacol 61(1):31-39.
13. Trevaskis NL, Shanker RM, Charman WN, Porter CJ. 2010. The mechanism of lymphatic access of two cholesteryl ester transfer protein inhibitors (CP524, 515 and CP532, 623) and evaluation of their impact on lymph lipoprotein profiles. Pharm Res 27(9):1949-1954.
14. Trevaskis NL, McEvoy CL, McIntosh MP, Edwards GA, Shanker RM, Charman WN, Porter CJ. 2010. The role of the intestinal lymphatics in the absorption of two highly lipophilic cholesterol ester transfer protein inhibitors (CP524, 515 and CP532, 623). Pharm Res 27(5):878-893.
15. Porter CJ, Trevaskis NL, Charman WN. 2007. Lipids and lipid-based formulations: Optimizing the oral delivery of lipophilic drugs. Nat Rev Drug Discov 6(3):231-248.
16. Wasan KM, Brocks DR, Lee SD, Sachs-Barrable K, Thornton SJ. 2008. Impact of lipoproteins on the biological activity and disposition of hydrophobic drugs: Implications for drug discovery. Nat Rev Drug Discov 7(1):84-99.
17. Gershkovich P, Hoffman A. 2007. Effect of a high-fat meal on absorption and disposition of lipophilic compounds: The importance of degree of association with triglyceride-rich lipoproteins. Eur J Pharm Sci 32(1):24-32.
18. Gershkovich P, Shtainer D, Hoffman A. 2007. The effect of a high-fat meal on the pharmacodynamics of a model lipophilic compound that binds extensively to triglyceride-rich lipoproteins. Int J Pharm 333(1-2):1-4.
19. Trevaskis NL, Charman WN, Porter CJ. 2010. Targeted drug delivery to lymphocytes: A route to site-specific immunomodulation? Mol Pharm 7(6):2297-2309.
20. Caliph SM, Trevaskis NL, Charman WN, Porter CJ. 2012. Intravenous dosing conditions may affect systemic clearance for highly lipophilic drugs: Implications for lymphatic transport and absolute bioavailability studies. J Pharm Sci 101:3540-3546.
21. Pocock DE, Vost A. 1974. DDT absorption and chylomicron transport in rat. Lipids 9(6):374-381.
22. Noguchi T, Charman WNA, Stella VJ. 1985. Lymphatic appearance of DDT in thoracic or mesenteric lymph duct cannulated rats. Int J Pharm 24(2-3):185-192.
23. Gershkovich P, Hoffman A. 2005. Uptake of lipophilic drugs by plasma derived isolated chylomicrons: Linear correlation with intestinal lymphatic bioavailability. Eur J Pharm Sci 26(5):394-404.
24. Johnson BM, Chen W, Borchardt RT, Charman WN, Porter CJ. 2003. A kinetic evaluation of the absorption, efflux, and metabolism of verapamil in the autoperfused rat jejunum. J Pharmacol Exp Ther 305(1):151-158.
25. Trevaskis NL, Porter CJ, Charman WN. 2005. Bile increases intestinal lymphatic drug transport in the fasted rat. Pharm Res 22(11):1863-1870.
26. Edwards GA, Porter CJ, Caliph SM, Khoo SM, Charman WN. 2001. Animal models for the study of intestinal lymphatic drug transport. Adv Drug Deliv Rev 50(1-2):45-60.
27. Trevaskis NL, Caliph SM, Nguyen G, Tso P, Charman WN, Porter CJ. 2013. A mouse model to evaluate the impact of species, sex, and lipid load on lymphatic drug transport. Pharm Res.
28. Caliph SM, Trevaskis NL, Charman WN, Porter CJ. 2012. Intravenous dosing conditions may affect systemic clearance for highly lipophilic drugs: Implications for lymphatic transport and absolute bioavailability studies. J Pharm Sci 101(9):3540-3546.
29. Bauer RJ, Guzy S, Ng C. 2007. A survey of population analysis methods and software for complex pharmacokinetic and pharmacodynamic models with examples. AAPS J 9(1):E60-E83.
30. Bulitta JB, Bingolbali A, Shin BS, Landersdorfer CB. 2011. Development of a new pre- and post-processing tool (SADAPT-TRAN) for nonlinear mixed-effects modeling in S-ADAPT. AAPS J 13(2):201-211.
31. Beal SL. 2001. Ways to fit a PK model with some data below the quantification limit. J Pharm Pharmacodyn 28(5):481-504.
32. Bulitta JB, Okusanya OO, Forrest A, Bhavnani SM, Clark K, Still JG, Fernandes P, Ambrose PG. 2013. Population pharmacokinetics of fusidic acid: Rationale for front-loaded dosing regimens due to autoinhibition of clearance. Antimicrob Agents Chemother 57(1):498-507.
33. Belfrage P, Borgström B, Olivecrona T. 1963. The tissue distribution of radioactivity following the injection of varying levels of fatty acid labeled chylomicrons in the rat. Acta Physiol Scand 58(2-3):111-123.
34. Olivecrona T. 1962. The metabolism of 1-C14-palmitic acid labeled chylomicrons in rats. Acta Physiol Scand 55(2-3):170-176.
35. Bragdon JH, Gordon RS, Jr. 1958. Tissue distribution of C14 after the intravenous injection of labeled chylomicrons and unesterified fatty acids in the rat. J Clin Invest 37(4):574-578.
36. Schemmel R, Mickelsen O, Gill JL. 1970. Dietary obesity in rats: Body weight and body fat accretion in seven strains of rats. J Nutr 100(9):1041-1048.
37. Stimpson SA, Turner SM, Clifton LG, Poole JC, Mohammed HA, Shearer TW, Waitt GM, Hagerty LL, Remlinger KS, Hellerstein MK, Evans WJ. 2012. Total-body creatine pool size and skeletal muscle mass determination by creatine-(methyl-d3) dilution in rats. J Appl Physiol 112(11):1940-1948.
38. Arola L, Herrera E, Alemany M. 1979. A method for the estimation of striated muscle mass in small laboratory animals. Revista Espanola de Fisiologia 35(2):215-218.
39. Bragdon JH. 1958. C1402 excretion after the intravenous administration of labeled chylomicrons in the rat. Arch Biochem Biophys 75(2):528-533.
40. Mc CC, Gates HS, c., Gordon RS, Jr. 1957. C1402 Excretion after the intravenous administration of albumin-bound palmitate-1-C14 to intact rats. Arch Biochem Biophys 71(2):346-351.
41. Wasan KM, Pritchard PH, Ramaswamy M, Wong W, Donnachie EM, Brunner LJ. 1997. Differences in lipoprotein lipid concentration and composition modify the plasma distribution of cyclosporine. Pharm Res 14(11):1613-1620.
42. Humberstone AJ, Porter CJ, Edwards GA, Charman WN. 1998. Association of halofantrine with postprandially derived plasma lipoproteins decreases its clearance relative to administration in the fasted state. J Pharm Sci 87(8):936-942.
43. Hauss DJ, Mehta SC, Radebauch GW. 1994. Targeted lymphatic transport and modified systemic distribution of CI-976, a lipophilic lipid-regulator drug, via a formulation approach. Int J Pharm 108(2):85-93.
44. Vost A, Maclean N. 1984. Hydrocarbon transport in chylomicrons and high-density lipoproteins in rat. Lipids 19(6):423-435.
45. Mohammed A, Eklund A, Ostlund-Lindqvist AM, Slanina P. 1990. Distribution of toxaphene, DDT, and PCB among lipoprotein fractions in rat and human plasma. Arch Toxicol 64(7):567-571.
46. Trevaskis NL, Tso P, Rider T, Charman WN, Porter CJ, Jandacek R. 2006. Tissue uptake of DDT is independent of chylomicron metabolism. Arch Toxicol 80(4):196-200.
47. Kohan AB, Vandersall AE, Yang Q, Xu M, Jandacek RJ, Tso P. 2013. The transport of DDT from chylomicrons to adipocytes does not mimic triacylglycerol transport. Biochim Biophys Acta 1831(2):300-305.
48. Maliwal BP, Guthrie FE. 1982. In vitro uptake and transfer of chlorinated hydrocarbons among human lipoproteins. J Lipid Res 23(3):474-479.
49. McIntosh MP, Porter CJ, Wasan KM, Ramaswamy M, Charman WN. 1999. Differences in the lipoprotein binding profile of halofantrine in fed and fasted human or beagle plasma are dictated by the respective masses of core apolar lipoprotein lipid. J Pharm Sci 88(3):378-384.
50. Patel JP, Fleischer JG, Wasan KM, Brocks DR. 2009. The effect of experimental hyperlipidemia on the stereoselective tissue distribution, lipoprotein association and microsomal metabolism of (+/-)-halofantrine. J Pharm Sci 98(7):2516-2528.
51. Brocks DR, Wasan KM. 2002. The influence of lipids on stereoselective pharmacokinetics of halofantrine: Important implications in food-effect studies involving drugs that bind to lipoproteins. J Pharm Sci 91(8):1817-1826.