Oral bioavailability assessment and intestinal lymphatic transport of Org 45697 and Org 46035, two highly lipophilic novel immunomodulator analogues

Current Drug Delivery

Volumn 6, Issue 4, 2009, Pages 359-366

  Caliph, Suzanne M ^a   Faassen, W A ^b   Vogel, Gerard M ^b   Porter, Christopher J H ^a  

^a MONASH UNIVERSITY   (Australia)

^b Department of Pharmaceutics Schering Plough ^*  (Netherlands)

Author keywords

Drug absorption; Lipid based delivery system; Lymphatic transport; Oral bioavailability

Indexed keywords

IMMUNOMODULATING AGENT; METHYLCELLULOSE; OLIVE OIL; ORG 45697; ORG 46035; POLYSORBATE 80; TRIACYLGLYCEROL; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; DISTRIBUTION VOLUME; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG ELIMINATION; DRUG HALF LIFE; DRUG SOLUBILITY; DRUG TRANSPORT; IMMUNOMODULATION; INTESTINE LYMPH; LIPOPHILICITY; MALE; NONHUMAN; PRIORITY JOURNAL; RAT; SUSPENSION; SYSTEMIC CIRCULATION;

ADMINISTRATION, ORAL; ANIMALS; BIOLOGICAL AVAILABILITY; BIOLOGICAL TRANSPORT; IMMUNOLOGIC FACTORS; INTESTINAL ABSORPTION; LEUCINE; LYMPHATIC SYSTEM; MALE; PLANT OILS; POLYSORBATES; PYRIMIDINES; RATS; RATS, SPRAGUE-DAWLEY; SOLUBILITY; SURFACE-ACTIVE AGENTS;

EID: 68949125157     PISSN: 15672018     EISSN: None     Source Type: Journal    
DOI: 10.2174/156720109789000500     Document Type: Article

References (30)

1. Pouton, C. W. Formulation of poorly water-soluble drugs for oral administration: physicochemical and physiological issues and the lipid formulation classification system. Eur. J. Pharm. Sci., 2006, 29, 278-287
2. Gershkovich, P.; Hoffman, A. 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., 2007, 32, 24-32.
3. Porter, C. J. H.; Trevaskis, N. L.; Charman, W. N. Lipids and lipid-based formulations: optimizing the oral delivery of lipophilic drugs. Nat. Rev. Drug. Discov., 2007, 6, 231-248
4. Trevaskis, N. L.; Charman, W. N.; Porter, C. J. H., Lipid-based delivery systems and intestinal lymphatic drug transport: a mechanistic update. Adv. Drug. Deliv. Rev., 2008, 60, 702-716
5. O'Driscoll, C. M. Lipid-based formulations for intestinal lymphatic delivery. Eur. J. Pharm. Sci., 2002, 15, 405-415
6. O'Driscoll, C. M.; Griffin, B. T., Biopharmaceutical challenges associated with drugs with low aqueous solubility - the potential impact of lipid-based formulations. Adv. Drug. Deliv. Rev., 2008, 60, 617-624
7. Edwards, G. A.; Porter, C. J. H.; Caliph, S. M.; Khoo, S. M.; Charman, W. N. Animal models for the study of intestinal lymphatic drug transport. Adv. Drug. Deliv. Rev., 2001, 50, 45-60.
8. Caliph, S. M.; Charman, W. N.; Porter, C. J. H. 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., 2000, 89, 1073-1084
9. Porter, C. J. H.; Charman, S. A.; Charman, W. N. Lymphatic transport of halofantrine in the triple cannulated anaesthetized model: effect of lipid vehicle dispersion. J. Pharm. Sci., 1996, 85, 351-356.
10. Charman, W. N. Lipids, lipophilic drugs, and oral drug delivery - Some emerging concepts. J. Pharm. Sci. 2000, 89, 967-978.
11. Hauss, D. J.; Fogal, S. E.; Ficorilli, J. V.; Price, C. A.; Roy, T.; Jayaraj, A. A.; Keirns, J. J. Lipid based delivery systems for improving the bioavailability and lymphatic transport of a poorly water soluble LB4 inhibitor. J. Pharm. Sci. 1997, 87, 164-169.
12. Sachs-Barrable, K.; Lee, S. D.; Wasan, E. K.; Thornton, S. J.; Wasan, K. M. Enhancing drug absorption using lipids: a case study presenting the development and pharmacological evaluation of a novel lipid-based oral amphotericin B formulation for the treatment of systemic fungal infections. Adv. Drug. Deliv. Rev., 2008, 60, 692-701.
13. Kossena, G. A.; Charman, W. N.; Wilson, C. G.; O'Mahony, B.; Lindsay, B.; Hempenstall, J. M.; Davison, C. L.; Crowley, P. J.; Porter, C. J. H. Low dose lipid formulations: effects on gastric emptying and biliary secretion. Pharm. Res., 2007, 24, 2084-2096
14. Trevaskis, N. L.; Porter, C. J. H.; Charman, W. N. Bile increases intestinal lymphatic drug transport in the fasted rat. Pharm. Res., 2005, 22, 1863-1870
15. Porter, C. J. H.; Kaukonen, A. M.; Taillardat-Bertschinger, A.; Boyd, B. J.; O'Connor, J. M.; Edwards, G. A.; Charman, W. N. Use of in vitro lipid digestion data to explain the in vivo performance of triglyceride-based oral lipid formulations of poorly water-soluble drugs: studies with halofantrine. J. Pharm. Sci., 2004, 93, 1110-1121
16. Dahan, A.; Hoffman, A. Use of a dynamic in vitro lipolysis model to rationalize oral formulation development for poor water soluble drugs: correlation with in vivo data and the relationship to intraenterocyte processes in rats. Pharm. Res., 2006, 23, 2165-2174
17. Mu, H.; Porsgaard, T. The metabolism of structured triacylglycerols. Prog. Lipid. Res., 2005, 44, 430-448
18. Ahn, H. J.; Kim, K. M.; Kim, C. K. Enhancement of bioavailability of ketoprofen using dry elixir as a novel dosage form. Drug. Dev. Ind. Pharm., 1998, 24, 697-701.
19. Araya, H.; Nagao, S.; Tomita, M.; Hayashi, M. The novel formulation design of self-emulsifying drug delivery systems (SEDDS) type O/W microemulsion I: enhancing effects on oral bioavailability of poorly water soluble compounds in rats and beagle dogs. Drug. Metab. Pharmacokinet., 2005, 20, 244-256
20. Sek, L.; Boyd, B. J.; Charman, W. N.; Porter, C. J. H. Examination of the impact of a range of Pluronic surfactants on the in-vitro solubilisation behaviour and oral bioavailability of lipidic formulations of atovaquone. J. Pharm. Pharmacol., 2006, 58, 809-820
21. Holm, R.; Porter, C. J.; Edwards, G. A.; Mullertz, A.; Kristensen, H. G.; Charman, W. N. Examination of oral absorption and lymphatic transport of halofantrine in a triple-cannulated canine model after administration in self-microemulsifying drug delivery systems (SMEDDS) containing structured triglycerides. Eur. J. Pharm. Sci., 2003, 20, 91-97
22. Ferrier, L.; Berard, F.; Debrauwer, L.; Chabo, C.; Langella, P.; Bueno, L.; Fioramonti, J., Impairment of the intestinal barrier by ethanol involves enteric microflora and mast cell activation in rodents. Am. J. Pathol., 2006, 168, 1148-1154
23. Ma, T. Y.; Nguyen, D.; Bui, V.; Nguyen, H.; Hoa, N., Ethanol modulation of intestinal epithelial tight junction barrier. Am. J. Physiol., 1999, 276, G965-74. (Pubitemid 29214111)
24. Nilsson, L. M.; Sjovall, J.; Strom, S.; Bodin, K.; Nowak, G.; Einarsson, C.; Ellis, E. Ethanol stimulates bile acid formation in primary human hepatocytes. Biochem. Biophys. Res. Commun., 2007, 364, 743-747 (Pubitemid 350087867)
25. Saunders, D. R.; Sillery, J.; McDonald, G. B. Effect of ethanol on transport from rat intestine during high and low rates of oleate absorption. Lipids, 1982, 17, 356-360
26. Mistilis, S. P.; Ockner, R. K. Effects of ethanol on endogenous lipid and lipoprotein metabolism in small intestine. J. Lab. Clin. Med., 1972, 80, 34-46.
27. Baraona, E.; Lieber, C. S. Intestinal lymph formation and fat absorption: stimulation by acute ethanol administration and inhibition by chronic ethanol administration and inhibition by chronic ethanol feeding. Gastroenterology, 1975, 68, 495-502.
28. Porter, C. J. H.; Charman, S. A.; Humberstone, A. J.; Charman, W. N. Lymphatic transport of halofantrine in the conscious rat when administered as either the free base of the hydrochloride salt: Effect of lipid class and lipid vehicle dispersion. J. Pharm. Sci., 1996, 85, 357-361.
29. Griffin, B. T.; O'Driscoll, C. M. A comparison of intestinal lymphatic transport and systemic bioavailability of saquinavir from three lipid-based formulations in the anaesthetised rat model. J. Pharm. Pharmacol., 2006, 58, 917-925
30. Grove, M.; Nielsen, J. L.; Pedersen, G. P.; Mullertz, A. Bioavailability of seocalcitol IV: evaluation of lymphatic transport in conscious rats. Pharm. Res., 2006, 23, 2681-2688 (Pubitemid 44691615)