Examination of the ability of the nasal administration route to confer a brain exposure advantage for three chemical inhibitors of P-glycoprotein

Journal of Pharmaceutical Sciences

Volumn 99, Issue 7, 2010, Pages 3226-3233

  Padowski, Jeannie M ^a   Pollack, Gary M ^a,b  

^a UNIVERSITY OF NORTH CAROLINA SCHOOL OF MEDICINE   (United States)

^b UNIVERSITY OF NORTH CAROLINA   (United States)

Author keywords

Blood brain barrier; CNS; GF120918; Nasal drug delivery; P glycoprotein; Quinidine; Rifampin; Targeted drug delivery; Tissue partition

Indexed keywords

ELACRIDAR; QUINIDINE; RIFAMPICIN;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BLOOD BRAIN BARRIER; BRAIN; COMPARATIVE STUDY; CONTROLLED STUDY; DRUG DELIVERY SYSTEM; DRUG EXPOSURE; INTRANASAL DRUG ADMINISTRATION; MOUSE; NONHUMAN;

EID: 77953315629     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.22070     Document Type: Article

References (28)

1. Pardridge WM. 2005. The blood-brain barrier: Bottleneck in brain drug development. NeuroRx 2:3-14. (Pubitemid 40128022)
2. Illum L. 2000. Transport of drugs from the nasal cavity to the central nervous system. Eur J Pharm Sci 11:1-18. (Pubitemid 30410839)
3. Czerniawska A. 1970. Experimental investigations on the penetration of 198Au from nasal mucous membrane into cerebrospinal fluid. Acta Otolaryngol 70:58-61.
4. Kristensson K, Olsson Y. 1971. Uptake of exogenous proteins in mouse olfactory cells. Acta Neuropathol 19:145-154.
5. Illum L. 2004. Is nose-to-brain transport of drugs in man a reality? J Pharm Pharmacol 56:3-17.
6. Mathison S, Nagilla R, Kompella UB. 1998. Nasal route for direct delivery of solutes to the central nervous system: Fact or fiction? J Drug Target 5:415-441. (Pubitemid 28499678)
7. Merkus FW, van den Berg MP. 2007. Can nasal drug delivery bypass the blood-brain barrier? Questioning the direct transport theory. Drugs R D 8:133-144.
8. Kiec-Kononowicz K, Stadnicka K, Mitka A, Pekala E, Filipek B, Sapa J, Zygmunt M. 2003. Synthesis, structure and antiarrhythmic properties evaluation of new basic derivatives of 5,5-diphenylhydantoin. Eur J Med Chem 38:555-566. (Pubitemid 36773860)
9. Courtney KR. 1987. Quantitative structure/activity relations based on use-dependent block and repriming kinetics in myocardium. J Mol Cell Cardiol 19:319-330.
10. Kalvass JC, Maurer TS, Pollack GM. 2007. Use of plasma and brain unbound fractions to assess the extent of brain distribution of 34 drugs: Comparison of unbound concentration ratios to in vivo p-glycoprotein efflux ratios. Drug Metab Dispos 35:660-666.
11. Al-Maaieh A, Flanagan DR. 2001. Salt and cosolvent effects on ionic drug loading into microspheres using an O/W method. J Control Release 70:169-181. (Pubitemid 32144801)
12. Ward KW, Azzarano LM. 2004. Preclinical pharmacokinetic properties of the P-glycoprotein inhibitor GF120918A (HCl salt of GF120918, 9, 10-dihydro-5-methoxy-9-oxo-N-[4-[2-(1,2,3,4-tetrahydro-6,7-dimethoxy-2-i soquinolinyl)ethyl]phenyl]-4-acridine-carboxamide) in the mouse, rat, dog, and monkey. J Pharmacol Exp Ther 310:703-709.
13. PJ, Young DB, (eds.) 2008. Rifampin. Tuberculosis (Edinb) 88: 151-154.
14. Gallo GG, Radaelli P. 1976. Rifampin. In: Florey K, editor. Analytical profiles of drug substances, 5 edition. New York: Academic Press. p 467.
15. Weiss J, Haefeli WE. 2006. Evaluation of inhibitory potencies for compounds inhibiting P-glycoprotein but without maximum effects: F2 values. Drug Metab Dispos 34: 203-207. (Pubitemid 43145021)
16. Zong J, Pollack GM. 2003. Modulation of P-glycoprotein transport activity in the mouse blood-brain barrier by rifampin. J Pharmacol Exp Ther 306:556-562. (Pubitemid 36886154)
17. Demeule M, Regina A, Jodoin J, Laplante A, Dagenais C, Berthelet F, Moghrabi A, Beliveau R. 2002. Drug transport to the brain: Key roles for the efflux pump P-glycoprotein in the blood-brain barrier. Vasc Pharmacol 38:339-348. (Pubitemid 36398255)
18. Leonard GD, Polgar O, Bates SE. 2002. ABC transporters and inhibitors: New targets, new agents. Curr Opin Invest Drugs 3:1652-1659. (Pubitemid 36266743)
19. McDevitt CA, Callaghan R. 2007. How can we best use structural information on P-glycoprotein to design inhibitors? Pharmacol Ther 113:429-441.
20. Dogrukol-Ak D, Kumar VB, Ryerse JS, Farr SA, Verma S, Nonaka N, Nakamachi T, Ohtaki H, Niehoff ML, Edwards JC, Shioda S, Morley JE, Banks WA. 2009. Isolation of peptide transport system-6 from brain endothelial cells: Therapeutic effects with antisense inhibition in Alzheimer and stroke models. J Cereb Blood Flow Metab 29:411-422.
21. Marzolini C, Paus E, Buclin T, Kim RB. 2004. Polymorphisms in human MDR1 (P-glycoprotein): Recent advances and clinical relevance. Clin Pharmacol Ther 75:13-33. (Pubitemid 38130115)
22. Gross EA, Swenberg JA, Fields S, Popp JA. 1982. Comparative morphometry of the nasal cavity in rats and mice. J Anat 135:83-88. (Pubitemid 12041734)
23. Dagenais C, Rousselle C, Pollack GM, Scherrmann JM. 2000. Development of an in situ mouse brain perfusion model and its application to mdr1a P-glycoprotein-deficient mice. J Cereb Blood Flow Metab 20:381-386. (Pubitemid 30108457)
24. Bailer AJ. 1988. Testing for the equality of area under the curves when using destructive measurement techniques. J Pharmacokinet Biopharm 16:303-309.
25. Hebert MF, Fisher RM, Marsh CL, Dressler D, Bekersky I. 1999. Effects of rifampin on tacrolimus pharmacokinetics in healthy volunteers. J Clin Pharmacol 39:91-96. (Pubitemid 29053157)
26. Graff CL, Pollack GM. 2005. Functional evidence for P-glycoprotein at the nose-brain barrier. Pharm Res 22:86-93. (Pubitemid 40558150)
27. Costantino HR, Illum L, Brandt G, Johnson PH, Quay SC. 2007. Intranasal delivery: Physicochemical and therapeutic aspects. Int J Pharm 337:1-24. (Pubitemid 46756063)
28. Moran DT, Rowley JC III, Jafek BW, Lovell MA. 1982. The fine structure of the olfactory mucosa in man. J Neurocytol 11:721-746.