Absorption barriers in the rat intestinal mucosa. 3: Effects of polyethoxylated solubilizing agents on drug permeation and metabolism

Journal of Pharmaceutical Sciences

Volumn 99, Issue 2, 2010, Pages 1016-1027

  Mudra, Daniel R ^a,b   Borchardt, Ronald T ^a  

^a UNIVERSITY OF KANSAS   (United States)

^b ELI LILLY AND COMPANY   (United States)

Author keywords

Cytochrome P450; Excipients; Ileum; Intestinal absorption; Intestinal metabolism; Jejunum; P glycoprotein; Passive diffusion transport; Permeability; Permeation enhancers

Indexed keywords

ATENOLOL; CREMOPHOR; CYTOCHROME P450 3A; GLYCOPROTEIN P; KETOCONAZOLE; MACROGOL; NORVERAPAMIL; POLYSORBATE 80; SOLUBILIZER; SUCCINIC ACID DERIVATIVE; VERAPAMIL;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; DRUG ABSORPTION; DRUG INHIBITION; DRUG METABOLISM; DRUG PENETRATION; INCUBATION TIME; INTESTINE MUCOSA; INTESTINE PERFUSION; MALE; MICROSOME; NONHUMAN; RAT;

EID: 74049147801     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.21836     Document Type: Article

References (27)

1. Hageman MJ. 2006. Solubility, solubilization and dissolution in drug delivery during lead optimization. In: Borchardt RT, Kerns EH, Hageman MJ, Thakker DR, Stevens JL, editors. Optimzing the "drug-like" properties of leads in drug discovery. New York: AAPS Press/Springer, New York.
2. Kim HJ, Bruckner JV, Dallas CE, Gallo JM. 1990. Effect of dosing vehicles on the pharmacokinetics of orally administered carbon tetrachloride in rats. Tox Appl Pharm 102:50-60.
3. Hermansky SJ, Neptun DA, Loughran KA, Leung HW. 1995. Effects of polyethylene glycol 400 (PEG 400) following 13 weeks of gavage treatment in Fischer-344 rats. Food Chem Toxicol 33:139-149.
4. Gao P, Guyton ME, Huang T, Bauer JM, Stefanski KJ, Lu Q. 2004. Enhanced oral bioavailability of a poorly water soluble drug PNU-91325 by supersaturatable formulations. Drug Dev Ind Pharm 30:221-229.
5. Takahashi Y, Kondo H, Yasuda T, Watanabe T, Kobayashi S, Yokohama S. 2002. Common solubilizers to estimate the Caco-2 transport of poorly water-soluble drugs. Int J Pharm 246:85-94.
6. Wacher VJ, Wong S, Wong HT. 2002. Peppermint oil enhances cyclosporine oral bioavailability in rats: Comparison with D-alpha-tocopheryl poly(-ethylene glycol 1000) succinate (TPGS) and ketoconazole. J Pharm Sci 91:77-90.
7. Varma MVS, Panchagnual R. 2005. Enhanced paclitaxel absorption with vitamin E-TPGS: Effect on solubility and permeability in vitro, in situ and in vivo. Eur J Pharm Sci 25:445-453.
8. Dintaman JM, Silverman JA. 1999. Inhibition of P-glycoprotein by D-alpha-tocopheryl polyethylene glycol 1000 succinate (TPGS). Pharm Res 16:1550-1556.
9. Woodcock DM, Linsenmeyer ME, Chojnowski G, Kriegler AB, Nink V, Webster LK, Sawyer WH. 1992. Reversal of multidrug resistance by surfactants. Br J Cancer 66:62-68.
10. Hugger ED, Novak BL, Burton PS, Audus KL, Borchardt RT. 2002b. A comparison of commonly used polyethoxylated pharmaceutical excipients on their ability to inhibit p-glycoprotein activity in vitro. J Pharm Sci 91:1991-2002.
11. Katneni K, Charman S, Porter CJ. 2007. Impact of cremophor-EL and polysorbate-80 on digoxin permeability across rat jejunum: Delineation of thermodynamic and transporter related events using the reciprocal permeability approach. J Pharm Sci 96:280-293.
12. Hugger ED, Audus KL, Borchardt RT. 2002a. Effects of poly(ethylene glycol) on efflux transporter activity in caco-2 cell monolayers. J Pharm Sci 91:1980-1990.
13. Johnson BM, Charman WN, Porter CJH. 2002. An in vitro examination of the impact of polyethylene glycol 400, pluronic P85, and vitamin E d-a-tocopheryl polyethylene glycol 1000 succinate on p-glycoprotein efflux and enterocyte based metabolism in excised rat intestine. AAPS Pharm Sci 4:40, 1-13.
14. Regev R, Assaraf YG, Eytan GD. 1999. Membrane fluidization by ether, other anesthetics, and certain agents abolishes P-glycoprotein ATPase activity and modulates efflux from multidrug-resistant cells. Eur J Biochem 259:18-24.
15. Batrakova EV, Li S, Vinogradov SV, Alakhov VY, Miller DW, Kabanov AV. 2001. Mechanism of pluronic effect on P-glycoprotein efflux system in bloodbrain barrier: Contributions of energy depletion and membrane fluidization. JPET 299:483-493.
16. Rege BD, Kao JPY, Polli JE. 2002. Effects of nonionic surfactants on membrane transporters in Caco-2 cell monolayers. Eur J Pharm Sci 16:237-246.
17. Johnson BM, Chen W, Borhcardt RT, Charman WN, Porter CJH. 2003a. A kinetic evaluation of the absorption, efflux, and metabolism of verapamil in the autoperfused rat jejunum. J Pharm Exp Ther 305:151-158.
18. Mudra DM, Borchardt RT. Absorption barriers in the rat intestinal mucosa. 1. Application of an in situ perfusion model to simultaneously assess drug permeation and metabolism. J Pharm Sci (submitted for publication).
19. Neuhoff S, Langguth P, Dressler C, Anderson TB, Regardh CG, Spahn-Langguth H. 2000. Affinities at the verapamil binding site of MDR1-encoded P-glycoprotein: Drugs and analogs, stereoisomers and metabolites. Int J Clin Pharmacol Ther 38:168-179.
20. Nerurkar MM, Ho NFH, Burton PS, Vidmar TJ, Borchardt RT. 1997. Mechanistic roles of neutral surfactants on concurrent polarized and passive membrane transport of a model peptide in caco-2 cells. J Pharm Sci 86:813-821.
21. Price JC. 2000. Polyethylene glycol. In: Kibbe AH, editor. Handbook of pharmaceutical excipients. 3rd edition. Washington, DC/London, United Kingdom: American Pharmaceutical Association/The Pharmaceutical Press. pp. 392-398.
22. Shen Q, Lin Y, Handa T, Masamichi D, Sugie M, Wakayama K, Okada N, Fujita T, Tamamoto A. 2006. Modulation of intestinal P-glycoprotein function by polytheylene glycols and their derivatives by in vitro transport and in situ absorption studies. Int J Pharm 313:49-56.
23. Yu L, Bridgers A, Polli J, Vickers A, Long S, Roy A, Winnike R, Coffin M. 1999. Vitamin E-TPGS increases absorption flux of an HIV protease inhibitor by enhancing its solubility and permeability. Pharm Res 16:1812-1817.
24. Benet LZ, Cummins CL,WuCY. 2003. Transporter-enzyme interactions: Implications for predicting drug-drug interactions from in vitro data. Curr Drug Metab 4:393-398.
25. Knight B, Troutman M, Thakker DR. 2006. Deconvoluting the effects of P-glycoprotein on intestinal CYP3A: A major challenge. Curr Opin Pharmacol 6:528-532.
26. Szebeni J, Muggia FM, Alving CR. 1998. Complement activation by cremophor EL as a possible contributor to hypersensitivity to paclitaxel: An in vitro study. J Natl Cancer Inst 90:300-306.
27. Lawrence MJ. 2000. Polyethoxylene sorbitan fatty acid esters. In: Kibbe AH, editor. Handbook of pharmaceutical excipients. 3rd edition. Washington, DC/London, United Kingdom: American Pharmaceutical Association/the Pharmaceutical Press. pp. 416-419.