Enhanced Oral Absorption of Paclitaxel in a Novel Self-Microemulsifying Drug Delivery System with or without Concomitant Use of P-Glycoprotein Inhibitors

Pharmaceutical Research

Volumn 21, Issue 2, 2004, Pages 261-270

  Yang, Shicheng ^a,d   Gursoy, R Neslihan ^a,e   Lambert, Gregory ^b   Benita, Simon ^a,c  

^a HEBREW UNIVERSITY OF JERUSALEM   (Israel)

^b Novagali Pharma   (France)

^c HEBREW UNIVERSITY OF JERUSALEM   (Israel)

^d PURDUE UNIVERSITY   (United States)

^e HACETTEPE UNIVERSITY   (Turkey)

Author keywords

Microemulsion; P glycoprotein inhibitors; Paclitaxel; Pharmacokinetics; Self microemulsifying drug delivery system (SMEDDS)

Indexed keywords

CYCLOSPORIN A; ETOPOSIDE; GLYCOPROTEIN P INHIBITOR; PACLITAXEL; TACROLIMUS; UNCLASSIFIED DRUG; VEPASID;

ANIMAL EXPERIMENT; AQUEOUS SOLUTION; AREA UNDER THE CURVE; ARTICLE; COMPARATIVE STUDY; CONTROLLED STUDY; DISSOLUTION; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DELIVERY SYSTEM; DRUG DOSE REGIMEN; DRUG EFFICACY; DRUG FORMULATION; DRUG POTENCY; DRUG POTENTIATION; DRUG SCREENING; MALE; MICROEMULSION; NONHUMAN; PHYSICAL CHEMISTRY; PRECIPITATION; PRIORITY JOURNAL; RAT; STATISTICAL SIGNIFICANCE; ZETA POTENTIAL;

ADMINISTRATION, ORAL; ANIMALS; ANTINEOPLASTIC AGENTS; BIOLOGICAL AVAILABILITY; CYCLOSPORINE; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DELIVERY SYSTEMS; DRUG INTERACTIONS; DRUG STABILITY; EMULSIONS; INJECTIONS, INTRAVENOUS; MALE; P-GLYCOPROTEIN; PACLITAXEL; RATS; RATS, SPRAGUE-DAWLEY; TIME FACTORS;

EID: 1242337284     PISSN: 07248741     EISSN: None     Source Type: Journal    
DOI: 10.1023/B:PHAM.0000016238.44452.f1     Document Type: Article

References (35)

1. L. van Zuylen, J. Verweij, and A. Sparreboom. Role of formulation vehicles in taxane pharmacology. Invest. New Drugs 19: 125-141 (2001).
2. R. T. Liggins, W. L. Hunter, and H. M. Burt. Solid-state characterization of paclitaxel. J. Pharm. Sci. 86:1458-1463 (1997).
3. M. T. Huizing, G. Giaccone, L. J. C. Van Warmerdam, H. Rosing, P. J. M. Bakker, J. B. Vermorken, P. E. Postmus, N. van Zandwijk, M. G. J. Van Koolen, W. W. ten Bokkel Huinink, W. J. van der Vijgh, F. J. Bierhorst, A. Lai, O. Dalesio, H. M. Pinedo, C. H. Veenhof, and J. H. Beijnen. Pharmacokinetics of paclitaxel and carboplatin in a dose escalating and dose sequencing study in patients with non small cell lung cancer. J. Clin. Oncol. 15:317-329 (1997).
4. H. Gelderblom, J. Verweij, K. Nooter, and A. Sparreboom. Cremophor EL: the drawbacks and advantages of vehicle selection for drug formulation. Eur. J. Cancer 37:1590-1598 (2001).
5. O. van Tellingen, M. T. Huizing, V. R. Panday, J. H. Schellens, W. J. Nooijen, and J. H. Beijnen. Cremophor EL causes (pseudo-) non-linear pharmacokinetics of paclitaxel in patients. Br. J. Cancer 81:330-335 (1999).
6. J. M. M. Terwogt, B. Nuijen, W. W. T. B. Huinink, and J. H. Beijnen. Alternative formulations of paclitaxel. Cancer Treat. Rev. 23:87-95 (1997).
7. M. M. Malingre, J. H. Beijnen, and J. H. M. Schellens. Oral delivery of taxanes. Invest New Drugs 19:155-162 (2001).
8. J. M. Meerum Terwogt, M. M. Malingre, J. H. Beijnen, W. W. ten Bokkel Huinink, H. Rosing, F. J. Koopman, O. van Tellingen, M. Swart, and J. H. Schellens. Coadministration of oral cyclosporin A enables oral therapy with paclitaxel. Clin. Cancer Res. 5:3379-3384 (1999).
9. J. van Asperen, O. van Tellingen, A. Sparreboom, A. H. Schinkel, P. Borst, W. J. Nooijen, and J. H. Beijnen. Enhanced oral bioavailability of paclitaxel in mice treated with the P-glycoprotein blocker SDZ PSC 833. Br. J. Cancer 76:1181-1183 (1997).
10. C. D. Britten, S. D. Baker, L. J. Denis, T. Johnson, R. Drengler, L. L. Siu, K. Duchin, J. Kuhn, and E. K. Rowinsky. Oral paclitaxel and concurrent cyclosporin A: targeting clinically relevant systemic exposure to paclitaxel. Clin. Cancer Res. 6:3459-3468 (2000).
11. Y. Zhang and L. Z. Benet. The gut as a barrier to drug absorption: combined role of cytochrome P450 3A and P-glycoprotein. Clin. Pharmacokinet. 40:159-168 (2001).
12. J. S. Woo, C. H. Lee, C. K. Shim, and S-J. Hwang. Enhanced oral bioavailability of paclitaxel by coadministration of the P-glycoprotein inhibitor KR30031. Pharm. Res. 20:24-30 (2003).
13. J. van Asperen, O. van Tellingen, M. A. van der Valk, M. Rozenhart, and J. H. Beijnen. Enhanced oral absorption and decreased elimination of paclitaxel in mice cotreated with cyclosporin A. Clin. Cancer Res. 4:2293-2297 (1998).
14. C. M. F. Kruijtzer, J. H. M. Schellens, J. Mezger, M. E. Scheulen, U. Keilholz, J. H. Beijnen, H. Rosing, R. A. A. Mathot, S. Marcus, H. van Tinteren, and P. Baas. Phase II and pharmacologic study of weekly oral paclitaxel plus cyclosporine in patients with advanced non-small-cell lung cancer. J. Clin. Oncol. 20:4508-4516 (2002).
15. M. M. Malingre, J. H. Beijnen, H. Rosing, F. J. Koopman, O. Van Tellingen, K. Duchin, W. W. t. B. Huinink, M. Swart, J. Lieverst, and J. H. M. Schellens. The effect of different doses of cyclosporin A on the systemic exposure of orally administered paclitaxel. Anticancer Drugs 12:351-358 (2001).
16. T. Gershanik and S. Benita. Self-dispersing lipid formulations for improving oral absorption of lipophilic drugs. Eur. J. Pharm. Biopharm. 50:179-188 (2000).
17. C. W. Pouton. Formulation of self-emulsifying drug delivery systems. Adv. Drug Deliv. Rev. 25:47-58 (1997).
18. S-M. Khoo, A. J. Humberstone, C. J. H. Porter, G. A. Edwards, and W. N. Charman. Formulation design and bioavailability assessment of lipidic self-emulsifying formulations of halofantrine. Int. J. Pharm. 167:155-164 (1998).
19. S. Tamilvanan, R. Neslihan Gursoy, and S. Benita. Emulsion-based delivery systems for enhanced drug absorption. Pharmatech 131:156-161 (2002).
20. J. M. Dintaman and J. A. Silverman. Inhibition of P-glycoprotein by D-alpha-tocopheryl polyethylene glycol 1000 succinate (TPGS). Pharm. Res. 16:1550-1556 (1999).
21. D. S. Chervinsky, M. L. Brecher, and M. J. Hoelcle. CremophorEL enhances taxol efficacy in a multi-drug resistant C1300 neuroblastoma cell line. Anticancer Res. 13:93-96 (1993).
22. D. L. Zhao and B. H. Hirst. Comparison of bile salt perturbation of duodenal and jejunal isolated brush-border membranes. Digestion 47:200-207 (1990).
23. Y. L. Lo and J. D. Huang. Effects of sodium deoxycholate and sodium caprate on the transport of epirubicin in human intestinal epithelial Caco-2 cell layers and everted gut sacs of the rats. Biochem. Pharmacol. 59:665-672 (2000).
24. A. Sharma, W. D. Conway, and R. M. Straubinger. Reversed-phase high-performance liquid chromatographic determination of taxol in mouse plasma. J. Chromatogr. B Biomed. Appl. 655: 315-319 (1994).
25. P. P. Constantinides, K. J. Lambert, A. K. Tustian, B. Schneider, S. Lalji, W. Ma, B. Wentzel, D. Kessler, D. Worah, and S. C. Quay. Formulation development and antitumor activity of a filter-sterilizable emulsion of paclitaxel. Pharm. Res. 17:175-182 (2000).
26. K. Matsuoka, Y. Kuranaga, and Y. Moroi. Solubilization of cholesterol and polycyclic aromatic compounds into sodium bile salt micelles (part 2). Biochim. Biophys. Acta 1580:200-214 (2002).
27. K. Kawakami, T. Yoshikawa, Y. Moroto, E. Kanaoka, K. Takahashi, Y. Nishihara, and K. Masuda. Microemulsion formulation for enhanced absorption of poorly soluble drugs. I. Prescription design. J. Contr. Rel. 81:65-74 (2002).
28. A. Sparreboom, L. van Zuylen, E. Brouwer, W. J. Loos, P. de Bruijn, H. Gelderblom, M. Pillay, K. Nooter, G. Stoter, and J. Verweij. Cremophor EL-mediated alteration of paclitaxel distribution in human blood: clinical pharmacokinetic implications. Cancer Res. 59:1454-1457 (1999).
29. H. A. Bardelmeijer, M. Ouwehand, M. M. Malingre, J. H. M. Schellens, J. H. Beijnen, and O. van Tellingen. Entrapment by Cremophor EL decreases the absorption of paclitaxel from the gut. Cancer Chemother. Pharmacol. 49:119-125 (2002).
30. T. Noguchi, Y. Tokunaga, H. Ichikawa, S. Muranishi, and H. Sezaki. Mechanism of the intestinal absorption of drugs from oil-in-water emulsions. Part VIII. Regional capacities of gastrointestinal absorption and lymphatic transport for lipid-soluble dyes in rats. Chem. Pharm. Bull 25:413-419 (1977).
31. C. J. H. Porter, S. A. Charman, A. J. Humberstone, and W. N. Charman. Lymphatic transport of halofantrine in the triple-cannulated anesthetized rat model: effect of lipid vehicle dispersion. J. Pharm. Sci. 85:351-356 (1996).
32. T. Tamura, T. Fujita, Y. Itoh, S. Sugimoto, H. Yamada, M. Murakami, A. Yamamoto, and S. Muranishi. Synergistic anti-tumor effects of mitomycin C and bile salts against L1210 cells. Biol. Pharm. Bull. 18:1109-1113 (1995).
33. M. M. Malingre, J. M. Terwogt, J. H. Beijnen, H. Rosing, F. J. Koopman, O. van Tellingen, K. Duchin, W. W. Huinink, M. Swart, J. Lieverst, and J. H. Schellens. Phase I and pharmacokinetic study of oral paclitaxel. J. Clin. Oncol. 18:2468-2475 (2000).
34. M. M. Malingre, W. W. Ten Bokkel Huinink, K. Duchin, J. H. M. Schellens, and J. H. Beijnen. Pharmacokinetics of oral cyclosporin A when co-administered to enhance the oral absorption of paclitaxel. Anticancer Drugs 12:591-593 (2001).
35. W. M. Kan, Y. T. Liu, C. L. Hsiao, C. Y. Shieh, J. H. Kuo, J. D. Huang, and S. F. Su. Effect of hydroxyzine on the transport of etoposide in rat small intestine. Anticancer Drugs 12:267-273 (2001).