Development of a polymeric micellar formulation for valspodar and assessment of its pharmacokinetics in rat

European Journal of Pharmaceutics and Biopharmaceutics

Volumn 75, Issue 2, 2010, Pages 90-95

  Binkhathlan, Ziyad ^a   Hamdy, Dalia A ^a   Brocks, Dion R ^a   Lavasanifar, Afsaneh ^a  

^a UNIVERSITY OF ALBERTA   (Canada)

Author keywords

Oral; Pharmacokinetics; Polymeric micelles; Protein binding; PSC 833; Valspodar

Indexed keywords

ALCOHOL; CREMOPHOR; CYCLOSPORIN A; MACROGOL; POLYCAPROLACTONE; VALSPODAR;

ANIMAL EXPERIMENT; ANIMAL TISSUE; AQUEOUS SOLUTION; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DRUG ADMINISTRATION; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG FORMULATION; DRUG HALF LIFE; DRUG SOLUBILITY; ENCAPSULATION; MAXIMUM PLASMA CONCENTRATION; MICELLIZATION; NONHUMAN; POLYMERIZATION; RAT; SPRAGUE DAWLEY RAT;

ADMINISTRATION, ORAL; ANIMALS; AREA UNDER CURVE; CYCLOSPORINS; DRUG CARRIERS; ETHANOL; EXCIPIENTS; GLYCEROL; INJECTIONS, INTRAVENOUS; MALE; MICELLES; POLYESTERS; POLYMERS; PROTEIN BINDING; RATS; RATS, SPRAGUE-DAWLEY; SOLUBILITY; TIME FACTORS; TISSUE DISTRIBUTION;

EID: 77952956172     PISSN: 09396411     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejpb.2010.03.010     Document Type: Article

References (43)

1. Loor F. Valspodar: current status and perspectives. Expert. Opin. Investig. Drugs 1999, 8(6):807-835.
2. Tai H.L. Technology evaluation: valspodar, Novartis AG. Curr. Opin. Mol. Ther. 2000, 2(4):459-467.
3. Boesch D., Muller K., Pourtier-Manzanedo A., Loor F. Restoration of daunomycin retention in multidrug-resistant P388 cells by submicromolar concentrations of SDZ PSC 833, a nonimmunosuppressive cyclosporin derivative. Exp. Cell Res. 1991, 196(1):26-32.
4. Lemaire M., Bruelisauer A., Guntz P., Sato H. Dose-dependent brain penetration of SDZ PSC 833, a novel multidrug resistance-reversing cyclosporin, in rats. Cancer Chemother. Pharmacol. 1996, 38(5):481-486.
5. Kusunoki N., Takara K., Tanigawara Y., Yamauchi A., Ueda K., Komada F., Ku Y., Kuroda Y., Saitoh Y., Okumura K. Inhibitory effects of a cyclosporin derivative, SDZ PSC 833, on transport of doxorubicin and vinblastine via human P-glycoprotein. Jpn. J. Cancer Res. 1998, 89(11):1220-1228.
6. Watanabe T., Tsuge H., Oh-Hara T., Naito M., Tsuruo T. Comparative study on reversal efficacy of SDZ PSC 833, cyclosporin A and verapamil on multidrug resistance in vitro and in vivo. Acta Oncol. 1995, 34(2):235-241.
7. Gottesman M.M., Pastan I. Biochemistry of multidrug resistance mediated by the multidrug transporter. Annu. Rev. Biochem. 1993, 62:385-427.
8. Aicher L., Meier G., Norcross A.J., Jakubowski J., Varela M.C., Cordier A., Steiner S. Decrease in kidney calbindin-D 28kDa as a possible mechanism mediating cyclosporine A- and FK-506-induced calciuria and tubular mineralization. Biochem. Pharmacol. 1997, 53(5):723-731.
9. Pourtier-Manzanedo A., Didier A.D., Muller C.D., Loor F. SDZ PSC 833 and SDZ 280-446 are the most active of various resistance-modifying agents in restoring rhodamine-123 retention within multidrug resistant P388 cells. Anticancer Drugs 1992, 3(4):419-425.
10. Fischer V., Rodriguez-Gascon A., Heitz F., Tynes R., Hauck C., Cohen D., Vickers A.E. The multidrug resistance modulator valspodar (PSC 833) is metabolized by human cytochrome P450 3A. Implications for drug-drug interactions and pharmacological activity of the main metabolite. Drug. Metab. Dispos. 1998, 26(8):802-811.
11. Boesch D., Gaverieaux C., Jachez B., Loor F. In vivo circumvention of P-glycoprotein-mediated multidrug resistance of tumor cells with SDZ PSC 833. Cancer Res. 1991, 51:4226-4233.
12. Cagliero E., Ferracini R., Morello E., Scotlandi K., Manara M.C., Buracco P., Comandone A., Baroetto Parisi R., Baldini N. Reversal of multidrug-resistance using Valspodar (PSC 833) and doxorubicin in osteosarcoma. Oncol. Rep. 2004, 12(5):1023-1031.
13. Boote D.J., Dennis I.F., Twentyman P.R., Osborne R.J., Laburte C., Hensel S., Smyth J.F., Brampton M.H., Bleehen N.M. Phase I study of etoposide with SDZ PSC 833 as a modulator of multidrug resistance in patients with cancer. J. Clin. Oncol. 1996, 14(2):610-618.
14. Chico I., Kang M.H., Bergan R., Abraham J., Bakke S., Meadows B., Rutt A., Robey R., Choyke P., Merino M., Goldspiel B., Smith T., Steinberg S., Figg W.D., Fojo T., Bates S. Phase I study of infusional paclitaxel in combination with the P-glycoprotein antagonist PSC 833. J. Clin. Oncol. 2001, 19(3):832-842.
15. Dorr R., Karanes C., Spier C., Grogan T., Greer J., Moore J., Weinberger B., Schiller G., Pearce T., Litchman M., Dalton W., Roe D., List A.F. Phase I/II study of the P-glycoprotein modulator PSC 833 in patients with acute myeloid leukemia. J. Clin. Oncol. 2001, 19(6):1589-1599.
16. Fracasso P.M., Westervelt P., Fears C.L., Rosen D.M., Zuhowski E.G., Cazenave L.A., Litchman M., Egorin M.J. Phase I study of paclitaxel in combination with a multidrug resistance modulator, PSC 833 (Valspodar), in refractory malignancies. J. Clin. Oncol. 2000, 18(5):1124-1134.
17. Bates S.E., Bakke S., Kang M., Robey R.W., Zhai S., Thambi P., Chen C.C., Patil S., Smith T., Steinberg S.M., Merino M., Goldspiel B., Meadows B., Stein W.D., Choyke P., Balis F., Figg W.D., Fojo T. A phase I/II study of infusional vinblastine with the P-glycoprotein antagonist valspodar (PSC 833) in renal cell carcinoma. Clin. Cancer Res. 2004, 10(14):4724-4733.
18. Giaccone G., Linn S.C., Welink J., Catimel G., Stieltjes H., van der Vijgh W.J., Eeltink C., Vermorken J.B., Pinedo H.M. A dose-finding and pharmacokinetic study of reversal of multidrug resistance with SDZ PSC 833 in combination with doxorubicin in patients with solid tumors. Clin. Cancer Res. 1997, 3(11):2005-2015.
19. Kivisto K.T., Kroemer H.K., Eichelbaum M. The role of human cytochrome P450 enzymes in the metabolism of anticancer agents: implications for drug interactions. Br. J. Clin. Pharmacol. 1995, 40(6):523-530.
20. Aliabadi H.M., Mahmud A., Sharifabadi A.D., Lavasanifar A. Micelles of methoxy poly(ethylene oxide)-b-poly(epsilon-caprolactone) as vehicles for the solubilization and controlled delivery of Cyclosporine A. J. Control. Release 2005, 104(2):301-311.
21. Aliabadi H.M., Elhasi S., Mahmud A., Gulamhusein R., Mahdipoor P., Lavasanifar A. Encapsulation of hydrophobic drugs in polymeric micelles through co-solvent evaporation: the effect of solvent composition on micellar properties and drug loading. Int. J. Pharm. 2007, 329(1-2):158-165.
22. Aliabadi H.M., Brocks D.R., Lavasanifar A. Polymeric micelles for the solubilization and delivery of cyclosporine A: pharmacokinetics and biodistribution. Biomaterials 2005, 26(35):7251-7259.
23. Aliabadi H.M., Brocks D.R., Mahdipoor P., Lavasanifar A. A novel use of an in vitro method to predict the in vivo stability of block copolymer based nano-containers. J. Control. Release 2007, 122(1):63-70.
24. Onetto N., Dougan M., Hellmann S., Gustafson N., Burroughs J., Florezyk A., Canetta R., Rozenweig M. Paclitaxel in Cancer Treatment 1995, 175-186. Marcel Dekker Inc., New York. W.P. McGuire, E.K. Rowinsky (Eds.).
25. Gelderblom H., Verweij J., Nooter K., Sparreboom A. Cremophor EL: the drawbacks and advantages of vehicle selection for drug formulation. Eur. J. Cancer 2001, 37(13):1590-1598.
26. Brat D.J., Windebank A.J., Brimijoin S. Emulsifier for intravenous cyclosporin inhibits neurite outgrowth, causes deficits in rapid axonal transport and leads to structural abnormalities in differentiating N1E.115 neuroblastoma. J. Pharmacol. Exp. Ther. 1992, 261(2):803-810.
27. Forrest M.L., Yanez J.A., Remsberg C.M., Ohgami Y., Kwon G.S., Davies N.M. Paclitaxel prodrugs with sustained release and high solubility in poly(ethylene glycol)-b-poly(epsilon-caprolactone) micelle nanocarriers: pharmacokinetic disposition, tolerability, and cytotoxicity. Pharm. Res. 2008, 25(1):194-206.
28. Forrest M.L., Zhao A., Won C.Y., Malick A.W., Kwon G.S. Lipophilic prodrugs of Hsp90 inhibitor geldanamycin for nanoencapsulation in poly(ethylene glycol)-b-poly(epsilon-caprolactone) micelles. J. Control. Release 2006, 116(2):139-149.
29. Xiong M.P., Yanez J.A., Remsberg C.M., Ohgami Y., Kwon G.S., Davies N.M., Forrest M.L. Formulation of a geldanamycin prodrug in mPEG-b-PCL micelles greatly enhances tolerability and pharmacokinetics in rats. J. Control. Release 2008, 129(1):33-40.
30. Brocks D.R. Stereoselective pharmacokinetics of desbutylhalofantrine, a metabolite of halofantrine, in the rat after administration of the racemic metabolite or parent drug. Biopharm. Drug Dispos. 2000, 21(9):365-371.
31. Watanabe T., Nakayama Y., Naito M., Oh-hara T., Itoh Y., Tsuruo T. Cremophor EL reversed multidrug resistance in vitro but not in tumor-bearing mouse models. Anticancer Drugs 1996, 7(8):825-832.
32. Schuhmacher J., Buhner K., Witt-Laido A. Determination of the free fraction and relative free fraction of drugs strongly bound to plasma proteins. J. Pharm. Sci. 2000, 89(8):1008-1021.
33. Binkhathlan Z., Hamdy D.A., Brocks D.R., Lavasanifar A. Pharmacokinetics of PSC 833 (valspodar) in its Cremophor EL formulation in rat. Xenobiotica 2009.
34. Binkhathlan Z., Somayaji V., Brocks D.R., Lavasanifar A. Development of a liquid chromatography-mass spectrometry (LC/MS) assay method for the quantification of PSC 833 (Valspodar) in rat plasma. J. Chromatogr. B Analyt. Technol. Biomed. Life Sci. 2008, 869(1-2):31-37.
35. Chiou W.L. Critical evaluation of the potential error in pharmacokinetic studies of using the linear trapezoidal rule method for the calculation of the area under the plasma level-time curve. J. Pharmacokinet. Biopharm. 1978, 6(6):539-546.
36. Davies B., Morris T. Physiological parameters in laboratory animals and humans. Pharm. Res. 1993, 10(7):1093-1095.
37. Mathot F., van Beijsterveldt L., Preat V., Brewster M., Arien A. Intestinal uptake and biodistribution of novel polymeric micelles after oral administration. J. Control. Release 2006, 111(1-2):47-55.
38. Ould-Ouali L., Noppe M., Langlois X., Willems B., Te Riele P., Timmerman P., Brewster M.E., Arien A., Preat V. Self-assembling PEG-p(CL-co-TMC) copolymers for oral delivery of poorly water-soluble drugs: a case study with risperidone. J. Control. Release 2005, 102(3):657-668.
39. Mathot F., des Rieux A., Arien A., Schneider Y.J., Brewster M., Preat V. Transport mechanisms of mmePEG750P(CL-co-TMC) polymeric micelles across the intestinal barrier. J. Control. Release 2007, 124(3):134-143.
40. Pierri E., Avgoustakis K. Poly(lactide)-poly(ethylene glycol) micelles as a carrier for griseofulvin. J. Biomed. Mater. Res. A 2005, 75(3):639-647.
41. Allen C., Yu Y., Eisenberg A., Maysinger D. Cellular internalization of PCL(20)-b-PEO(44) block copolymer micelles. Biochim. Biophys. Acta 1999, 1421(1):32-38.
42. Luo L., Tam J., Maysinger D., Eisenberg A. Cellular internalization of poly(ethylene oxide)-b-poly(epsilon-caprolactone) diblock copolymer micelles. Bioconjug. Chem. 2002, 13(6):1259-1265.
43. Nam Y.S., Kang H.S., Park J.Y., Park T.G., Han S.H., Chang I.S. New micelle-like polymer aggregates made from PEI-PLGA diblock copolymers: micellar characteristics and cellular uptake. Biomaterials 2003, 24(12):2053-2059.