Docetaxel microemulsion for enhanced oral bioavailability: Preparation and in vitro and in vivo evaluation

Journal of Controlled Release

Volumn 140, Issue 2, 2009, Pages 86-94

  Yin, Yong Mei ^a,b,c   Cui, Fu De ^a   Mu, Chao Feng ^a,b   Choi, Min Koo ^d   Kim, Jung Sun ^e   Chung, Suk Jae ^b   Shim, Chang Koo ^b   Kim, Dae Duk ^b  

^a SHENYANG PHARMACEUTICAL UNIVERSITY   (China)

^b Seoul National University   (South Korea)

^c NANKAI UNIVERSITY   (China)

^d Inje University   (South Korea)

^e Dongseo University   (South Korea)

Author keywords

Bioavailability; Docetaxel; Microemulsions; Solubility

Indexed keywords

BIOAVAILABILITY; CACO-2 CELLS; CO-SURFACTANTS; COMBINED EFFECT; COMMERCIAL PRODUCTS; DOCETAXEL; FURTHER DEVELOPMENT; HYDROPHOBIC DRUG; IN-VITRO; MEAN DIAMETER; MICROEMULSION SYSTEMS; ORAL DRUG DELIVERY SYSTEM; PSEUDOTERNARY PHASE DIAGRAMS; SOLUBILITY STUDIES; SOLUBILIZATION CAPACITIES; TAXOTERE;

BIOCHEMISTRY; CONTROLLED DRUG DELIVERY; DIALYSIS; MONOLAYERS; PHASE DIAGRAMS; SOLUBILITY; SURFACE ACTIVE AGENTS; TERNARY SYSTEMS; ULTRAFILTRATION;

MICROEMULSIONS;

CAPRYOL; CREMOPHOR; DIETHYLENE GLYCOL MONOETHYL ETHER; DOCETAXEL; EMULSIFYING AGENT; GLYCOPROTEIN P; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; BASOLATERAL MEMBRANE; CONTROLLED STUDY; DIALYSIS; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DELIVERY SYSTEM; DRUG DOSAGE FORM COMPARISON; DRUG FORMULATION; DRUG PENETRATION; DRUG RELEASE; DRUG SOLUBILITY; DRUG SYNTHESIS; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; MALE; MAXIMUM PLASMA CONCENTRATION; MICROEMULSION; NONHUMAN; PARTICLE SIZE; PRIORITY JOURNAL; RAT; TIME TO MAXIMUM PLASMA CONCENTRATION; ULTRAFILTRATION;

ADMINISTRATION, ORAL; ANIMALS; ANTINEOPLASTIC AGENTS, PHYTOGENIC; BIOLOGICAL AVAILABILITY; CACO-2 CELLS; CHEMISTRY, PHARMACEUTICAL; DRUG CARRIERS; DRUG COMPOUNDING; EMULSIONS; ETHYLENE GLYCOLS; GLYCEROL; HUMANS; INTESTINAL ABSORPTION; INTESTINAL MUCOSA; MALE; OILS; PARTICLE SIZE; PERMEABILITY; RATS; RATS, SPRAGUE-DAWLEY; SOLUBILITY; SURFACE-ACTIVE AGENTS; TAXOIDS;

EID: 70350618790     PISSN: 01683659     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.jconrel.2009.08.015     Document Type: Article

References (33)

1. Lavelle F., Bissery M.C., Combeau C., Riou J.F., Vrignaud P., and André S. Preclinical evaluation of docetaxel (Taxotere). Semin. Oncol. 22 (1995) 3-16
2. MacConnachie A.M. Docetaxel (taxotere, Rhone-Poulenc Rorer). Intensive Crit. Care Nurs. 13 (1997) 119-120
3. Kuppens I.E., Bosch T.M., van Maanen M.J., Rosing H., Fitzpatrick A., Beijnen J.H., and Schellens J.H. Oral bioavailability of docetaxel in combination with OC144-093 (ONT-093). Cancer Chemother. Pharmacol. 55 (2005) 72-78
4. Gao K., Sun J., Liu K., Liu X., and He Z. Preparation and characterization of a submicron lipid emulsion of docetaxel: submicron lipid emulsion of docetaxel. Drug Dev. Ind. Pharm. 34 (2008) 1227-1237
5. Wils P., Phung-Ba V., Warnery A., Lechardeur D., Raeissi S., Hidalgo I.J., and Scherman D. Polarized transport of docetaxel and vinblastine mediated by P-glycoprotein in human intestinal epithelial cell monolayers. Biochem. Pharmacol. 48 (1994) 1528-1530
6. van Herwaarden A.E., Wagenaar E., van der Kruijssen C.M., van Waterschoot R.A., Smit J.W., Song J.Y., van der Valk M.A., van Tellingen O., van der Hoorn J.W., Rosing H., Beijnen J.H., and Schinkel A.H. Knockout of cytochrome P450 3A yields new mouse models for understanding xenobiotic metabolism. J. Clin. Invest. 117 (2007) 3583-3592
7. Pfeiffer P., Mortensen J.P., Bjerregaard B., Eckhoff L., Schønnemann K., Sandbergd E., Aabo K., and Jakobsen A. Patient preference for oral or intravenous chemotherapy: a randomised cross-over trial comparing capecitabine and Nordic fluorouracil/leucovorin in patients with colorectal cancer. Eur. J. Cancer 42 (2006) 2738-2743
8. Malingré M.M., Richel D.J., Beijnen J.H., Rosing H., Koopman F.J., Ten Bokkel Huinink W.W., Schot M.E., and Schellens J.H. Coadministration of cyclosporine strongly enhances the oral bioavailability of docetaxel. J. Clin. Oncol. 19 (2001) 1160-1166
9. Ben Reguiga M., Bonhomme-Faivre L., and Farinotti R. Bioavailability and tissular distribution of docetaxel, a P-glycoprotein substrate, are modified by interferon-alpha in rats. J. Pharm. Pharmacol. 59 (2007) 401-408
10. Kawakami K., Yoshikawa T., Moroto Y., Kanaoka E., Takahashi K., Nishihara Y., and Masuda K. Microemulsion formulation for enhanced absorption of poorly soluble drugs prescription design. J. Control. Release 81 (2002) 65-74
11. Kawakami K., Yoshikawa T., Hayashi T., Nishihara Y., and Masuda K. Microemulsion formulation for enhanced absorption of poorly soluble drugs II. In vivo study. J. Control. Release 81 (2002) 75-82
12. Araya H., Tomita M., and Hayashi M. The novel formulation design of O/W microemulsion for improving the gastrointestinal absorption of poorly water soluble compounds. Int. J. Pharm. 305 (2005) 61-74
13. Shah N.H., Carvajal M.T., Patel C.I., Infeld M.H., and Malick A.W. Self-emulsifying drug delivery systems (SEDDS) with polyglycolyzed glycerides for improving in vitro dissolution and oral absorption of lipophilic drugs. Int. J. Pharm. 106 (1994) 15-23
14. Constantinides P.P. Lipid microemulsions for improving drug dissolution and oral absorption: physical and biopharmaceutical aspects. Pharm. Res. 12 (1995) 1561-1572
15. Rege B.D., Kao J.P., and Polli J.E. Effects of nonionic surfactants on membrane transporters in Caco-2 cell monolayers. Eur. J. Pharm. Sci. 16 (2002) 237-246
16. Takahashi Y., Kondo H., Yasuda T., Watanabe T., Kobayashi S., and Yokohama S. Common solubilizers to estimate the Caco-2 transport of poorly water-soluble drugs. Int. J. Pharm. 246 (2002) 85-94
17. Lin Y.L., Shen Q., Katsumi H., Okada N., Fujita T., Jiang X.H., and Yamamoto A. Effects of Labrasol and other pharmaceutical excipients on the intestinal transport and absorption of rhodamine123, a P-glycoprotein substrate, in rats. Biol. Pharm. Bull. 30 (2007) 1301-1307
18. Porter C.J., Kaukonen A.M., Boyd B.J., Edwards G.A., and Charman W.N. Susceptibility to lipase-mediated digestion reduces the oral bioavailability of danazol after administration as a medium-chain lipid-based microemulsion formulation. Pharm. Res. 21 (2004) 1405-1412
19. Nassar T., Rom A., Nyska A., and Benita S. A novel nanocapsule delivery system to overcome intestinal degradation and drug transport limited absorption of P-glycoprotein substrate drugs. Pharm. Res. 25 (2008) 2019-2029
20. Ciccolini J., Catalin J., Blachon M.F., and Durand A. Rapid high-performance liquid chromatographic determination of docetaxel (Taxotere) in plasma using liquid-liquid extraction. J. Chromatogr. B Biomed. Sci. Appl. 759 (2001) 299-306
21. New Pharmacopoeia Monographs for Gattefossé Speciality Excipients. 2007. Available from URL:http://www.in-pharmatechnologist.com/smartlead/view/199590/4/New-Pharmacopoeia-Monographs-for-Gattefosse-Speciality-Excipients.
22. Mandawgade S.D., Sharma S., Pathak S., and Patravale V.B. Development of SMEDDS using natural lipophile: application to β-Artemether delivery. Int. J. Pharm. 362 (2008) 179-183
23. Raymond C.R., Paul J.S., and Paul J.W. Handbook of Pharmaceutical Excipients. Fourth edition (2003), Pharmaceutical Press and American Pharmaceutical Association, Washington, USA
24. Zhang Q.Z., Jiang X.G., Jiang W.M., Lu W., Su L.N., and Shi Z.Q. Preparation of nimodipine-loaded microemulsion for intranasal delivery and evaluation on the targeting efficiency to the brain. Int. J. Pharm. 275 (2004) 85-96
25. Dahan A., and Hoffman A. Rationalizing the selection of oral lipid based drug delivery systems by an in vitro dynamic lipolysis model for improved oral bioavailability of poorly water soluble drugs. J. Control. Release 129 (2008) 1-10
26. Atef E., and Belmonte A.A. Formulation and in vitro and in vivo characterization of a phenytoin self-emulsifying drug delivery system (SEDDS). Eur. J. Pharm. Sci. 35 (2008) 257-263
27. Twentyman P.R., and Luscombe M. A study of some variables in a tetrazolium dye (MTT) based assay for cell growth and chemosensitivity. Br. J. Cancer 56 (1987) 279-285
28. Ben Reguiga M., Bonhomme-Faivre L., and Farinotti R. Bioavailability and tissular distribution of docetaxel, a P-glycoprotein substrate, are modified by interferon-alpha in rats. J. Pharm. Pharmacol. 59 (2007) 401-408
29. Nerurkar M.M., Burton P.S., and Borchardt R.T. The use of surfactants to enhance the permeability of peptides through Caco-2 cells by inhibition of an apically polarized efflux system. Pharm. Res. 13 (1996) 528-534
30. Shono Y., Nishihara H., Matsuda Y., Furukawa S., Okada N., Fujita T., and Yamamoto A. Modulation of intestinal P-glycoprotein function by Cremophor EL and other surfactants by an in vitro diffusion chamber method using the isolated rat intestinal membranes. J. Pharm. Sci. 93 (2004) 877-885
31. Buggins T.R., Dickinson P.A., and Taylor G. The effects of pharmaceutical excipients on drug disposition. Adv. Drug Deliv. Rev. 59 (2007) 1482-1503
32. Yamagata T., Kusuhara H., Morishita M., Takayama K., Benameur H., and Sugiyama Y. Effect of excipients on breast cancer resistance protein substrate uptake activity. J. Control. Release 124 (2007) 1-5
33. Ren X., Mao X., Si L., Cao L., Xiong H., Qiu J., Schimmer A.D., and Li G. Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur. J. Pharm. Biopharm. 70 (2008) 279-288