Study of drug concentration effects on in vitro lipolysis kinetics in medium-chain triglycerides by considering oil viscosity and surface tension

European Journal of Pharmaceutical Sciences

Volumn 44, Issue 3, 2011, Pages 351-358

  Arnold, Yvonne Elisabeth ^a,b   Imanidis, Georgios ^a,b   Kuentz, Martin ^b  

^a UNIVERSITY OF BASEL   (Switzerland)

^b UNIVERSITY OF APPLIED SCIENCES AND ARTS NORTHWESTERN SWITZERLAND   (Switzerland)

Author keywords

Drug load; In vitro lipolysis; Oil viscosity; Surface tension

Indexed keywords

DANAZOL; FELODIPINE; FENOFIBRATE; GRISEOFULVIN; HEXANOIC ACID; LAURIC ACID; MEDIUM CHAIN TRIACYLGLYCEROL; MYRISTIC ACID; PROBUCOL; TETRAHYDROLIPSTATIN;

ARTICLE; AUTOMATION; COMPETITIVE INHIBITION; CONCENTRATION RESPONSE; DIGESTION; DRUG FORMULATION; DRUG RELEASE; DRUG SOLUBILITY; IN VITRO STUDY; LIPOLYSIS; MOLECULAR MODEL; PH; PRIORITY JOURNAL; SURFACE TENSION; VISCOMETRY; VISCOSITY;

ANIMALS; DOSE-RESPONSE RELATIONSHIP, DRUG; FATTY ACIDS; KINETICS; LIPOLYSIS; MODELS, BIOLOGICAL; MODELS, MOLECULAR; PANCREATIN; PHARMACEUTICAL PREPARATIONS; SOLUBILITY; SURFACE TENSION; SWINE; TRIGLYCERIDES; VISCOSITY;

EID: 80053929855     PISSN: 09280987     EISSN: 18790720     Source Type: Journal    
DOI: 10.1016/j.ejps.2011.08.009     Document Type: Article

References (40)

1. A. Aloulou, J.A. Rodriguez, S. Fernandez, D. van Oosterhout, D. Puccinelli, and F. Carrire Exploring the specific features of interfacial enzymology based on lipase studies Biochim. Biophys. Acta 1761 2006 995 1013 (Pubitemid 44354291)
2. Y. Cao, M. Marra, and B.D. Andersen Predictive relationships for the effects of triglyceride ester concentration and water uptake on solubility and partitioning of small molecules into lipid vehicles J. Pharm. Sci. 93 11 2004 2768 2779 (Pubitemid 39506627)
3. W.N. Charman, C.J. Porter, S. Mithani, and J.B. Dressman Physiochemical and physiological mechanisms for the effects of food on drug absorption: the role of lipids and pH J. Pharm. Sci. 86 3 1997 269 282 (Pubitemid 27113759)
4. J.O. Christensen, K. Schultz, B. Mollgaard, H.G. Kristensen, and A. Müllertz Solubilization of poorly water-soluble medium- and long-chain triacylglycerols Eur. J. Pharm. Sci. 23 2004 287 296 (Pubitemid 39369884)
5. J.F. Cuiné, C.L. McEvoy, W.N. Charman, C.W. Pouton, G.A. Edwards, H. Benameur, and C.J.H. Porter Evaluation of the impact of surfactant digestion on the bioavailability of danazol after oral administration of lipidic self-emulsifying formulations to dogs J. Pharm. Sci. 97 2 2008 993 1010
6. J.K. Embleton, and C.W. Pouton Structure and function of gastro-intestinal lipases Adv. Drug Delivery Rev. 25 1997 15 32 (Pubitemid 27107788)
7. D. Fatouros, and A. Müllertz In vitro lipid digestion models in design of drug delivery systems for enhancing oral bioavailability Expert Opin. Drug Metab. Toxicol. 4 1 2008 65 76 (Pubitemid 351234101)
8. D.G. Fatouros, G.R. Deen, L. Arleth, B. Bergenstahl, F.S. Nielsen, S.N. Flemming, J.K. Pedersen, and A. Müllertz Structural development of self nano emulsifying drug delivery systems (SNEDDS) during in vitro digestion monitored by small-angle X-ray scattering Pharm. Res. 24 10 2007 1844 1853 (Pubitemid 47389238)
9. S. Fernandez, V. Jannin, J.D. Rodier, N. Ritter, B. Mahler, and F. Carrire Comparative study of digestive lipase activities on the self emulsifying excipient Labrasol®, medium-chain glycerides and PEG esters Biochim. Biophys. Acta 1771 2007 633 640 (Pubitemid 46670793)
10. S. Fernandez, J.D. Rodier, N. Ritter, B. Mahler, F. Demarne, F. Carrire, and V. Jannin Lipolysis of the semi-solid self-emulsifying excipient Gelucire® 44/14 by digestive lipases Biochim. Biophys. Acta 1781 2008 367 375
11. E. Galia, E. Nicolaides, D. Hörter, R. Löbenberg, C. Reppas, and J.B. Dressman Evaluation of various dissolution media for predicting in vivo performance of Class I and II drugs Pharm. Res. 15 5 1998 698 705 (Pubitemid 28275645)
12. C. Goddeeris, J. Coacci, and G. Van de Mooter Correlation between digestion of the lipid phase of smedds and the release of the anti-HIV drug UC 781 and the anti-mycotic drug enilconazol from smedds Eur. J. Pharm. Biopharm. 66 2007 173 181 (Pubitemid 46654766)
13. P. Hadvry, H. Lengsfeld, and H. Wolfer Inhibition of pancreatic lipase in vitro by the covalent inhibitor tetrahydrolipstatin Biochem. J. 256 2 1988 357 361 (Pubitemid 19005994)
14. D.G. Hall The dependence of lipid monolayer lipolysis on surface pressure Biochem. J. 278 1992 73 78
15. S.F. Han, T.T. Yao, X.X. Zhang, L. Gan, C. Zhu, H.Z. Yu, and Y. Gan Lipid-based formulations to enhance oral bioavailability of the poorly water-soluble drug anethol trithione: effects of lipid composition and formulation Int. J. Pharm. 379 2009 18 24
16. J.B. Hauptmann, F.S. Jeunet, and D. Hartmann Initial studies in humans with the novel gastrointestinal lipase inhibitor Ro 18-0647 (tetrahydrolipstatin) Am. J. Clin. Nutr. 55 1 1992 309S 313S
17. J. Hong, J. Kim, Y. Song, J. Park, and C. Kim A new self-emulsifying formulation of itraconazole with improved dissolution and oral absorption J. Controlled Release 100 2006 332 338 (Pubitemid 41827486)
18. A.J. Humberstone, and W.N. Charman Lipid-based vehicles for the oral delivery of poorly water soluble drugs Adv. Drug Delivery Rev. 25 1997 103 128
19. K. Hutchison Digestible emulsions and microemulsions for optimal oral delivery of hydrophobic drugs Bull. Tech. Gattefossé 87 1994 67 74
20. D. Ilardia-Arana, H.G. Kristensen, and A. Müllertz Biorelevant dissolution media: aggregation of amphiphiles and solubility of estradiol J. Pharm. Sci. 95 2 2006 248 255 (Pubitemid 43241968)
21. Jahnke, S., 1998. The theory of high-pressure homogenization. In: Müller, R.H., Benita, S., Böhm, B. (Eds.), Emulsions and Nanosuspensions for the Formulation of Poorly Soluble Drugs, pp. 177-200.
22. E. Jantratid, N. Janssen, C. Reppas, and J.B. Dressman Dissolution media simulating conditions in the proximal human gastrointestinal tract: an update Pharm. Res. 25 7 2008 1663 1676
23. A.M. Kaukonen, B.J. Boyd, C.J.H. Porter, and W.N. Charman Drug solubilization behavior during in vitro digestion of simple triglyceride lipid solution formulations Drug Pharm. Res. 21 2 2004 245 260
24. J.G.T. Kierkels, L.F.W. Vleugels, J.H. Kern, E.M. Meijer, and M. Kloosterman Lipase kinetics: on-line measurement of the interfacial area of emulsions Enzyme Microb. Technol. 12 1990 760 763 (Pubitemid 20303114)
25. M. Kuentz Oral self-emulsifying drug delivery systems, from biopharmaceutical to technical formulation aspects J. Drug Delivery Sci. Technol. 21 1 2011 17 26
26. S. Laurent, M.G. Ivanova, D. Pioch, J. Graille, and R. Verger Interactions between β-cyclodextrin and insoluble glyceride molecular films at the argon/water interface: application to lipase kinetics Chem. Phys. Lipids 70 1994 35 42 (Pubitemid 24129173)
27. C.M. O'Driscoll, and B.T. Griffin Biopharmaceutical challenges associated with drugs of low aqueous solubility - the potential impact of lipid-based formulations Adv. Drug Delivery Rev. 60 2008 617 624
28. I. Panaiotov, M. Ivanova, and R. Verger Interfacial and temporal organization of enzymatic lipolysis Curr. Opin. Colloid Interface Sci. 2 5 1997 517 525
29. C.J.H. Porter, and W.N. Charman In vitro assessment of oral lipid based formulations Adv. Drug Delivery Rev. 50 2001 S127 S147 (Pubitemid 32905359)
30. C.J.H. Porter, N.L. Trevaskis, and W.N. Charman Lipids and lipid-based formulations: optimizing the oral delivery of lipophilic drugs Nat. Rev. Drug Discovery 6 2007 231 248 (Pubitemid 46344627)
31. C.J.H. Porter, C.W. Pouton, J.F. Cuine, and W.N. Charman Enhancing intestinal drug solubilisation using lipid-based delivery systems Adv. Drug Delivery Rev. 60 2008 673 691
32. C.W. Pouton Lipid formulations for oral administration of drugs: non-emulsifying, self-emulsifying, and self-microemulsifying drug delivery systems Eur. J. Pharm. Sci. 11 2 2000 S93 S98
33. C.W. Pouton Formulation of poorly water-soluble drugs for oral administration: physicochemical and physiological issues and the lipid formulation classification system Eur. J. Pharm. Sci. 29 2006 278 287 (Pubitemid 44740131)
34. H.J. Schwebel, P. van Hoogevest, M.L.S. Leight, and M. Kuentz The apparent solubilizing capacity of simulated intestinal fluids for poorly water-soluble drugs Pharm. Dev. Technol. 16 3 2010 278 286
35. L. Sek, C.J.H. Porter, A.M. Kaukonen, and W.N. Charman Evaluation of in-vitro digestion profiles of long and medium-chain glycerides and the phase behaviour of their lipolytic products J. Pharm. Pharmacol. 54 2002 29 41 (Pubitemid 34116220)
36. A. Tiss, H. Lengsfeld, F. Carrire, and R. Verger Inhibition of human pancreatic lipase by tetrahydrolipstatin: further kinetic studies showing its reversibility J. Mol. Catal. B: Enzym. 58 2009 41 47
37. D.W. Van Krevelen Properties of Polymers: Their Correlation with Chemical Structure; Their Numerical Estimation and Prediction from Additive Group Contributions 1997 Elsevier Amsterdam, Netherlands p. 898
38. R. Verger, and G.H. Haas Interfacial enzyme kinetics of lipolysis Ann. Rev. Biophys. Bioeng. 5 1976 77 117
39. N.H. Zangenberg, A. Müllertz, H.G. Kristensen, and L. Hovgard A dynamic in vitro lipolysis model. I. Controlling the rate of lipolysis by continuous addition of calcium Eur. J. Pharm. Sci. 14 2001 115 122 (Pubitemid 32737533)
40. N.H. Zangenberg, A. Müllertz, H.G. Kristensen, and L. Hovgard A dynamic in vitro lipolysis model. II. Evaluation of the model Eur. J. Pharm. Sci. 14 2001 237 244 (Pubitemid 32884320)