The effect of composition and gastric conditions on the self-emulsification process of ibuprofen-loaded self-emulsifying drug delivery systems: A microscopic and dynamic gastric model study

Pharmaceutical Research

Volumn 28, Issue 7, 2011, Pages 1540-1551

  Mercuri, Annalisa ^a   Passalacqua, Antonio ^b   Wickham, Martin S J ^b   Faulks, Richard M ^b   Craig, Duncan Q M ^a   Barker, Susan A ^a  

^a UNIVERSITY OF EAST ANGLIA   (United Kingdom)

^b INSTITUTE OF FOOD RESEARCH   (United Kingdom)

Author keywords

droplet size; dynamic gastric model; mechanism of self emulsification; phase diagram; self emulsifying systems

Indexed keywords

IBUPROFEN; POLYSORBATE 80; SORBITAN OLEATE; SOYBEAN OIL;

ARTICLE; CONTROLLED STUDY; DIGESTION; DRUG DELIVERY SYSTEM; DRUG SOLUBILITY; DYNAMICS; EMULSION; HUMAN; HUMAN EXPERIMENT; INTERMETHOD COMPARISON; MATHEMATICAL MODEL; MICROSCOPY; NORMAL HUMAN; PARTICLE SIZE; PHYSICAL CHEMISTRY; PRIORITY JOURNAL; SELF EMULSIFYING DRUG DELIVERY SYSTEM; STOMACH; VALIDATION PROCESS;

ANIMALS; DRUG DELIVERY SYSTEMS; EMULSIFYING AGENTS; GASTRIC ACID; GASTRIC MUCOSA; IBUPROFEN; MODELS, BIOLOGICAL; PARTICLE SIZE; POLYSORBATES; SOLUBILITY; SWINE;

EID: 79959904472     PISSN: 07248741     EISSN: 1573904X     Source Type: Journal    
DOI: 10.1007/s11095-011-0387-8     Document Type: Article

References (42)

1. CW Pouton 1997 Formulation of self-emulsifying drug delivery systems Adv Drug Deliv Rev 25 47 58 10.1016/S0169-409X(96)00490-5 1:CAS:528: DyaK2sXhtlOqsrc%3D (Pubitemid 27107790)
2. A Mullertz A Ogbonna S Ren T Rades 2010 New perspectives on lipid and surfactant based drug delivery systems for oral delivery of poorly soluble drugs J Pharm Pharmacol 62 1622 1636 21039546 10.1111/j.2042-7158.2010.01107.x 1:CAS:528:DC%2BC3cXhtlGlsbbN
3. CW Pouton 2006 Formulation of poorly water-soluble drugs for oral administration: physicochemical and physiological issues and the lipid formulation classification system Eur J Pharm Sci 29 278 287 16815001 10.1016/j.ejps.2006.04.016 1:CAS:528:DC%2BD28XhtFentrrM (Pubitemid 44740131)
4. KJ MacGregor JK Embleton JE Lacy EA Perry LJ Solomon H Seager CW Pouton 1997 Influence of lipolysis on drug absorption from the gastro-intestinal tract Adv Drug Deliv Rev 25 33 46 10.1016/S0169-409X(96)00489-9 1:CAS:528: DyaK2sXhtlOqsrY%3D (Pubitemid 27107789)
5. Y Ito T Kusawake YVR Prasad N Sugioka N Shibata K Takada 2006 Preparation and evaluation of oral solid heparin using emulsifier and adsorbent for in vitro and in vivo studies Int J Pharm 317 114 119 16631328 10.1016/j.ijpharm. 2006.02.056 1:CAS:528:DC%2BD28Xmt1ajtr0%3D
6. M Serratoni M Newton S Booth A Clarke 2007 Controlled drug release from pellets containing water-insoluble drugs dissolved in a self-emulsifying system Eur J Pharm Biopharm 65 94 98 17056237 10.1016/j.ejpb.2006.07.011 1:CAS:528:DC%2BD28Xht1KlsLzP (Pubitemid 44834468)
7. SA Charman WN Charman MC Rogge TD Wilson FJ Dutko CW Pouton 1992 Self-emulsifying drug delivery systems: formulation and biopharmaceutic evaluation of an investigational lipophilic compound Pharm Res 9 87 93 1589415 10.1023/A:1018987928936 1:CAS:528:DyaK38XptFaluw%3D%3D
8. DQM Craig HSR Lievens KG Pitt DE Storey 1993 An investigation into the physico-chemical properties of self-emulsifying systems using low frequency dielectric spectroscopy, surface tension measurements and particle size analysis Int J Pharm 96 147 155 10.1016/0378-5173(93)90222-2 1:CAS:528: DyaK3sXmtFSmsrw%3D (Pubitemid 23233280)
9. TD Thi M Van Speybroeck V Barillaro J Martens P Annaert P Augustijns J Van Humbeeck J Vermant G Van den Mooter 2009 Formulate-ability of ten compounds with different physicochemical profiles in SMEDDS Eur J Pharm Sci 38 479 488 19782131 10.1016/j.ejps.2009.09.012 1:CAS:528:DC%2BD1MXhsVKgsL%2FF
10. BD Tarr SH Yalkowsky 1989 Enhanced intestinal absorption of cyclosporine in rats through the reduction of emulsion droplet size Pharm Res 6 40 43 2717516 10.1023/A:1015843517762 1:CAS:528:DyaL1MXhtVOmtLk%3D (Pubitemid 19060820)
11. JM Kovarik EA Mueller JB Van Bree W Tetzloff K Kutz 1994 Reduced inter- and intraindividual variability in cyclosporine pharmacokinetics from a microemulsion formulation J Pharm Sci 83 444 446 8207699 10.1002/jps.2600830336 1:CAS:528:DyaK2cXhtFKmu7g%3D (Pubitemid 24224228)
12. Z-G Gao H-G Choi H-J Shin K-M Park S-J Lim K-J Hwang C-K Kim 1998 Physicochemical characterization and evaluation of a microemulsion system for oral delivery of cyclosporin A Int J Pharm 161 75 86 10.1016/S0378-5173(97) 00325-6 1:CAS:528:DyaK1cXhsFeitLs%3D (Pubitemid 28080661)
13. S-M Khoo AJ Humberstone CJH Porter GA Edwards WN Charman 1998 Formulation design and bioavailability assessment of lipidic self-emulsifying formulations of halofantrine Int J Pharm 167 155 164 10.1016/S0378-5173(98)00054-4 1:CAS:528:DyaK1cXksF2mu7s%3D (Pubitemid 28341517)
14. R Holm CJH Porter GA Edwards A Müllertz HG Kristensen WN Charman 2003 Examination of oral absorption and lymphatic transport of halofantrine in a triple-cannulated canine model after administration in self-microemulsifying drug delivery systems (SMEDDS) containing structured triglycerides Eur J Pharm Sci 20 91 97 13678797 10.1016/S0928-0987(03)00174-X 1:CAS:528: DC%2BD3sXnt1Glsrc%3D (Pubitemid 37103236)
15. CJH Porter AM Kaukonen BJ Boyd GA Edwards WN Charman 2004 Susceptibility to lipase-mediated digestion reduces the oral bioavailability of danazol after administration as a medium-chain lipid-based microemulsion formulation Pharm Res 21 1405 1412 15359575 10.1023/B:PHAM.0000036914.22132.cc 1:CAS:528: DC%2BD2cXmtlGnurY%3D (Pubitemid 39149655)
16. FS Nielsen KB Petersen A Müllertz 2008 Bioavailability of probucol from lipid and surfactant based formulations in minipigs: influence of droplet size and dietary state Eur J Pharm Biopharm 69 553 562 18294829 10.1016/j.ejpb.2007.12.020 1:CAS:528:DC%2BD1cXmtVSgsrg%3D
17. CJH Porter WN Charman 2001 In vitro assessment of oral lipid based formulations Adv Drug Deliv Rev 50 S127 S147 11576699 10.1016/S0169-409X(01) 00182-X 1:CAS:528:DC%2BD3MXntVWku7o%3D (Pubitemid 32905359)
18. CM O'Driscoll BT Griffin 2008 Biopharmaceutical challenges associated with drugs with low aqueous solubility-The potential impact of lipid-based formulations Adv Drug Deliv Rev 60 617 624 18155800 10.1016/j.addr.2007.10.012
19. Lee KWY, Porter CJH, Boyd BJ. Gastric processing is a critical determinant of the ability of lipid-based formulations to enhance the oral bioavailability of a model poorly water-soluble drug. Transactions of the 36th Annual Meeting and Exposition of the Controlled Reslease Society, Copenhagen, Denmark; 2009, p. 681.
20. M Grove A Müllertz GP Pedersen JL Nielsen 2007 Bioavailability of seocalcitol: III. Administration of lipid-based formulations to minipigs in the fasted and fed state Eur J Pharm Sci. 31 8 15 17383165 10.1016/j.ejps.2007.01. 007 1:CAS:528:DC%2BD2sXksFegsbY%3D (Pubitemid 46601865)
21. M Armand P Borel B Pasquier C Dubois M Senft M Andre J Peyrot J Salducci D Lairon 1996 Physicochemical characteristics of emulsions during fat digestion in human stomach and duodenum Am J Phys 271 G172 G183 1:CAS:528: DyaK28XkslynsrY%3D
22. M Armand B Pasquier M Andre P Borel M Senft J Peyrot J Salducci H Portugal V Jaussan D Lairon 1999 Digestion and absorption of 2 fat emulsions with different droplet sizes in the human digestive tract Am J Clin Nutr 70 1096 1106 10584056 1:CAS:528:DyaK1MXnslKksbo%3D
23. The Department of Health. Appendix XII B. Dissolution guidance on dissolution testing. Artificial Gastric Juice. British Pharmacopoeia 2009 Volume I & II Monographs: Medicinal and Pharmaceutical Substances. London: The Stationery Office; 2008.
24. JC Lim CA Miller 1991 Dynamic behavior and detergency in systems containing nonionic surfactants and mixtures of polar and nonpolar oils Langmuir 7 2021 2027 10.1021/la00058a010 1:CAS:528:DyaK3MXlvVGkur8%3D
25. M Armand P Borel C Dubois M Senft J Peyrot J Salducci H Lafont D Lairon 1994 Characterization of emulsions and lipolysis of dietary lipids in the human stomach Am J Phys 266 G372 G381 1:CAS:528:DyaK2cXivFCrs7Y%3D
26. M Vertzoni J Dressman J Butler J Hempenstall C Reppas 2005 Simulation of fasting gastric conditions and its importance for the in vivo dissolution of lipophilic compounds Eur J Pharm Biopharm 60 413 417 15893920 10.1016/j.ejpb.2005.03.002 1:CAS:528:DC%2BD2MXlvFarsL0%3D (Pubitemid 40922839)
27. Gowland PA, Marciani L, Fillery-Travis A, Spiller RC. MRI of gastric function. In: Webb GA, Belton PS, Gil AM, and Delgadillo I, editors. Magnetic resonance in food science, a view to the future. The Royal Society of Chemistry, Cambridge; 2001. p. 85-97.
28. L Marciani D Bush P Wright MSJ Wickham B Pick J Wright RM Faulks A Fillery-Travis RC Spiller PA Gowland 2005 Monitoring of gallbladder and gastric coordination by EPI J Magn Reson Imag. 21 82 85 10.1002/jmri.20223 (Pubitemid 40041425)
29. L Marciani RM Faulks MSJ Wickham D Bush B Pick J Wright EF Cox A Fillery-Travis PA Gowland RC Spiller 2009 Effect of intragastric acid stability of fat emulsions on gastric emptying, plasma lipid profile and postprandial satiety Br J Nutr 101 919 928 18680634 10.1017/S0007114508039986 1:CAS:528:DC%2BD1MXktleis78%3D
30. L Marciani C Ramanathan DJ Tyler P Young P Manoj MSJ Wickham A Fillery-Travis RC Spiller PA Gowland 2001 Fat emulsification measured using NMR transverse relaxation J Mag Res. 153 1 6 10.1006/jmre.2001.2421 1:CAS:528:DC%2BD3MXotF2hsrw%3D
31. L Marciani MSJ Wickham D Bush RM Faulks J Wright A Fillery-Travis R Spiller PA Gowland 2006 Magnetic resonance imaging of the behaviour of oil-in-water emulsions in the gastric lumen of man Br J Nutr 95 331 339 16469150 10.1079/BJN20051628 1:CAS:528:DC%2BD28XjtF2qsr0%3D
32. L Marciani MSJ Wickham BP Hills J Wright D Bush RM Faulks A Fillery-Travis RC Spiller PA Gowland 2004 Intragastric oil-in-water emulsion fat fraction measured using inversion recovery echo-planar magnetic resonance imaging J Food Sci 69 E290 E296 10.1111/j.1365-2621.2004.tb11000.x 1:CAS:528:DC%2BD2cXmslKhur4%3D
33. L Marciani MSJ Wickham G Singh D Bush B Pick EF Cox A Fillery-Travis RM Faulks C Marsden PA Gowland R Spiller 2007 Enhancement of intragastric acid stability of a fat emulsion meal delays gastric emptying and increases cholecystokinin release and gall bladder contraction Am J Phys 292 G1607 G1613 1:CAS:528:DC%2BD2sXmvF2lsrY%3D
34. L Marciani J Wright D Bush A Fillery-Travis PA Gowland R Spiller 2001 Assessment of antral grinding of a model solid meal with echo-planar imaging Am J Phys - GI Liver Phys. 280 G844 G849 1:CAS:528:DC%2BD3MXjsVahsb0%3D
35. L Marciani M Wickham J Wright D Bush R Faulks A Fillery-Travis P Gowland RC Spiller 2003 Magnetic resonance imaging (MRI) insights into how fat emulsion stability alters gastric emptying Gastroenterology 124 A581 A581 10.1016/S0016-5085(03)82941-4
36. Vardakou M. Personal communication, 2009.
37. R Aboofazeli N Patel M Thomas MJ Lawrence 1995 Investigations into the formation and characterization of phospholipid microemulsions. IV. Pseudo-ternary phase diagrams of systems containing water-lecithin-alcohol and oil; The influence of oil Int J Pharm 125 107 116 10.1016/0378-5173(95)00125-3 1:CAS:528:DyaK2MXot12jsrs%3D
38. SS Funari G Klose 1995 Phase behaviour of the ternary system POPC/C12E2/2H2O Chem Phys Lipids 75 145 154 10.1016/0009-3084(94)02415-2 1:CAS:528:DyaK2MXksVyku7k%3D
39. A Fini G Fazio G Feroci 1995 Solubility and solubilization properties of non-steroidal anti-inflammatory drugs Int J Pharm 126 95 102 10.1016/0378-5173(95)04102-8 1:CAS:528:DyaK28XksVSrtQ%3D%3D (Pubitemid 26015628)
40. BC Stephenson CO Rangel-Yagui AP Junior LC Tavares K Beers D Blankschtein 2006 Experimental and theoretical investigation of the micellar-assisted solubilization of ibuprofen in aqueous media Langmuir 22 1514 1525 16460069 10.1021/la052530k 1:CAS:528:DC%2BD28XjtFWntQ%3D%3D
41. Wakerly MG, Pouton CW, Meakin BJ, Morton FS. Self-emulsification of vegetable oil-nonionic surfactant mixtures. Phenomena in Mixed Surfactant Systems, American Chemical Society, Washington, DC; 1986. pp. 242-255.
42. FB Rosevear 1954 The microscopy of the liquid crystalline neat and middle phases of soaps and synthetic detergents J Am Oil Chem Soc 31 628 639 10.1007/BF02545595 1:CAS:528:DyaG2MXhtVensw%3D%3D