Toward the establishment of standardized in vitro tests for lipid-based formulations, part 4: Proposing a new lipid formulation performance classification system

Journal of Pharmaceutical Sciences

Volumn 103, Issue 8, 2014, Pages 2441-2455

  Williams, Hywel D ^a,b   Sassene, Philip ^c   Kleberg, Karen ^c   Calderone, Marilyn ^d   Igonin, Annabel ^b   Jule, Eduardo ^b   Vertommen, Jan ^b   Blundell, Ross ^d   Benameur, Hassan ^b   Müllertz, Anette ^c   Porter, Christopher J H ^a   Pouton, Colin W ^a  

^a MONASH UNIVERSITY   (Australia)

^b CAPSUGEL   (France)

^c UNIVERSITY OF COPENHAGEN   (Denmark)

^d SANOFI   (France)

Author keywords

bioavailability; drug solubilization; in vitro digestion testing; in vitro models; LFCS Consortium; lipid based drug delivery systems; precipitation; SEDDS; solubility; supersaturation

Indexed keywords

BILE SALT; CAPTEX 300; CREMOPHOR; DIETHYLENE GLYCOL MONOETHYL ETHER; EXCIPIENT; FENOFIBRATE; LIPID; MAISINE 35 1; MEDIUM CHAIN ACYLGLYCEROL; OCTANOIN; POLYSORBATE 85; SURFACTANT; TOLFENAMIC ACID; TRANSCUTOL HP; UNCLASSIFIED DRUG; ANALGESIC AGENT; ANTHRANILIC ACID DERIVATIVE; ANTILIPEMIC AGENT; BILE ACID; DRUG;

ARTICLE; CLASSIFICATION; CONCENTRATION (PARAMETERS); DIGESTION; DISPERSION; DRUG FORMULATION; DRUG SOLUBILITY; HYDROPHILICITY; IN VITRO STUDY; PH; CHEMISTRY; MEDICINAL CHEMISTRY; PROCEDURES; SOLUBILITY;

ANALGESICS; BILE ACIDS AND SALTS; CHEMISTRY, PHARMACEUTICAL; EXCIPIENTS; FENOFIBRATE; HYDROGEN-ION CONCENTRATION; HYPOLIPIDEMIC AGENTS; LIPIDS; ORTHO-AMINOBENZOATES; PHARMACEUTICAL PREPARATIONS; SOLUBILITY; SURFACE-ACTIVE AGENTS;

EID: 84905103012     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.24067     Document Type: Article

References (39)

1. Pouton CW,. 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 (3-4): 278-287.
2. Cuine JF, McEvoy CL, Charman WN, Pouton CW, Edwards GA, Benameur H, Porter CJH,. 2008. 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): 995-1012.
3. Christiansen A, Backensfeld T, Weitschies W,. 2010. Effects of non-ionic surfactants on in vitro triglyceride digestion and their susceptibility to digestion by pancreatic enzymes. Eur J Pharm Sci 41 (2): 376-382.
4. Fernandez S, Jannin V, Rodier JD, Ritter N, Mahler B, Carriere F,. 2007. Comparative study on digestive lipase activities on the self emulsifying excipient Labrasol (R), medium chain glycerides and PEG esters. Biochim Biophys Acta 1771 (5): 633-640.
5. Igonin A, Vertommen J, Benameur H,. 2012. Physical and Biological Parameters of Poorly Bioavailable Compounds That Influence the Development of Lipid-Based Oral Drug Delivery Systems. Annual meeting of the Academy of the American Pharmaceutical Scientists. Chicago.
6. Gao P, Rush BD, Pfund WP, Huang TH, Bauer JM, Morozowich W, Kuo MS, Hageman MJ,. 2003. Development of a supersaturable SEDDS (S-SEDDS) formulation of paclitaxel with improved oral bioavailability. J Pharm Sci 92 (12): 2386-2398.
7. Cuine JF, Charman WN, Pouton CW, Edwards GA, Porter CJH,. 2007. Increasing the proportional content of surfactant (Cremophor EL) relative to lipid in self-emulsifying lipid-based formulations of danazol reduces oral bioavailability in beagle dogs. Pharm Res 24 (4): 748-757.
8. Williams HD, Sassene P, Kleberg K, Bakala N'Goma JC, Calderone M, Jannin V, Igonin A, Partheil A, Marchaud D, Jule E, Vertommen J, Maio M, Blundell R, Benameur H, Carriere F, Mullertz A, Porter CJH, Pouton CW,. 2012. Toward the establishment of standardized in vitro tests for lipid-based formulations: 1) Method parameterization and comparison of in vitro digestion profiles across a range of representative formulations. J Pharm Sci 101 (9): 3360-3380.
9. Williams HD, Anby MU, Sassene P, Kleberg K, Bakala N'Goma JC, Calderone M, Jannin V, Igonin A, Partheil A, Marchaud D, Jule E, Vertommen J, Maio M, Blundell R, Benameur H, Carriere F, Mullertz A, Pouton CW, Porter CJH,. 2012. Toward the establishment of standardized in vitro tests for lipid-based formulations: 2) The effect of bile salt concentration and drug loading on the performance of type I, II, IIIA, IIIB and IV formulations during in vitro digestion. Mol Pharm 9 (11): 3286-3300.
10. Williams HD, Sassene P, Kleberg K, Calderone M, Igonin A, Jule E, Vertommen J, Blundell R, Benameur H, Mullertz A, Pouton CW, Porter CJH,. 2013. Toward the establishment of standardized in vitro tests for lipid-based formulations, part 3: Understanding supersaturation versus precipitation potential during the in vitro digestion of type I, II, IIIA, IIIB and IV lipid-based formulations. Pharm Res 30 (12): 3059-3076.
11. Sassene P, Kleberg K, Williams HD, Bakala N'Goma JC, Calderone M, Jannin V, Igonin A, Partheil A, Marchaud D, Jule E, Vertommen J, Maio M, Blundell R, Benameur H, Carriere F, Mullertz A, Porter CJH, Pouton CW,. 2013. Toward the establishment of standardized in vitro tests for lipid-based formulations: 6) Effect of varying pancreatin and calcium levels. Submitted AAPS Journal.
12. Amidon GL, Lennernas H, Shah VP, Crison JR,. 1995. A theoretical basis for a biopharmaceutic drug classification-The correlation of in-vitro drug product dissolution and in-vivo bioavailability. Pharm Res 12 (3): 413-420.
13. Jule E,. 2013. Accelerating lipid-based drug formulation through application of an expert system. Capsugel White Paper.
14. Williams HD, Anby MU, McEvoy C, Thomas N, Vertommen J, Blundell R, Benameur H, Mullertz A, Porter CJH, Pouton CW,. 2013. The LFCS Consortium-(1) In vitro dispersion tests are an effective first screen during lipid-based formulation development and evaluation. San Antonio, Texas: AAPS Annual Meeting.
15. Kalantzi L, Goumas K, Kalioras V, Abrahamsson B, Dressman J, Reppas C,. 2006. Characterization of the human upper gastrointestinal contents under conditions simulating bioavailability/bioequivalence studies. Pharm Res 23 (1): 165-176.
16. Moreno MPdlC, Oth M, Deferme S, Lammert F, Tack J, Dressman J, Augustijns P,. 2006. Characterization of fasted-state human intestinal fluids collected from duodenum and jejunum. J Pharm Pharmacol 58 (8): 1079-1089.
17. Clarysse S, Tack J, Lammert F, Duchateau G, Reppas C, Augustijns P,. 2009. Postprandial evolution in composition and characteristics of human duodenal fluids in different nutritional states. J Pharm Sci 98 (3): 1177-1192.
18. Kossena GA, Charman WN, Wilson CG, O'Mahony B, Lindsay B, Hempenstall JM, Davison CL, Crowley PJ, Porter CJH,. 2007. Low dose lipid formulations: Effects on gastric emptying and biliary secretion. Pharm Res 24 (11): 2084-2096.
19. Devraj R, Williams HD, Warren DB, Mohsin K, Porter CJH, Pouton CW,. 2013. In vitro assessment of drug-free and fenofibrate-containing lipid formulations using dispersion and digestion testing gives detailed insights into the likely fate of formulations in the intestine. Eur J Pharm Sci 49 (4): 748-760.
20. Devraj R, Williams HD, Warren DB, Porter CJH, Pouton CW,. 2013. Choice of nonionic surfactant used to formulate Type IIIA self-emulsifying drug delivery systems has a pronounced influence on the degree of drug supersaturation that develops during in vitro digestion. J Pharm Sci 103 (4): 1050-1060.
21. Kleberg K, Jacobsen F, Fatouros DG, Mullertz A,. 2010. Biorelevant media simulating fed state intestinal fluids: Colloid phase characterization and impact on solubilization capacity. J Pharm Sci 99 (8): 3522-3532.
22. Pouton CW, Porter CJH,. 2008. Formulation of lipid-based delivery systems for oral administration: Materials, methods and strategies. Adv Drug Deliv Rev 60 (6): 625-637.
23. Gao P, Morozowich W,. 2006. Development of supersaturatable self-emulsifying drug delivery system formulations for improving the oral absorption of poorly soluble drugs. Expert Opin Drug Deliv 3 (1): 97-110.
24. Narang AS, Delmarre D, Gao D,. 2007. Stable drug encapsulation in micelles and microemulsions. Int J Pharm 345 (1): 9-25.
25. Chen X-Q, Gudmundsson OS, Hageman MJ,. 2012. Application of lipid-based formulations in drug discovery. J Med Chem 55: 7945-7956.
26. Williams HD, Trevaskis NL, Yeap YY, Anby MU, Pouton CW, Porter CJ,. 2013. Lipid-based formulations and drug supersaturation: Harnessing the unique benefits of the lipid digestion/absorption pathway. Pharm Res 30 (12): 2979-2992.
27. Anby MU, Williams HD, McIntosh M, Benameur H, Edwards GA, Pouton CW, Porter CJH,. 2012. Lipid digestion as a trigger for supersaturation: In vitro and in vivo evaluation of the utility of polymeric precipitation inhibitors in self emulsifying drug delivery systems. Mol Pharm 9: 2063-2079.
28. Williams HD, Trevaskis NL, Charman SA, Shanker RM, Charman WN, Pouton CW, Porter CJH,. 2013. Strategies to address low drug solubility in discovery and development. Pharm Rev 65 (1): 315-499.
29. Porter CJH, Kaukonen AM, Boyd BJ, Edwards GA, Charman WN,. 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 (8): 1405-1412.
30. Porter CJH, Kaukonen AM, Taillardat-Bertschinger A, Boyd BJ, O'Connor JM, Edwards GA, Charman WN,. 2004. Use of in vitro lipid digestion data to explain the in vivo performance of triglyceride-based oral lipid formulations of poorly water-soluble drugs: Studies with halofantrine. J Pharm Sci 93 (5): 1110-1121.
31. Griffin BT, Kuentz M, Vertzoni M, Kostewicz ES, Fei Y, Faisal W, Stillhart C, O'Driscoll C, Reppas C, Dressman JB,. 2013. Comparison of in vitro tests at various levels of complexity for the prediction of in vivo performance of lipid-based formulations: Case studies with fenofibrate. Eur J Pharm Biopharm 86 (3): 427-437.
32. Yeap YY, Trevaskis NL, Porter CJH,. 2013. The supersaturation tendency of drugs during intestinal processing of lipid-based formulations is greater for basic than neutral/acidic drugs. Mol Pharm 10 (7): 2601-2615.
33. Yeap YY, Trevaskis NL, Quach T, Tso P, Charman WN, Porter CJH,. 2013. Intestinal bile secretion promotes drug absorption from lipid colloidal phases via induction of supersaturation. Mol Pharm 10 (5): 1874-1889.
34. Hofmann AF, Mysels KJ,. 1987. Bile salts as biological surfactants. Colloids Surf 30 (1): 145-173.
35. Hofmann A, Small D,. 1967. Detergent properties of bile salts: Correlation with physiological function. Ann Rev Med 18 (1): 333-376.
36. Mohsin K, Long MA, Pouton CW,. 2009. Design of lipid-based formulations for oral administration of poorly water-soluble drugs: Precipitation of drug after dispersion of formulations in aqueous solution. J Pharm Sci 98 (10): 3582-3595.
37. Gao P, Akrami A, Alvarez F, Hu J, Li L, Ma C, Surapaneni S,. 2009. Characterization and optimization of AMG 517 supersaturatable self-emulsifying drug delivery system (S-SEDDS) for improved oral absorption. J Pharm Sci 98 (2): 516-528.
38. Tønsberg H, Holm R, Bisgaard J, Jacobsen J, Müllertz A,. 2010. Effects of polysorbate 80 on the in-vitro precipitation and oral bioavailability of halofantrine from polyethylene glycol 400 formulations in rats. J Pharm Pharmacol 62 (1): 63-70.
39. Butler JM, Dressman JB,. 2010. The developability classification system: Application of biopharmaceutics concepts to formulation development. J Pharm Sci 99 (12): 4940-4954.