Toward the establishment of standardized in vitro tests for lipid-based formulations, part 1: Method parameterization and comparison of in vitro digestion profiles across a range of representative formulations

Hywel D. Williams; Philip Sassene; Karen Kleberg; Jean-Claude Bakala-N'Goma; Marilyn Calderone; Vincent Jannin; Annabel  Igonin; Anette Partheil; Delphine Marchaud; Eduardo Jule; Jan Vertommen; Mario Maio; Ross Blundell; Hassan Benameur; Fréderic Carrière; Anette Müllertz; Crhistopher J. H. Porter; Colin W. Pouton

doi:10.1002/jps.23205

Toward the establishment of standardized in vitro tests for lipid-based formulations, part 1: Method parameterization and comparison of in vitro digestion profiles across a range of representative formulations

Hywel D. Williams, Philip Sassene, Karen Kleberg, Jean-Claude Bakala-N'Goma, Marilyn Calderone, Vincent Jannin, Annabel Igonin, Anette Partheil, Delphine Marchaud, Eduardo Jule, Jan Vertommen, Mario Maio, Ross Blundell, Hassan Benameur, Fréderic Carrière, Anette Müllertz, Crhistopher J. H. Porter, Colin W. Pouton

169 Citations (Scopus)

Abstract

The Lipid Formulation Classification System Consortium is an industry-academia collaboration, established to develop standardized in vitro methods for the assessment of lipid-based formulations (LBFs). In this first publication, baseline conditions for the conduct of digestion tests are suggested and a series of eight model LBFs are described to probe test performance across different formulation types. Digestion experiments were performed in vitro using a pH-stat apparatus and danazol employed as a model poorly water-soluble drug. LBF digestion (rate and extent) and drug solubilization patterns on digestion were examined. To evaluate cross-site reproducibility, experiments were conducted at two sites and highly consistent results were obtained. In a further refinement, bench-top centrifugation was explored as a higher throughput approach to separation of the products of digestion (and compared with ultracentrifugation), and conditions under which this method was acceptable were defined. Drug solubilization was highly dependent on LBF composition, but poorly correlated with simple performance indicators such as dispersion efficiency, confirming the utility of the digestion model as a means of formulation differentiation.

Original language	English
Journal	Journal of Pharmaceutical Sciences
Volume	101
Issue number	9
Pages (from-to)	3360-3380
ISSN	0022-3549
DOIs	https://doi.org/10.1002/jps.23205
Publication status	Published - Sept 2012

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Williams, H. D., Sassene, P., Kleberg, K., Bakala-N'Goma, J.-C., Calderone, M., Jannin, V., Igonin, A., Partheil, A., Marchaud, D., Jule, E., Vertommen, J., Maio, M., Blundell, R., Benameur, H., Carrière, F., Müllertz, A., Porter, C. J. H., & Pouton, C. W. (2012). Toward the establishment of standardized in vitro tests for lipid-based formulations, part 1: Method parameterization and comparison of in vitro digestion profiles across a range of representative formulations. Journal of Pharmaceutical Sciences, 101(9), 3360-3380. https://doi.org/10.1002/jps.23205

Toward the establishment of standardized in vitro tests for lipid-based formulations, part 1: Method parameterization and comparison of in vitro digestion profiles across a range of representative formulations. / Williams, Hywel D.; Sassene, Philip; Kleberg, Karen et al.
In: Journal of Pharmaceutical Sciences, Vol. 101, No. 9, 09.2012, p. 3360-3380.

Research output: Contribution to journal › Journal article › Research › peer-review

Williams, HD, Sassene, P, Kleberg, K, Bakala-N'Goma, J-C, Calderone, M, Jannin, V, Igonin, A, Partheil, A, Marchaud, D, Jule, E, Vertommen, J, Maio, M, Blundell, R, Benameur, H, Carrière, F, Müllertz, A, Porter, CJH & Pouton, CW 2012, 'Toward the establishment of standardized in vitro tests for lipid-based formulations, part 1: Method parameterization and comparison of in vitro digestion profiles across a range of representative formulations', Journal of Pharmaceutical Sciences, vol. 101, no. 9, pp. 3360-3380. https://doi.org/10.1002/jps.23205

Williams HD, Sassene P, Kleberg K, Bakala-N'Goma JC, Calderone M, Jannin V et al. Toward the establishment of standardized in vitro tests for lipid-based formulations, part 1: Method parameterization and comparison of in vitro digestion profiles across a range of representative formulations. Journal of Pharmaceutical Sciences. 2012 Sept;101(9):3360-3380. doi: 10.1002/jps.23205

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abstract = "The Lipid Formulation Classification System Consortium is an industry-academia collaboration, established to develop standardized in vitro methods for the assessment of lipid-based formulations (LBFs). In this first publication, baseline conditions for the conduct of digestion tests are suggested and a series of eight model LBFs are described to probe test performance across different formulation types. Digestion experiments were performed in vitro using a pH-stat apparatus and danazol employed as a model poorly water-soluble drug. LBF digestion (rate and extent) and drug solubilization patterns on digestion were examined. To evaluate cross-site reproducibility, experiments were conducted at two sites and highly consistent results were obtained. In a further refinement, bench-top centrifugation was explored as a higher throughput approach to separation of the products of digestion (and compared with ultracentrifugation), and conditions under which this method was acceptable were defined. Drug solubilization was highly dependent on LBF composition, but poorly correlated with simple performance indicators such as dispersion efficiency, confirming the utility of the digestion model as a means of formulation differentiation.",

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AU - Bakala-N'Goma, Jean-Claude

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AU - Jannin, Vincent

AU - Igonin, Annabel

AU - Partheil, Anette

AU - Marchaud, Delphine

AU - Jule, Eduardo

AU - Vertommen, Jan

AU - Maio, Mario

AU - Blundell, Ross

AU - Benameur, Hassan

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AU - Porter, Crhistopher J. H.

AU - Pouton, Colin W.

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