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Type: Journal article
Title: Silica nanoparticles to control the lipase-mediated digestion of lipid-based oral delivery systems
Author: Tan, A.
Simovic, S.
Davey, A.
Rades, T.
Boyd, B.
Prestidge, C.
Citation: Molecular Pharmaceutics, 2010; 7(2):522-532
Publisher: American Chemical Society
Issue Date: 2010
ISSN: 1543-8384
Statement of
Angel Tan, Spomenka Simovic, Andrew K. Davey, Thomas Rades, Ben J. Boyd, and Clive A. Prestidge
Abstract: We investigate the role of hydrophilic fumed silica in controlling the digestion kinetics of lipid emulsions, hence further exploring the mechanisms behind the improved oral absorption of poorly soluble drugs promoted by silica-lipid hybrid (SLH) microcapsules. An in vitro lipolysis model was used to quantify the lipase-mediated digestion kinetics of a series of lipid vehicles formulated with caprylic/capric triglycerides: lipid solution, submicrometer lipid emulsions (in the presence and absence of silica), and SLH microcapsules. The importance of emulsification on lipid digestibility is evidenced by the significantly higher initial digestion rate constants for SLH microcapsules and lipid emulsions (>15-fold) in comparison with that of the lipid solution. Silica particles exerted an inhibitory effect on the digestion of submicrometer lipid emulsions regardless of their initial location, i.e., aqueous or lipid phases. This inhibitory effect, however, was not observed for SLH microcapsules. This highlights the importance of the matrix structure and porosity of the hybrid microcapsule system in enhancing lipid digestibility as compared to submicrometer lipid emulsions stabilized by silica. For each studied formulation, the digestion kinetics is well correlated to the corresponding in vivo plasma concentrations of a model drug, celecoxib, via multiple-point correlations (R(2) > 0.97). This supports the use of the lipid digestion model for predicting the in vivo outcome of an orally dosed lipid formulation. SLH microcapsules offer the potential to enhance the oral absorption of poorly soluble drugs via increased lipid digestibility in conjunction with improved drug dissolution/dispersion.
Keywords: Lipid-based formulations; poorly soluble drugs; hydrophilic fumed silica; in vitro lipolysis; in vitro−in vivo correlations
Rights: © 2010 American Chemical Society
DOI: 10.1021/mp9002442
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