Silica nanoparticles to control the lipase-mediated digestion of lipid-based oral delivery systems

Research output: Contribution to journalJournal articlepeer-review

Standard

Silica nanoparticles to control the lipase-mediated digestion of lipid-based oral delivery systems. / Tan, Angel; Simovic, Spomenka; Davey, Andrew K; Rades, Thomas; Boyd, Ben J; Prestidge, Clive A.

In: Molecular Pharmaceutics, Vol. 7, No. 2, 2010, p. 522-32.

Research output: Contribution to journalJournal articlepeer-review

Harvard

Tan, A, Simovic, S, Davey, AK, Rades, T, Boyd, BJ & Prestidge, CA 2010, 'Silica nanoparticles to control the lipase-mediated digestion of lipid-based oral delivery systems', Molecular Pharmaceutics, vol. 7, no. 2, pp. 522-32. https://doi.org/10.1021/mp9002442

APA

Tan, A., Simovic, S., Davey, A. K., Rades, T., Boyd, B. J., & Prestidge, C. A. (2010). Silica nanoparticles to control the lipase-mediated digestion of lipid-based oral delivery systems. Molecular Pharmaceutics, 7(2), 522-32. https://doi.org/10.1021/mp9002442

Vancouver

Tan A, Simovic S, Davey AK, Rades T, Boyd BJ, Prestidge CA. Silica nanoparticles to control the lipase-mediated digestion of lipid-based oral delivery systems. Molecular Pharmaceutics. 2010;7(2):522-32. https://doi.org/10.1021/mp9002442

Author

Tan, Angel ; Simovic, Spomenka ; Davey, Andrew K ; Rades, Thomas ; Boyd, Ben J ; Prestidge, Clive A. / Silica nanoparticles to control the lipase-mediated digestion of lipid-based oral delivery systems. In: Molecular Pharmaceutics. 2010 ; Vol. 7, No. 2. pp. 522-32.

Bibtex

@article{1c63b45eacf64e25a22d949aecd5f292,
title = "Silica nanoparticles to control the lipase-mediated digestion of lipid-based oral delivery systems",
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.",
author = "Angel Tan and Spomenka Simovic and Davey, {Andrew K} and Thomas Rades and Boyd, {Ben J} and Prestidge, {Clive A}",
year = "2010",
doi = "10.1021/mp9002442",
language = "English",
volume = "7",
pages = "522--32",
journal = "Molecular Pharmaceutics",
issn = "1543-8384",
publisher = "American Chemical Society",
number = "2",

}

RIS

TY - JOUR

T1 - Silica nanoparticles to control the lipase-mediated digestion of lipid-based oral delivery systems

AU - Tan, Angel

AU - Simovic, Spomenka

AU - Davey, Andrew K

AU - Rades, Thomas

AU - Boyd, Ben J

AU - Prestidge, Clive A

PY - 2010

Y1 - 2010

N2 - 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.

AB - 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.

U2 - 10.1021/mp9002442

DO - 10.1021/mp9002442

M3 - Journal article

C2 - 20063867

VL - 7

SP - 522

EP - 532

JO - Molecular Pharmaceutics

JF - Molecular Pharmaceutics

SN - 1543-8384

IS - 2

ER -

ID: 40349011