Abstract
Purpose. Novel porous silicon microparticles were fabricated and loaded with fluorescein isothiocyanate (FITC)-insulin, a model hydrophilic pharmacologically active protein, along with varied doses of sodium laurate (C12), a well-known permeation enhancer.
Methods. Particle and liquid formulations were compared as a function of apical to basolateral flux of FITC-insulin across differentiated human intestinal Caco-2 cell monolayers grown on Transwell® inserts.
Results. The flux of FITC-insulin from silicon particles across cell monolayers was nearly 10-fold higher compared with liquid formulations with permeation enhancer and approximately 50-fold compared with liquid formulations without enhancer. By increasing C12 dose per particle with a concomitant decrease in total particles added per monolayer, the percent of FITC-insulin transport resulted in a linear increase up to 25% monolayer coverage.
Conclusions. Although maintaining monolayer integrity and transepithelial electrical resistance, maximum drug transport (20%/h) was achieved with 0.337 μg C12 dose per particle, and total particle loading at 25% monolayer coverage.
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Foraker, A.B., Walczak, R.J., Cohen, M.H. et al. Microfabricated Porous Silicon Particles Enhance Paracellular Delivery of Insulin Across Intestinal Caco-2 Cell Monolayers. Pharm Res 20, 110–116 (2003). https://doi.org/10.1023/A:1022211127890
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DOI: https://doi.org/10.1023/A:1022211127890