Preparation of spray-dried microparticles using Gelucire 44/14 and porous calcium silicate or spherical microcrystalline cellulose to enhance transport of water-insoluble pranlukast hemihydrate across Caco-2 monolayers

The aim of this work was to prepare spray-dried microparticles using Gelucire®44/14 (GLC) and porous calcium silicate (FLR) or spherical crystalline cellulose (M06) to enhance transport of poorly water-soluble pranlukast hemihydrate (PLH) across Caco-2 monolayers. FLR or M06 were added to the PLH–GLC aqueous mixture prepared by adding distilled water at 60 °C to a melted mixture of PLH/GLC (1/1) at a PLH–GLC/carrier ratio of 1/1 or 1/17. Spray-dried FLR microparticles have the PLH–GLC solid dispersion (SD) in their pores and spray-dried M06 microparticles have the PLH–GLC SD on their surface. The dissolutions of PLH from the spray-dried FLR (SD/FLR = 1/1), spray-dried M06 (SD/M06 = 1/1), and spray-dried M06 (SD/M06 = 1/17) microparticles in Tween 80 aqueous solution were markedly fast. The transport of PLH from the spray-dried FLR (SD/FLR = 1/1) across Caco-2 monolayers was hardly observed. The transport of PLH across Caco-2 monolayers from the spray-dried M06 (SD/M06 = 1/17) increased with time, and the transport was significantly higher compared to that from PLH powder. The addition of polyethylene glycol 1500 into GLC of the spray-dried M06 was effective to increase the transport of PLH across Caco-2 monolayers. Spray-dried microparticles of PLH using GLC and M06 are a feasible means of enhancing transport across Caco-2 monolayers.