Effect of inorganic mesoporous carriers on 1-palmitoyl-2-linoleoyl-3-acetyl-rac-glycerol-loaded solid self-emulsifying drug delivery system: Physicochemical characterization and bioavailability in rats

The purpose of this study was to assess the impact of inorganic mesoporous carriers on the physicochemical properties and oral bioavailability of 1-palmitoyl-2-linoleoyl-3-acetyl-rac-glycerol (PLAG)-loaded solid self-emulsifying drug delivery system (solid SEDDS). Numerous PLAG-loaded solid SEDDS formulations were prepared by spray drying technique with sodium laurylsulfate (SLS), butylated hydroxyanisole (BHA) and inorganic mesoporous materials as a surfactant, antioxidant and solid carrier, respectively. The mesoporous materials, such as calcium silicate, silicon dioxide and magnesium aluminosilicate were used as the solid carriers. Their physicochemical properties, solubility, dissolution and pharmacokinetic studies in rats were performed compared with drug alone. Three solid SEDDSs composed of PLAG/BHA/SLS/mesopous carrier at the weight ratio of 1:0.0002:0.25:0.5 resulted in a small emulsion droplet and excellent drug loading efficiency. The solid SEDDS formulations prepared with calcium silicate and silicon dioxide showed a rough-surfaced irregular shape and rough-surfaced spheres, respectively. Magnesium aluminosilicate generated a sticky powder, due to its relatively low specific surface area, resulting in insufficient adsorption of PLAG. These solid SEDDSs improved the solubility, dissolution and oral bioavailability of PLAG. Ultimately, the solid SEDDS prepared with silicon dioxide resulted in the best drug loading efficiency, shape, solubility, dissolution and oral bioavailability due to its great specific surface area. Therefore, mesoporous carriers with different specific surface areas markedly influenced the physicochemical properties, solubility, dissolution and oral bioavailability of PLAG-loaded solid SEDDS. (C) 2017 Elsevier B.V. All rights reserved.This work was supported by National Research Foundation (NRF) of South Korea grants funded by the South Korea government (MEST) (nos. 2015R1A2A2A05027872 & 2017R1D1A1B03032530) and a grant (16173MFDS542) from the Ministry of Food and Drug Safety in 2016