Development of solid SEDDS, III: application of Acconon® C-50 and Gelucire® 50/13 as both solidifying and emulsifying agents for medium chain triglycerides

Abstract

Solid self-emulsifying drug delivery systems (SEDDS) for medium chain triglycerides (Captex® 355, ABITEC) were developed using stearoyl polyoxyl glycerides (Acconon® C-50, ABITEC and Gelucire® 50/13, Gattefosse) as both solidifying and emulsifying agents. Different mixtures of the lipid and each solidifying agent were heated to 65ºC until homogenously mixed clear liquids were formed. Probucol was dissolved as the model drug. The molten mass was then filled into hard gelatin capsules, which upon cooling to room temperature converted to a solid mass inside capsules. The triglyceride could be incorporated into the system to a concentration as high as 80% w/w, still maintaining the solid or semisolid consistency of the system. Powder XRD, DSC, microscopy (cross-polarization and confocal fluorescence techniques), dispersion test and particle size analysis of the solid systems with, and without, drug were conducted to characterize different formulations. The solidifying agents maintained their crystallinity in solid systems, while the lipids were interspersed in between crystalline regions. The drug remained solubilized in the lipid phase. The formulations dispersed almost completely in 2 hours with particle size of the dispersed lipid in the range of 250 to 500 nm when the lipid content in the formulation was up to 50% w/w. Thus, a novel method of developing solid formulations of liquid triglycerides by incorporating lipids in stearoyl polyoxyl glycerides has been developed.