Development and in vitro characterization of an oral self-emulsifying delivery system (SEDDS) for rutin fatty ester with high mucus permeating properties

Abstract

The aim of this study was to develop and evaluate a self-emulsifying delivery system (SEDDS) for oral rutin fatty ester administration and to improve its mucus permeating properties by the incorporation of the silicon polymer poly [dimethylsiloxane-co-(3-(2-(2-hydroxyethoxy)ethoxy)propyl]methylsiloxane] (PDMSHEPMS) in the formulation. In order to increase the lipophilicity of the flavonoid and to dissolve it in SEDDS, enzymatic acylation of rutin with lauric acid was catalyzed by lipase from Candida antarctica in acetone. Different formulations were evaluated regarding their emulsifying properties and ability to dissolve the rutin ester. Suitable SEDDS was chosen and characterized regarding droplet size, polydispersity index, and zeta potential. The rutin fatty ester was loaded into SEDDS to 7% (w/w). Different concentrations of PDMSHEPMS were incorporated in SEDDS for following mucus permeation studies. Formulation with 10% of PDMSHEPMS showed 1.9-fold increase in mucus permeation compared to the formulation without PDMSHEPMS. Furthermore, the formulation with 10% of PDMSHEPMS showed a significant increase in mucus permeation compared with rutin fatty ester without formulation. According to these results, SEDDS containing PDMSHEPMS might be a promising strategy to increase the oral bioavailability of rutin.

Keywords: Mucus permeation; Polysiloxane; Rutin; Rutin fatty ester; Self-emulsifying drug delivery systems (SEDDS).