Role of Biorelevant Media in the Estimation of In Vitro Lipolysis and Food Impact on Self-emulsifying Drug Delivery Systems

Abstract

Self-emulsifying drug delivery systems (SEDDS) include self-microemulsifying drug delivery system (SMEDDS) and self-nanoemulsifying drug delivery system (SNEDDS) whose major benefits are reduction of inter/intrasubject variability and food effect that results in a better pharmacological response of the drug. Oral intake of these formulations triggers the digestion process because of pancreatic lipase which emulsifies/digests the lipidic ingredients of the formulation leading to precipitation of the drug. As a tool to foresee in vivo medicament precipitation, in vitro lipolysis models are established. Biorelevant media play an important role to study the effect of in vitro lipolysis and food impact on the bioavailability of SEDDS formulations. It is vital to generate the composition of fluids for both fed and fasting conditions of gastric, small intestine and colon to investigate the impact of in vitro lipolysis and food on drug’s release behavior from the formulation. Fed/Fasted state simulated gastric fluid (Fe/FaSSGF), and Fed/Fasted state simulated gastric fluid (Fe/FaSSIF) (Phosphate buffers) are first-generation. While Fa/FeSSIF-V2 (maleate) are second- generation biorelevant media utilized for these studies. FaSSIF-V3 belongs to the thirdgeneration which differs from other generations in the composition and source of bile salts. With updates in physiological data, it is vital to incorporate changes in dissolution media composition to make it more biorelevant. This review paper mainly emphasized the compositions of biorelevant media of gastric and small intestine for both fed and fasting conditions. Besides, applications of biorelevant media to investigate the effect of in vitro lipolysis and food on SEDDS are discussed with some recent research reports.