Solidification of self-emulsifying drug delivery systems (SEDDS): Impact on storage stability of a therapeutic protein

Four solidification methods for self-emulsifying drug delivery systems (SEDDS) were compared to evaluate the impact of on storage stability an incorporated protein. Papain was loaded in SEDDS via hydrophobic ion pairing (HIP). Liquid (l-SEDDS) either solidified by adsorption solid excipients such as magnesium-aluminometasilicate wet granulation (ssilica-SEDDS) and carbohydrates lyophilisation (scarbo-SEDDS) or incorporation high-melting PEG-surfactants (sPEG-SEDDS) triglycerides (soil-SEDDS) preconcentrates. L- s-SEDDS regarding intrinsic emulsion properties, solid-state form papain, enzyme activity during storage. HIP with deoxycholate showed a precipitation efficiency 82% papain maintained 90% its initial activity. Incorporated present amorphous state, confirming molecular dispersion all In comparison l-SEDDS each method investigated improved papain. Neither nor phase separation observed s-SEDDS. sPEG-SEDDS demonstrated 87.8% highest enzymatic displayed according following rank order: > soil-SEDDS ssilica-SEDDS scarbo-SEDDS remaining after 30 days This work clearly demonstrates that can provide significantly therapeutic proteins corresponding liquid formulations.