The
aim of this study was to investigate the fate and the impact
of cosolvents in self-emulsifying drug delivery systems (SEDDS). Three
different SEDDS comprising the cosolvents DMSO (F
D
), ethanol
(F
E
), and benzyl alcohol (F
BA
) as well as the
corresponding formulations without these cosolvents (F
D0
, F
E0
, and F
BA0
) were developed. Mean droplet
size, polydispersity index (PDI), ζ potential, stability, and
emulsification time were determined. Cosolvent release studies were
performed via the dialysis membrane method and Taylor dispersion analysis
(TDA). Furthermore, the impact of cosolvent utilization on payloads
in SEDDS was examined using quinine as a model drug. SEDDS with and
without a cosolvent showed no significant differences in droplet size,
PDI, and ζ potential. The emulsification time was 3-fold (F
D0
), 80-fold (F
E0
), and 7-fold (F
BA0
)
longer due to the absence of the cosolvents. Release studies in demineralized
water provided evidence for an immediate and complete release of DMSO,
ethanol, and benzyl alcohol. TDA confirmed this result. Moreover,
a 1.4-fold (F
D
), 2.91-fold (F
E
), and 2.17-fold
(F
BA
) improved payload of the model drug quinine in the
selected SEDDS preconcentrates was observed that dropped after emulsification
within 1–5 h due to drug precipitation. In parallel, the quinine
concentrations decreased until reaching the same levels of the corresponding
SEDDS without cosolvents. Due to the addition of hydrophilic cosolvents,
the emulsifying properties of SEDDS are strongly improved. As hydrophilic
cosolvents are immediately released from SEDDS during the emulsification
process, however, their drug solubilizing properties in the resulting
oily droplets are very limited.