Cellular uptake of self-emulsifying drug-delivery systems: polyethylene glycol versus polyglycerol surface

Comparison of the impact of polyethylene glycol (PEG) and polyglycerol (PG) surface decoration on self-emulsifying drug delivery system (SEDDS)-membrane interaction and cellular uptake.   PEG-, PEG/PG- and PG-SEDDS were assessed regarding their self-emulsifying properties, surface charge, bile salt...

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Published in:Nanomedicine (London, England) England), 2020-08, Vol.15 (19), p.1829-1841
Main Authors: Friedl, Julian David, Steinbring, Christian, Zaichik, Sergey, Le, Nguyet-Minh Nguyen, Bernkop-Schnürch, Andreas
Format: Article
Language:English
Subjects:
Bile
cellular uptake
confocal microscopy
nanoemulsion
PEG-free self-emulsifying drug-delivery system
Phenols
Polyethylene glycol
polyglycerol surfactants
SEDDS
Surfactants
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Summary:Comparison of the impact of polyethylene glycol (PEG) and polyglycerol (PG) surface decoration on self-emulsifying drug delivery system (SEDDS)-membrane interaction and cellular uptake.   PEG-, PEG/PG- and PG-SEDDS were assessed regarding their self-emulsifying properties, surface charge, bile salt fusibility, cellular uptake and interaction with endosome-mimicking membranes. SEDDS exhibited droplet sizes between 150 and 175 nm, a narrow size distribution and self-emulsified within 7 min. Higher PEG-surfactant amounts in SEDDS resulted in charge-shielding and thus in a decrease of ζ potential up to Δ11 mV. The inert PEG-surface hampered bile salt fusion and interfered SEDDS–cell interaction. By reducing the PEG-surfactant amount to 10%, cellular uptake increased twofold compared with PEG-SEDDS containing 40% PEG-surfactant. PG-SEDDS containing no PEG-surfactants showed a threefold increased cellular uptake. Furthermore, complete replacement of PEG-surfactants by PG-surfactants led to enhanced cellular interaction and improved disruption endosome-like membranes.  PG-surfactants demonstrated high potential to address PEG-surface associated drawbacks in SEDDS.
ISSN:1743-5889
1748-6963
DOI:10.2217/nnm-2020-0127