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@ARTICLE{Schwarzinger:640697,
author = {Schwarzinger, Jacqueline and Bello, Gianluca and Tropin,
Timur and Wölk, Christian and Blanchet, Clement and
Adelsberger, Sigrid and Hädrich, Gabriela and Rollinger,
Judith M. and Grienke, Ulrike and Harvey, Richard and
Dailey, Lea Ann},
title = {{P}ulmonary delivery of anti-infectives from natural
sources: {D}evelopment and characterization of liposomal
sanggenon formulations},
journal = {European journal of pharmaceutical sciences},
volume = {215},
issn = {0928-0987},
address = {New York, NY [u.a.]},
publisher = {Elsevier},
reportid = {PUBDB-2025-04837},
pages = {107361},
year = {2025},
abstract = {Sanggenon C (SGC) and sanggenon D (SGD) are stereoisomeric
natural products with promising anti-infective potential,
especially against pathogens involved in acute respiratory
infections. However, their bulky structures, poor aqueous
solubility, and low oral bioavailability present major
therapeutic challenges. Inhalation enables direct delivery
to the site of infection while minimizing systemic exposure.
Liposomal formulations DMPC:DMPG (2:1 w/w) of SGC and SGD,
prepared via ethanol injection, achieved high drug loadings
(> 3.5 mg/mL). Drug-lipid interactions were evaluated via
DSC, Langmuir trough studies, SAXS, and cryo-TEM, showing
incorporation of the compounds in the lipid bilayer. While
stereochemistry-dependent differences were evident in
vesicle size and thermotropic behavior, other biophysical
data indicated that these differences were largely mitigated
upon formulation. Liposomal formulations showed an excellent
stability during nebulization with a vibrating mesh
nebulizer (mass median aerodynamic diameters: 1.30–1.35
µm) and the high affinity of the compounds for the lipid
bilayer resulted in a sustained in vitro release profile
(8–9 $\%$ after 240 h). The retention of the drugs in the
liposomes also significantly reduced cytotoxicity at 24 h
compared to neat compounds. These findings highlight the
importance of stereochemistry in drug-membrane interaction,
yet their similar formulation performance suggests that both
compound formulations are promising candidates for pulmonary
anti-infective therapy.},
cin = {EMBL-User / EMBL},
ddc = {610},
cid = {I:(DE-H253)EMBL-User-20120814 / I:(DE-H253)EMBL-20120731},
pnm = {6G3 - PETRA III (DESY) (POF4-6G3)},
pid = {G:(DE-HGF)POF4-6G3},
experiment = {EXP:(DE-H253)P-P12-20150101},
typ = {PUB:(DE-HGF)16},
doi = {10.1016/j.ejps.2025.107361},
url = {https://bib-pubdb1.desy.de/record/640697},
}