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@ARTICLE{Khoshakhlagh:281842,
author = {Khoshakhlagh, Pooneh and Johnson, Raphael and Langguth,
Peter and Nawroth, Thomas and Schmueser, Lars and Hellmann,
Nadja and Decker, Heinz and Szekely, Noemi},
title = {{F}asted-{S}tate {S}imulated {I}ntestinal {F}luid
'{F}a{SSIF}-{C}', a {C}holesterol {C}ontaining {I}ntestinal
{M}odel {M}edium for {I}n {V}itro {D}rug {D}elivery
{D}evelopment},
journal = {Journal of pharmaceutical sciences},
volume = {104},
number = {7},
issn = {0022-3549},
address = {New York, NY},
publisher = {Wiley},
reportid = {FZJ-2016-01509},
pages = {2213 - 2224},
year = {2015},
abstract = {A set of biorelevant media "fasted-state simulated
intestinal fluid with cholesterol (FaSSIF-C)" for the in
vitro study of intestinal drug dissolution in the duodenum
was developed. These contain cholesterol at the same levels
as in human bile: the cholesterol content of FaSSIF-7C is
equivalent to healthy female, FaSSIF-10C to healthy male
persons, and FaSSIF-13C to several disease cases that lead
to gallstones. The fluids were studied in three aspects:
biocompatibility, intestinal nanostructure, and solubilizing
power of hydrophobic drugs of the BCS class II. The
biocompatibility study showed no toxic effects in a Caco-2
cell system. The drug-solubilizing capacity toward
Fenofibrate, Danazol, Griseofulvin, and Carbamazepine was
assessed as example. It varied with the cholesterol content
widely from a fourfold improvement to a twofold reduction.
The nanostructure study by dynamic light scattering and
small-angle neutron scattering indicated vesicles as the
main component of FaSSIF-C in equilibrium (> 1 h), but at
high cholesterol content, larger particles were observed as
a minor contribution. The neutron experiments indicated the
presence of complex micelle-vesicle mixtures, even after 1 h
development of fed-state bile model to FaSSIF. The results
indicate that cholesterol affects some drugs in
solubilization and particle size in intestinal model
fluids.},
cin = {JCNS (München) ; Jülich Centre for Neutron Science JCNS
(München) ; JCNS-FRM-II / Neutronenstreuung ; JCNS-1},
ddc = {610},
cid = {I:(DE-Juel1)JCNS-FRM-II-20110218 /
I:(DE-Juel1)JCNS-1-20110106},
pnm = {6G15 - FRM II / MLZ (POF3-6G15) / 6G4 - Jülich Centre for
Neutron Research (JCNS) (POF3-623)},
pid = {G:(DE-HGF)POF3-6G15 / G:(DE-HGF)POF3-6G4},
experiment = {EXP:(DE-MLZ)KWS2-20140101},
typ = {PUB:(DE-HGF)16},
UT = {WOS:000356705500012},
pubmed = {pmid:25964103},
doi = {10.1002/jps.24470},
url = {https://juser.fz-juelich.de/record/281842},
}