TY  - JOUR
AU  - Khoshakhlagh, Pooneh
AU  - Johnson, Raphael
AU  - Langguth, Peter
AU  - Nawroth, Thomas
AU  - Schmueser, Lars
AU  - Hellmann, Nadja
AU  - Decker, Heinz
AU  - Szekely, Noemi
TI  - Fasted-State Simulated Intestinal Fluid 'FaSSIF-C', a Cholesterol Containing Intestinal Model Medium for In Vitro Drug Delivery Development
JO  - Journal of pharmaceutical sciences
VL  - 104
IS  - 7
SN  - 0022-3549
CY  - New York, NY
PB  - Wiley
M1  - FZJ-2016-01509
SP  - 2213 - 2224
PY  - 2015
AB  - 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.
LB  - PUB:(DE-HGF)16
UR  - <Go to ISI:>//WOS:000356705500012
C6  - pmid:25964103
DO  - DOI:10.1002/jps.24470
UR  - https://juser.fz-juelich.de/record/281842
ER  -