%0 Journal Article
%A Khoshakhlagh, Pooneh
%A Johnson, Raphael
%A Langguth, Peter
%A Nawroth, Thomas
%A Schmueser, Lars
%A Hellmann, Nadja
%A Decker, Heinz
%A Szekely, Noemi
%T Fasted-State Simulated Intestinal Fluid 'FaSSIF-C', a Cholesterol Containing Intestinal Model Medium for In Vitro Drug Delivery Development
%J Journal of pharmaceutical sciences
%V 104
%N 7
%@ 0022-3549
%C New York, NY
%I Wiley
%M FZJ-2016-01509
%P 2213 - 2224
%D 2015
%X 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.
%F PUB:(DE-HGF)16
%9 Journal Article
%U <Go to ISI:>//WOS:000356705500012
%$ pmid:25964103
%R 10.1002/jps.24470
%U https://juser.fz-juelich.de/record/281842