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@ARTICLE{Hirlak:893390,
author = {Hirlak, Ozan and Dieluweit, Sabine and Merkel, Rudolf and
Wagner, Karl G.},
title = {{P}olymer-mediated drug supersaturation – {A} spotlight
on the interplay between phase-separated amorphous drug
colloids and dissolved molecules},
journal = {Journal of colloid and interface science},
volume = {603},
issn = {0021-9797},
address = {Amsterdam [u.a.]},
publisher = {Elsevier},
reportid = {FZJ-2021-02731},
pages = {370 - 379},
year = {2021},
abstract = {HypothesisColloidal aggregation phenomena have been found
responsible for the supersaturation of poorly water-soluble
drugs, potentially leading to bioavailability enhancements.
Unlike coarse precipitates, phase separation in the form of
colloids, is expected to enhance drug supersaturation
performance. Therefore, a high proportion of these colloids
should correlate with the extent and the kinetics of
supersaturation. The prime objective of the current study is
to provide a mechanistic understanding on supersaturation
for the model drug albendazole (ALB) in combination with
twelve polymers.ExperimentsSpecies separated after a
pH-shift were characterized by dynamic light scattering
(DLS), freeze-fracture electron microscopy (FF-EM) and
transmission X-ray diffraction (XRD). Laser diffraction (LD)
in a liquid cell was introduced for a relative
quantification of the colloidally separated species,
described as colloid fraction. The pH-dependent
supersaturation was assessed online using a miniaturized
dissolution assay.FindingsHere, a measure of the extent of
amorphous colloidal phase separation was established, and
its impact on supersaturation was evaluated. As a result, a
correlation was found between the extent of supersaturation
and the colloid fraction. This confirmed the dependence of
polymer-mediated enabling and preservation of
supersaturation on the ability of polymers to stabilize
colloid fractions. Furthermore, a fixed ratio was suggested
between the dissolved drug and colloidally separated drug as
the kinetic profiles of both species showed similar
trajectories. In conclusion, colloid fractions were
identified to be responsible for dissolved and potentially
bioavailable drug molecules.},
cin = {IBI-2},
ddc = {540},
cid = {I:(DE-Juel1)IBI-2-20200312},
pnm = {5241 - Molecular Information Processing in Cellular Systems
(POF4-524)},
pid = {G:(DE-HGF)POF4-5241},
typ = {PUB:(DE-HGF)16},
pubmed = {34197986},
UT = {WOS:000703595700007},
doi = {10.1016/j.jcis.2021.06.089},
url = {https://juser.fz-juelich.de/record/893390},
}