Unit:
Κατεύθυνση Φαρμακευτική Ανάλυση - Έλεγχος ποιότηταςLibrary of the School of Science
Author:
Tsagkrasouli Maria
Supervisors info:
Α. Τσαντίλη, Ομ. Καθηγήτρια, Τμήμα Φαρμακευτικής, ΕΚΠΑ
Ε. Παντερή, Αν. Καθηγήτρια, Τμήμα Φαρμακευτικής, ΕΚΠΑ
Κ. Γιαγκίνης, Επικ. Καθηγητής, Τμήμα Επιστήμης Τροφίμων και Διατροφής, Πανεπιστήμιο Αιγαίου
Original Title:
Προσδιορισμός χρωματογραφικών δεικτών φλαβονοειδών με τη χρήση χρωματογραφίας ακινητοποιημένων τεχνητών μεμβρανών και συσχέτισή τους με την εντερική διαπερατότητα
Translated title:
Estimation of intestinal permeability of flavonoid analogues by the use of biomimetic chromatography
Summary:
The retention behavior of 41 flavonoid analogues on two immobilized artificial membrane (IAM) stationary phases, IAM.PC.MG and IAM.PC.DD2 types was investigated using phosphate- buffered saline at pH=7.4 as eluent.The flavonoids followed a uniform elution mechanism on both columns, considering the strong linear correlation between extrapolated to pure aqueous phase retention factors, logkw(IAM) and the slopes, S, of the extrapolation procedure. The interrelation between logkw(IAM) values determined on the two stationary phases was satisfactory, although logkw(IAM.PC.DD2) values are generally higher than logkw(IAM.PC.MG). IAM retention factors were also compared with octanol- water partition (logP) and distribution coefficient (logD) at pH= 7.4. Both expressions of lipophilicity exhibited similar performance on their linear correlations with logkw(IAM). The role of electrostatic interactions to IAM retention of flavonoids was less pronounced compared to previous studies with structurally- diverse drugs due to the limited ionization of the investigated compounds at pH=7.4. Finally, the relationship between IAM retention and data of passage through Caco-2 cultured cell lines (logPapp) taken from the literature was established. Statistically significant linear and non- linear models between IAM retention factors and experimental Caco-2 permeability were constructed, including Abraham’s acidity and basicity parameters as additional physicochemical descriptors. These models were comparable or better in terms of statistics with those constructed by the use of octanol- water partitioning. The two IAM stationary phases showed similar predictive performance towards cell- based permeability.
Main subject category:
Science
Other subject categories:
Pharmacy
Keywords:
Immobilized Artificial Membrane (IAM) Chromatography; Lipophilicity; Phospholipophilicity; Flavonoids; Intestinal permeability; Caco-2 permeability assay
Number of references:
218
