Evaluation of the interaction of propranolol with 1,2-dimyristoyl-sn-glycero-3-phosphocholine (DMPC) liposomes: the partitioning model.
The sorption behavior of the amine containing beta-receptor blocking agent propranolol (Ppn) in 1,2-dimyristoyl-sn-glycero-3-phosphocholine (DMPC) vesicles was investigated. Both protonated and unprotonated Ppn were measured in the continuous phase after removal of the vesicles containing sorbed Ppn by centrifugation. In contrast, by analyzing the surface charge density, deduced from electrophoretic mobility measurements, only the sorbed protonated Ppn was determined. A partitioning model was used to describe the sorption behavior. Sensitivity analysis revealed that sufficiently reliable and independent parameters were obtained. The partition coefficient of the unprotonated Ppn was about 22 times higher than that of the protonated analogue. Statistical analysis revealed a significant increase in the intrinsic partition coefficients of both Ppn analogues with an increase in the salt concentration.
Cocquyt
Jan
J
Particle and Interfacial Technology Group, Faculty of Bioscience Engineering, Ghent University, Coupure Links 653, B-9000 Ghent, Belgium. Jan.Cocquyt@Ugent.be
Saveyn
Pieter
P
Van der Meeren
Paul
P
De Cuyper
Marcel
M
D004134:Dimyristoylphosphatidylcholine / Q000737:chemistry*; D006863:Hydrogen-Ion Concentration; D008081:Liposomes; D008956:Models, Chemical; D015394:Molecular Structure; D011433:Propranolol / Q000737:chemistry*; D012680:Sensitivity and Specificity
D008081:Liposomes; D011433:Propranolol; D004134:Dimyristoylphosphatidylcholine