Wk. Subczynski et al., PARTITIONING AND LOCALIZATION OF SPIN-LABELED AMANTADINE IN LIPID BILAYERS - AN EPR STUDY, Journal of pharmaceutical sciences, 87(10), 1998, pp. 1249-1254
EPR was used to study the distribution of the spin-labeled amantadine
(AA-SL) between the bulk hydrophobic-hydrocarbon solvent, light paraff
in oil, and water and between hydrophobic-hydrocarbon chain region of
lipid membranes and water. The AA-SL molecules were soluble in both hy
drophobic and polar regions of investigated systems. It was shown that
the partition coefficient of AA-SL between the hydrocarbon region of
the L-alpha-dimyristoylphosphatidylcholine fluid-phase membrane and wa
ter is much higher than between bulk hydrocarbon solvent and water. Fu
rthermore, the partitioning of AA-SL into membranes of multilamellar l
iposomes made of L-alpha-dimyristoylphosphatidylcholine, L-alpha-dipal
mitoylphosphatidylcholine, and L-alpha-distearoylphosphatidylcholine w
as studied as a function of temperature, indicating no abrupt change a
t the main phase transition of these membranes. It is also clear from
our data that AA-SL can penetrate into the gel-phase membrane practica
lly with the same partitioning as into the fluid-phase membrane. Furth
ermore, it was shown that at least part of the AA-SL molecule is deepl
y buried in the hydrocarbon chain region of the membrane.