Amiodarone (AMI) is a low water-solubility
drug, which is very useful in the treatment of severe
cardiac disease. Its adverse effects are associated with toxicity in different tissues. Several
antioxidants have been shown to reduce, and prevent AMI toxicity. The aim of this work was to develop and characterize
Dimyristoylphosphatidylcholine (
DMPC) liposomal carriers doped with
ascorbyl palmitate (Asc16) as
antioxidant, in order to either minimize or avoid the adverse effects produced by AMI. The employment of
liposomes would avoid the use of cosolvents in AMI formulations, and Asc16 could minimize the adverse effects of AMI. To evaluate the partition and integration of AMI and Asc16 in
lipid membranes, penetration studies into
DMPC monolayers were carried out. The disturbance of the
liposomes membranes was studied by generalized polarization (GP). The stability of
liposomes was evaluated experimentally and by means of the Derjaguin-Landau-Verwey-Overbeek (DLVO) theory. The size particle and zeta potential (ζ) values of the
liposomes were used for application in calculations for attractive and repulsive forces in DLVO theory. In experimental conditions all of these vesicles showed stability at time 0, but only DMPC + Asc16 10% + AMI 10%
liposomes kept their size stable and ζ during 28 days. These results are encouraging and suggest that such systems could be suitable for AMI delivery formulations.