Negatively charged liposomes of sertraline hydrochloride: Formulation, characterization and pharmacokinetic studies

The present study was carried out with an objective to study the extent of delivery of negatively charged liposomes of sertraline hydrochloride to brain via intravenous route for treatment of depressive –like symptoms. Liposomes of sertraline hydrochloride were formulated by film hydration technique using cholesterol, hydrogenated soya phosphatidylcholine-l-α-phosphatidylcholine, and distearoyl phosphatidyl glycerol sodium. Uniform sized vesicles with porous surface morphology with vesicle size of 151.59 nm were prepared. Radioactive imaging performed using 99mTcO4 showed ~5% of uptake of labelled liposomes in brain within 2 h of administration. On administration of liposomes and free drug suspension, approximately, 205.06 ng/ml and 87.18 ng/ml of sertraline were estimated in brain at 36 h. The liposomes can be transported by transcelluar transport which includes phagocytosis and the use of phosphatidylcholine enhances macrophage internalization and delivery to brain. The study indicated significantly higher concentration of sertraline in brain after 36 h, on administration of liposomes as compared to free sertraline suspension. [Display omitted]