A novel candidate named 5-(3,5-dichloro-2-hydroxybenzylamino)-2-
hydroxybenzoic acid (ZL006) can effectively treat focal cerebral ischemic stroke.
However, the application potential of ZL006 was compromised by its poor solubility.
In this study, ZL006 was loaded effectively into liposomes to improve the solubility
and bioavailability. The particle size of ZL006-loaded liposomes (LPs) was about
115.5 nm with acceptable polydispersity index. The in vitro release profiles indicated that ZL006 could keep sustained
release from LPs for more than 48 h. The results of pharmacokinetics study proved that the mean residence time of LPs
group was 1.5-fold (P < 0.05) higher than that of free ZL006 group. Besides, the results of tissue distribution showed that
the accumulation of ZL006 in brain tissue was significantly improved compared with the free ZL006 group at 1 h time
after intravenous. Anti- ischemic stroke results showed that LPs could significantly enhance neuroprotection of ischemic
stroke on middle cerebral artery occlusion (MCAO) rats model. In conclusion, LPs had been demonstrated to be a
promising drug delivery system for ZL006 to treat ischemic stroke.
Keywords: Liposomes, pharmacodynamics pharmacokinetics, pre-formulation, stroke, tissue distribution.
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