Ligustrazine-Loaded Borneol Liposome Alleviates Cerebral Ischemia-Reperfusion Injury in Rats.

Our team's pharmacological and clinical trials proved that ligustrazine/borneol spray had a definite effect on ischemic stroke (IS). To solve the shortcomings of ligustrazine/borneol spray, such as low bioavailability, short half-life, and poor compatibility between borneol and ligustrazine, ligustrazine-loaded borneol liposomes (LIP@TMP) were successfully prepared by a thin-film ultrasonication method. The average particle size of LIP@TMP was 282.4 ± 3.6 nm, the drug loading rate was 14.5 ± 0.6%, and the entrapment efficiency was 42.7 ± 1.0%, which had excellent stability and sustained release ability. In addition, live/dead fluorescent staining and the CCK-8 test confirmed that LIP@TMP had good biocompatibility. Moreover, middle cerebral artery occlusion (MCAO) rat model experiments further demonstrated that LIP@TMP could significantly alleviate cerebral ischemia and reperfusion injury by improving neurological scores, reducing cerebral infarct volume, promoting neurogenesis, inhibiting inflammation, and reducing tissue damage. In addition, LIP@TMP enhanced neuronal marker doublecortin (DCX) and neuronal nuclei (NEUN), inhibited inflammatory factors (TNF-α and IL-1β), and reduced apoptosis signal molecules (TUNEL and caspase-3). The findings of this study suggested that the prepared LIP@TMP had tremendous potential for the treatment of cerebral ischemia.