In this work, nano-levodopa-liposomes (L-dopa-Lip) suspension was prepared by rotary-evaporated film-ultrasonic method, and freeze-drying powders of L-dopa-Lip were also obtained to improve the stability. The products were characterized by TEM, DLS, and TG-DSC, and the phase-transition temperature (T) and encapsulation efficiency were calculated. The brain-targeting and in vitro release of the drug was also studied. The results showed that L-dopa-Lip were well-formed spherical vesicles, and the sizes were about 100 nm, and the encapsulation efficiency was higher than 90%. The drug release temperature of L-dopa-Lip was 68 °C, and the in vitro release property and mathematical model were also studied. The brain targeting of L-dopa-Lip in vivo was explored by injecting the gold nanoparticles (AuNPs) labeled L-dopa-Lip (AuNPs-L-dopa-Lip) through the tail vein. ICP-MS and TEM showed that L-dopa-Lip had brain targeting, suggesting the potential treatment of L-dopa-Lip on brain dysfunction. The results of this work might be helpful for designing drug-loaded liposomes for the treatment of central nervous system (CNS) diseases and monitoring their distributions in vivo.
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