Background: Drug delivery to the brain tumor is limited due to the presence of the
blood-brain barrier (BBB).
Objective: This study aimed to evaluate the therapeutic effects of cisplatin-loaded PEGylated liposomes,
targeted with the OX26 antibody (targeted liposomal cisplatin) against transferrin receptor
expressing rat glioma C6 cells in vitro.
Methods: The liposomes were synthesized using reverse phase evaporation method and were conjugated
to the OX26 monoclonal antibody. They were characterized in terms of size, drug encapsulation
efficiency, morphology and drug release experiments using dynamic light scattering, atomic
absorption spectrometry, scanning electron microscopy, and dialysis membrane methods. Then,
their biological activities were evaluated on targeting the BBB.
Results and Discussion: The characterization results showed that spherical nanodrug with a size of
157 nm and drug loading efficiency of 24% was synthesized, which released 64% of the loaded cisplatin
after 72 h in a controlled release manner. The nanoparticles caused an increase in the cisplatin
cytotoxicity effects by 1.7-, 1.8- and 1.8-fold, compared to cisplatin-loaded PEGylated liposomes
(liposomal cisplatin) after 24, 48 and 72h incubation, respectively against C6 cells. Moreover, targeted
liposomal cisplatin showed promising results in the transport of cisplatin across the BBB, in
which it caused an increase in the cisplatin cytotoxicity on C6 cells by 2.7- and 2.4-fold, compared
to cisplatin and liposomal cisplatin, respectively.
Conclusion: Regarding the properties of the targeted liposomal cisplatin, it suggests that the potency
of the formulation, to be evaluated, for the transport of cisplatin across the BBB, delivers it to the
brain tumor in vivo.