Despite its potent in vitro anti-cancer activity, the vitamin E extract tocotrienol
has its therapeutic potential hampered by its poor bioavailability and by its inability to reach
tumors in a specific way after intravenous administration. One possibility to overcome this
issue would be to entrap tocotrienol within vesicles bearing transferrin, whose receptors are
present in abundance on many cancer cell types. In this study, we demonstrated that the systemic
administration of tocotrienol entrapped within transferrin-bearing vesicles led to tumor
suppression of 20% of A431 epidermoid carcinoma tumors and 50% of B16-F10 melanoma tumors at the
end of the treatment. The survival of animals treated with these vesicles was improved by more than 20 days
in comparison with the controls, for the two cancer models tested. Animals did not show any secondary effects
following administration of the treatment. The entrapment of tocotrienol within transferrin-bearing vesicles
is therefore a promising therapeutic strategy, which could result in tumor suppression after systemic administration
of this delivery system.
Keywords: Cancer therapy, delivery system, in vivo, tocotrienol, transferrin, tumor targeting.
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