Sevilla, España
Δ9-tetrahydrocannabinol (Δ9-THC) is known for its antitumor activity and palliative effects. However, its unfavorable physicochemical and biopharmaceutical properties, including low bioavailability, psychotropic side effects and resistance mechanisms associated to dosing make mandatory the development of successful drug delivery systems. In this work, several steps forward were taken by including a targeting ligand and a multifunctional fluorescent labeling strategy in the presented approach. Transferrin (Tf), a targeting moiety for cancer cells based on a higher expression of the Tf receptor in tumor cells , was coupled to Δ9-THC-loded PLGA NPs to modulate the interaction of the particles with the target cells. In addition, a double fluorescent labeling of the formulations, both through chemical linkage to the polymer and through dye encapsulation, was performed in order to selectively track the internalization pathway and intracellular fate of both the carrier and the cargo. The resulting formulations were evaluated in order to correlate the modulation of their anticancer effect with their cell internalization mechanics.
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