In vitro assessment of transferrin-conjugated liposomes as drug delivery systems for inhalation therapy of lung cancer

Investigators developing an inhalable nanoparticle for treating lung cancer have shown that a surface molecule found on malignant lung cells can serve as an effective target for improving drug delivery.

The research team, led by Carsten Ehrhardt, Ph.D., of the University of Dublin, has published its results in the European Journal of Pharmaceutical Sciences.

Aiming to improve the performance of a nanoparticle formulation of the drug doxorubicin, the investigators decided to target a cell surface protein known as the transferrin receptor, which is involved in satisfying cellular demands for iron. To determine if this receptor was a suitable target, the researchers first quantified levels of the transferrin receptor on malignant and healthy lung epithelial cells. Their results showed clearly that malignant cells possessed far higher levels of this protein than did their healthy counterparts.

Next, the investigators prepared lipid-based, doxorubicin-loaded nanoparticles decorated with the molecule transferrin. When they compared cell uptake of these targeted nanoparticles with that of nanoparticles lacking transferrin, the researchers found that uptake of the targeted nanoparticles was far greater. More importantly, the targeted nanoparticles were far more toxic to malignant cells than were the untargeted nanoparticles. In addition, the targeted nanoparticles were more toxic to malignant cells than they were to healthy cells, suggesting that targeting the transferrin receptor could prove to be an effective means of improving the ability of anticancer nanoparticles to deliver drug specifically to tumor cells.

This work is detailed in a paper titled, “In vitro assessment of transferrin-conjugated liposomes as drug delivery systems for inhalation therapy of lung cancer.” Investigators from Saarland University, Philipps University, and the Völklingen Heart Centre, all in Germany, also participated in this study. This paper was published online in advance of print publication. An abstract of this paper is available through PubMed. View abstract.


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