Innovative Drug Delivery System in Lung Cancer: Combining Quantum Dots and TKIs
Posted: Monday, June 17, 2019
To improve outcomes for patients with non–small cell lung cancer, researchers are studying a novel delivery system that may aid in both the diagnosis and treatment of this type of cancer. According to research published in the European Journal of Pharmaceutical Sciences, the tyrosine kinase inhibitor (TKI) erlotinib may prove to be more effective at tumor detection when it is conjugated with quantum dots (QDs), a multifunctional delivery system using photoluminescent nanoparticles.
“This study, being one of its kind, explores the feasibility of conjugating OSI-420 [active metabolite of erlotinib] with QDs as an alternative to traditional anti-cancer therapy, by improving intracellular drug delivery,” noted Vivek Gupta, PhD, of the College of Pharmacy and Health Sicences at St. John’s University in Queens, New York, and colleagues.
The study focused specifically on conjugating the active metabolite of erlotinib—desmethyl erlotinib (OSI-420)—which has anticancer properties similar to erlotinib. To create a delivery system, OSI-420 was conjugated to QDs and then identified by several characteristics, including particle size, zeta potential, and fluorescence spectroscopy. Ultraviolet visible spectroscopy was used to determine the drug-loading capacity (52.2 ± 7.5%). Cellular uptake and cellular recovery studies evaluated the internalization potential of QD-OSI-420.
Via cell viability studies, QD-OSI-420 conjugates were found to have significantly higher efficacy than erlotinib or OSI-420 alone in all tested cell lines. QD-OSI-420 showed an IC60 of 2.5 μM in A549 cell lines, which are erlotinib-resistant, whereas neither erlotinib nor OSI-420 exhibited 60% inhibition up to 20 μM. In addition, a three-dimensional SCC model of A549 cell lines showed that QD-OSI-420 was markedly more effective at reducing in-vitro 3D tumor volume when compared to erlotinib or OSI-420 alone.
Disclosure: The study authors’ disclosure information may be found at sciencedirect.com.