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Poor medication solubility, low bioavailability, systemic toxicity, and lack of target specificity are frequently barriers to cancer treatment. A second-generation tyrosine kinase inhibitor with strong antitumor effects, nilotinib has inconsistent pharmacokinetics and poor water solubility. The goal of the current study was to create carbon dot-based nanocarriers functionalized with folic acid for better Nilotinib distribution and therapeutic efficacy. To create NF1– NF9 formulations, carbon dots were effectively synthesized, functionalized with folic acid, and loaded with nilotinib. Good colloidal stability was indicated by dynamic light scattering analysis, which verified nanoscale particle sizes between 6.22 and 12.3 nm, low polydispersity indices (0.121–0.394), and negative zeta potential values (–14.5 to – 25.2 mV). Because of its highest drug concentration (96.37%), maximum encapsulation efficiency (88.27%), and smallest particle size (6.22 nm), NF5 was determined to be the optimal formulation. Successful drug encapsulation and drug integrity preservation were verified by FTIR and UV–visible spectroscopy. The results of SEM and TEM investigations showed spherical, evenly distributed nanoparticles with a smooth shape and little agglomeration. While XRD studies demonstrated partial to complete amorphization of Nilotinib within the carbon dot matrix, favoring improved dissolution, DSC analysis revealed an endothermic peak at about 238.31 °C, suggesting the creation of a new crystalline or co-crystal phase. The structural integrity was confirmed by Raman spectroscopy, which revealed distinctive Nilotinib peaks at around 1648, 1611, 1446, and 1308 cm⁻¹. According to in vitro release experiments, NF5 achieved 96.92% release in 12 hours, demonstrating sustained drug release. Studies on A549 cells' cytotoxicity showed that NF5 had more anticancer activity than pure nilotinib. Apoptotic cell death was confirmed by fluorescence imaging with Hoechst 33342 and Calcein-AM. All things considered, folic acid-functionalized carbon dots loaded with nilotinib are a promising nanocarrier technology for theranostic and targeted anticancer treatments.
Published in: International Journal of Drug Delivery Technology
Volume 16, Issue 8s