Design, Synthesis, Characterization, and Evaluation of the Anti-HT-29 Colorectal Cell Line Activity of Novel 8-Oxyquinolinate-Platinum(II)-Loaded Nanostructured Lipid Carriers Targeted with Riboflavin

BOZTEPE, T.; SCIOLI-MONTOTO, S.; GAMBARO R.; RUIZ, M. E.; CABRERA S; ALEMAN J; ISLAN, G.A.; CASTRO GR; LEON I.E

Pharmaceutics

AMER CHEMICAL SOC

Lugar: Washington; Año: 2023

1999-4923

Abstract: Colorectal cancer is occasionally called colon or rectal cancer, depending on where cancerbegins to form, and is the second leading cause of cancer death among both men and women.The platinum-based [PtCl(8-O-quinolinate)(dmso)] (8-QO-Pt) compound has demonstrated encouraginganticancer activity. Three different systems of 8-QO-Pt-encapsulated nanostructured lipid carriers(NLCs) with riboflavin (RFV) were investigated. NLCs of myristyl myristate were synthesized byultrasonication in the presence of RFV. RFV-decorated nanoparticles displayed a spherical shape anda narrow size dispersion in the range of 144–175 nm mean particle diameter. The 8-QO-Pt-loadedformulations of NLC/RFV with more than 70% encapsulation efficiency showed sustained in vitrorelease for 24 h. Cytotoxicity, cell uptake, and apoptosis were evaluated in the HT-29 human colorectaladenocarcinoma cell line. The results revealed that 8-QO-Pt-loaded formulations of NLC/RFVshowed higher cytotoxicity than the free 8-QO-Pt compound at 5.0 M. All three systems exhibiteddifferent levels of cellular internalization. Moreover, the hemotoxicity assay showed the safety profileof the formulations (less than 3.7%). Taken together, RFV-targeted NLC systems for drug deliveryhave been investigated for the first time in our study and the results are promising for the future ofchemotherapy in colon cancer treatment.