TY  - JOUR
TI  - In vitro hepatotoxicity evaluation of methotrexate-loaded niosome formulation: fabrication, characterization and cell culture studies
AB  - Background/aim: Methotrexate (MTX) is a folic acid antagonist that is widely used to treat osteosarcoma, leukemia, breast cancer, and autoimmune and inflammatory diseases. The most important concerns with MTX are its poor solubility and high toxicity, particularly in liver cells. To enhance its solubility and to minimize its toxicity, we encapsulated MTX in niosomes and investigated its hepatotoxicity mechanisms using genetic biomarkers. Materials and methods: Niosomes were successfully prepared using a modified thin film method, and the prepared monodisperse small- sized formulation was subsequently characterized. In vitro cytotoxicity studies were performed both in hepatocarcinoma (HEP3G) and healthy liver (AML12) cell lines. Specifically, immunofluorescence assay and evaluation of the expression levels of apoptotic, antioxidant, heat shock protein, and oxidative stress genes were performed. Results: The formulation had a particle size of 117.1 ± 33 nm, a surface charge of −38.41 ± 0.7 mV, and an encapsulation efficiency of 59.7% ± 2.3%. The results showed that the niosomal formulation exhibited significantly higher cytotoxic effects in HEP3G than in AML12. The immunofluorescence and genetic analyses showed that the increased cytotoxicity of niosomes resulted mainly from oxidative stress and slight apoptosis. Conclusion: These results demonstrated that niosomal drug delivery systems could be a new potential formulation for minimizing MTX-related hepatotoxicity.
AU  - Ergin, Ahmet Doğan
AU  - Oltulu, Cagatay
AU  - TÜRKER, N.Pelin
AU  - DEMİRBOLAT, Gulen Melike
DO  - 10.55730/1300-0144.5651
PY  - 2023
JO  - Turkish Journal of Medical Sciences
VL  - 53
IS  - 4
SN  - 1300-0144
SP  - 872
EP  - 882
DB  - TRDizin
UR  - http://search/yayin/detay/1194018
ER  -