The objective of the study was to investigate the cytotoxic and apoptotic effects of Methotrexate (MTX)-loaded chitosan (CS) on LNCaP prostate cancer cell line in vitro. For this purpose, CS nanoparticles (NPs) were synthesized through ionic gelation method and MTX was loaded into the carrier with encapsulation. SEM images of the CS NPs have revealed that they have size of about 85 nm in mono-disperse manner. Drug loading yield was found to be 95.7 % with 470 μg drug/mg NP loading capacity. In vitro drug release study showed that MTX was released in a controlled manner. Cell viability was detected by using trypan blue dye exclusion test and WST-1 cell proliferation assay was performed to show cytotoxic effects of the CS, the MTX and the MTX-loaded NP. IC50 values of CS, MTX and MTX-loaded NPs were assigned from the cell survival plot and were determined as 67.18 μM, 20.21 μM and 2.94 μM at the 72nd hour, respectively. As for apoptosis analysis results, following to MTX-loaded CS treatment of LNCAP cells, apoptotic cell percent was detected as 39.3 % at the 72nd hour, that is, MTX-loaded CS induces 1.85-fold increase in apoptotic cell percent in comparison with that of MTX- induced apoptosis.
Purpose: Gemcitabine is nucleoside analogue and used for various carcinomas like non-small cell lung cancer. Nanoparticle-based therapeutic agents have been developed for use in cancer therapy. Trimethyl chitosan (TMC) is methylated derivative of chitosan. TMC can be preferable because of the limited solubility of chitosan. Magnetic nanoparticles can be concentrated at cancerous tissue which provide targeted cancer therapy. In this study, we tried to develop and compare magnetically targeted trimethyl chitosan and chitosan nanoparticles for gemcitabine delivery in lung cancer therapy.Methods: Chitosan was trimethylated using methyl iodide. Magnetic nanoparticles were synthesized using co-precipitation method. TMC and chitosan nanoparticles were prepared by cross-linking method with tripolyphosphate. Gemcitabine was loaded onto nanoparticles via adsorption technique. After that characterization studies were performed and in vitro drug release tests were carried out. In order to determine cytotoxicites against A549-luc-C8 and CRL5809 cell lines, MTT assays were performed.Results and conclusion: Trimethylation of chitosan was verified with FTIR analysis. Gemcitabine was loaded with 54.7 and 30.3% on magnetic TMC nanoparticles and chitosan nanoparticles, respectively. According to drug release experiments, both carrier system had controlled drug release profile. IC 50 values of gemcitabine loaded magnetic TMC nanoparticles were lower than that of magnetic chitosan nanoparticles. In conclusion, it was suggested that trimethyl chitosan nanoparticles had greater potential than chitosan nanoparticles for further analysis as a magnetically targeted therapy agent for lung cancer.
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