Preparation, characterisation andin vitrocytotoxicity studies of chelerythrine-loaded magnetic Fe₃O₄@O-carboxymethylchitosan nanoparticles

Abstract

In this work, a novel, active tumour-targeting system (Fe 3 O 4 @OCMCS-CHE) was designed by surface-modifying superparamagnetic iron oxide nanoparticles (Fe 3 O 4 ) with O-carboxymethylchitosan (OCMCS) to improve their biocompatibility and ability to target specific tumour cells. The chelerythrine (CHE) was used as the model of anti-tumour drug in this system. The optimised formulation was characterised and confirmed by scanning electron microscopy (SEM), transmission electron microscope (TEM), vibrating sample magnetometer (VSM), Xray diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR), in vitro drug release and so on. It was found that the synthesised nanoparticles were spherical in shape with an average size of 60 nm, the drug loading content and entrapment efficiency were 8.32 AE 0.25% (w/w) and 90.65 AE 0.46% (w/w), respectively, and the saturated magnetisation reached 27.06 emu/g. The in vitro drugrelease behaviour from nanoparticles displayed a biphasic drug-release pattern with initial burst release and consequently sustained release. Also, the effect of magnetic targeted nanoparticles on the proliferation of human hepatoma cell line (HepG2) in vitro was investigated. The results from 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) and Hochest assays suggested that the Fe 3 O 4 @OCMCS-CHE nanoparticles could effectively inhibit the proliferation of HepG2 cells, which displayed time-dependent and concentration-dependent manner. All these results indicated that the multifunctional Fe 3 O 4 @OCMCS nanoparticles possess a high drug loading efficiency, have low cytotoxicity, and are promising candidates for targeted drug delivery.

Targeted delivery of silibinin via magnetic niosomal nanoparticles: potential application in treatment of colon cancer cells

“…Thus, nanocarriers can increase the cell cytotoxicity of the drug against HT-29 cells, and there is a dose-dependent and relatively time-dependent manner regarding using complex. These results confirm the previous studies reported that the cytotoxicity of the drug-loaded MNNPs follows dose-dependent and time-dependent trends ( Huang et al, 2015 ; Dhavale et al, 2021 ). The IC50 of the MNNPs complex was observed at 40 μg/mL within 48 h, therefore this concentration was considered for the following tests.…”

Optimization of a novel chelerythrine-loaded magnetic Fe3O4/chitosan alpha-ketoglutaric acid system and evaluation of its anti-tumour activities

“…It showed that higher drug loading content was achieved when the microparticles were obtained at lower ultrasonic time for higher oil/water ratio. The drug loading content of this nanoparticles was much higher than that of Fe3O4@O‐carboxymethyl chitosan nanoparticles …”