Mannosylated Solid Lipid Nanocarriers of Chrysin to Target Gastric Cancer: Optimization and Cell Line Study

Despite significant biological effects, the clinical use of chrysin has been restricted because of its poor oral bioavailability.

The purpose of the present research was to investigate the targeting potential of Mannose decorated chrysin (5,7- dihydroxyflavone) loaded solid lipid nanocarrier (MC-SLNs) for gastric cancer.

The Chrysin loaded SLNs (C-SLNs) were developed, optimized, characterized and further mannosylated. The C-SLNs were developed with a high shear homogenizer, optimized with 32 full factorial designs and characterized by Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), X-Ray Diffraction (XRD) and Scanning Electron Microscope (SEM) and evaluated for particle size/polydispersity index, zeta-potential, entrapment efficiency, % release and haemolytic toxicity. The ex-vivo cytotoxicity study was performed on gastric cancer (ACG) and normal cell lines.

DSC and XRD data predict the chrysin encapsulation in the lipid core and FTIR results confirm the mannosylation of C-SLNs. The optimized C-SLNs exhibited a narrow size distribution with a particle size of 285.65 nm. The % Entrapment Efficiency (%EE) and % controlled release were found to be 74.43% and 64.83%. Once C-SLNs were coated with mannose, profound change was observed in a dependent variable - an increase in the particle size of MC-SLNs (307.1 nm) was observed with 62.87% release and 70.8% entrapment efficiency. Further, the in vitro studies depicted MC- SLNs to be least hemolytic than pure chrysin and C-SLNs. MC-SLNs were most cytotoxic and were preferably taken up ACG tumor cells as evaluated against C-SLNs.

These data suggested that the MC-SLNs demonstrated better biocompatibility and targeting efficiency to treat gastric cancer.