High-pressure homogenization and tailoring of size-tunable Ganoderma lucidum spore oil nanosystem for enhanced anticancer therapy

Ganoderma lucidum spore oil (GLSO) has been long practiced and widely recognized as a healthy food composite performing potential anticancer and antioxidant activity. However, its further application might be limited by the native poorly soluble and instable properties. Herein, size-tunable GLSO nanosystems have been designed and tailored to three sizes of particles at 20 nm, 40 nm and 80 nm by high-pressure homogenization, for achieving robust therapeutic effect against cancer cells. As expected, toxicity of biocompatible different-sized [email protected] on MGC803 cancer cells significantly enhanced, thanks to the improved cellular uptake and retention efficacy of [email protected] In addition, middle-sized 40  [email protected] performed superior permeability across Caco-2 intestinal absorption barrier to improve internalized quantity of GLSO. More importantly, [email protected] could effectively prevent cell migration and invasion, simultaneously activating caspase activity to trigger cell death. Interestingly, middle size of 40  [email protected] performed superior accumulation efficacy in cells. Ultimately, 40  [email protected] showed potent suppression effect on tumors in vivo , effectively reversing liver and kidney damage induced by cancer, which was accompanied with no obvious toxicity and side effects during treatment. Therefore, this study not only provides a simple method for preparation of GLSO-like traditionally functional composite by high-pressure homogenization, but also sheds light on the application in future clinical cancer therapy.