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.