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

This study demonstrates a simple method for preparation of size-tunable oil-based nanotherapeutics by high-pressure homogenization, and also sheds light on the application in future clinical cancer therapy. • Size-tunable GLSO@NEs has been simply prepared by high-pressure homogenization to achieve enhanced therapeutic effect. • GLSO@NEs could perform superior anti-metastasis and anti-cancer activity. • Nanotechnology increases traditional Chinese medicine preparations with better efficacy. 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 GLSO@NEs on MGC803 cancer cells significantly enhanced, thanks to the improved cellular uptake and retention efficacy of GLSO@NEs. In addition, middle-sized 40 nm-GLSO@NEs performed superior permeability across Caco-2 intestinal absorption barrier to improve internalized quantity of GLSO. More importantly, GLSO@NEs could effectively prevent cell migration and invasion, simultaneously activating caspase activity to trigger cell death. Interestingly, middle size of 40 nm-GLSO@NEs performed superior accumulation efficacy in cells. Ultimately, 40 nm-GLSO@NEs 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. [ABSTRACT FROM AUTHOR]