Stable Loading and Delivery of Icaritin Using PEG-PCL Micelles for Effective Treatment of Oral Squamous Cell Carcinoma

Abstract

BACKGROUND: Icaritin can inhibit cell proliferation and induce apoptosis in Oral Squamous Cell Carcinoma (OSCC). However, low solubility limits its clinical usage. OBJECTIVES: To improve the efficacy of icaritin treatment, a micelle system was designed for targeted delivery of drugs to OSCC cells. METHODS: In the present study, the micelles loaded with icaritin were self-assembled from the amphipathic polymer via film dispersion. Nanoparticles were characterized with the transmission electron microscope and dynamic light scattering. The cytotoxicity of icaritin nanoparticles was analyzed by CCK-8, and in vitro target-selective intracellular uptake behaviors were observed using a laser confocal microscope. RESULTS: The micelles were spherical with the mean diameter of 121.2 nm. in vitro studies revealed that icaritin was stablely and slowly released from micelles. Cytotoxicity analysis demonstrated that icartin-loaded micelles exhibited better therapeutic efficacy compared with free icaritin. Cellular uptake and intracellular release results revealed that micelles efficiently delivered icaritin into OSCC cells. CONCLUSION: These results suggest that encapsulated icaritin in polycaprolactone - polyethylene glycol (PCL-PEG) micelles may provide safe and effective drug delivery in OSCC treatments.