Title:Stable Loading and Delivery of Icaritin Using PEG-PCL Micelles for Effective Treatment of Oral Squamous Cell Carcinoma
Volume: 18
Issue: 7
Author(s): Jian-Guang Yang, Jing Zhang, Xiao-Jie Chen and Gang Zhou*
Affiliation:
- The State Key Laboratory Breeding Base of Basic Science of Stomatology (Hubei-MOST) and Key Laboratory of Oral Biomedicine Ministry of Education, School and Hospital of Stomatology, Wuhan University, Wuhan,China
Keywords:
Drug delivery, icaritin, micelles, oral squamous cell carcinoma, PEG, PCL.
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.