ENCAPSULATION IN NANOSTRUCTURED LIPID CARRIERS ENABLES CONTROLLED RELEASE AND ENHANCES ANTITUMOR ACTIVITY OF GREEN PROPOLIS DERIVATIVES

Nanostructured lipid carriers (NLCs) have been investigated as promising systems to improve the solubility and bioavailability of hydrophobic bioactive compounds. Green propolis extract (PROP) and Artepillin C (ARTC) present recognized therapeutic activities, including antitumor properties, but their clinical application is limited by poor aqueous solubility. The aim of this study was to develop and characterize PROP- and ARTC-loaded NLCs, evaluating physicochemical parameters, release profile, and biological effects in comparison with the free compounds. The formulations were prepared by emulsification–ultrasonication using solid and liquid lipids combined with a surfactant. The obtained particles showed an average diameter between 110 and 130 nm, PDI < 0.200, zeta potential around -12 mV, encapsulation efficiency close to 100%, and stability maintained for up to 190 days. Preliminary in vitro release studies using a dialysis bag demonstrated a controlled release profile, while the free compounds exhibited rapid release, confirming the ability of NLCs to prolong drug availability. Cell viability assays (MTT) performed on human melanoma cells (A375) showed that the nanoencapsulated formulations exhibited greater cytotoxic effect in the cell line when compared to the free compounds, indicating that lower doses of encapsulated formulations already produce a potentiated effect. In conclusion, the developed NLCs displayed robust physicochemical performance, sustained release profile, and superior biological effects, consolidating themselves as promising systems for biomedical application of green propolis derivatives.

Acknowledgments: CAPES, FAPESP and CNPq (311368/2022-0).