Silibinin-Loaded Liposomes: The Influence of Modifications on Physicochemical Characteristics, Stability, and Bioactivity Associated with Dermal Application.

BACKGROUND/OBJECTIVES: The aims of the presented study were the development of four types of silibinin-loaded liposomes (multilamellar liposomes-MLVs, sonicated small unilamellar liposomes-SUVs, UV-irradiated liposomes, and lyophilized liposomes) and their physicochemical characterization and biological potential related to skin health benefits.

METHODS

The characterization was performed via the determination of the encapsulation efficiency (EE), particle size, polydispersity index, zeta potential, conductivity, mobility, storage stability, density, surface tension, viscosity, FT-IR, and Raman spectra. In addition, cytotoxicity on the keratinocytes and antioxidant and anti-inflammatory potential were also determined.

RESULTS

UV irradiation significantly changed the rheological and chemical properties of the liposomes and increased their cytotoxic effect. The lyophilization of the liposomes caused significant changes in their EE and physical characteristics, decreased their ABTS and DPPH radical scavenging potential, and increased their potential to reduce the expression of interleukin 1 beta (IL-1β) in cells treated with bacterial lipopolysaccharide. Sonication significantly changed the EE and physical and rheological properties of the liposomes, and slightly increased their cytotoxicity and reduction effect on IL-1β, while the anti-ABTS and anti-DPPH capacity of the liposomes significantly increased. All developed liposomes showed an increasing trend in particle size and a decreasing trend in zeta potential (absolute values) during storage.

CONCLUSIONS

Silibinin-loaded liposomes (MLVs and lyophilized) showed promising antioxidant activity (toward reactive oxygen species generated in cells) and anti-inflammatory effects (reducing macrophage inhibitory factor expression) on keratinocytes and did not lead to a change in their viability. Future perspectives will focus on wound healing, anti-aging, and other potential of developed liposomes with silibinin in sophisticated cell-based models of skin diseases, wounds, and aging.