Karkad Amjed Abdullah, Pirković Andrea, Milošević Milena, Stojadinović Bojan, Šavikin Katarina, Marinković Aleksandar, Jovanović Aleksandra A
Faculty of Technology and Metallurgy, University of Belgrade, 11000 Belgrade, Serbia.
Faculty of Medical Technology, Elmergib University, Msallata 7310500, Libya.
Pharmaceutics. 2024 Nov 19;16(11):1476. doi: 10.3390/pharmaceutics16111476.
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.
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.
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.
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.
背景/目的：本研究的目的是开发四种类型的水飞蓟宾脂质体（多层脂质体-MLVs、超声处理的小单层脂质体-SUVs、紫外线照射脂质体和冻干脂质体），并对其进行物理化学表征以及评估它们与皮肤健康益处相关的生物学潜力。
通过测定包封率（EE）、粒径、多分散指数、ζ电位、电导率、迁移率、储存稳定性、密度、表面张力、粘度、傅里叶变换红外光谱（FT-IR）和拉曼光谱进行表征。此外，还测定了对角质形成细胞的细胞毒性以及抗氧化和抗炎潜力。
紫外线照射显著改变了脂质体的流变学和化学性质，并增加了它们的细胞毒性作用。脂质体的冻干导致其包封率和物理特性发生显著变化，降低了它们清除ABTS和DPPH自由基的潜力，并增加了它们降低用细菌脂多糖处理的细胞中白细胞介素1β（IL-1β）表达的潜力。超声处理显著改变了脂质体的包封率以及物理和流变学性质，并略微增加了它们的细胞毒性和对IL-1β的降低作用，而脂质体的抗ABTS和抗DPPH能力显著增加。在储存期间，所有开发的脂质体均呈现出粒径增加和ζ电位（绝对值）降低的趋势。
负载水飞蓟宾的脂质体（MLVs和冻干脂质体）对角质形成细胞显示出有前景的抗氧化活性（针对细胞内产生的活性氧）和抗炎作用（降低巨噬细胞抑制因子表达），并且不会导致其活力发生变化。未来的研究方向将聚焦于在复杂的皮肤疾病、伤口和衰老的细胞模型中，开发的含水飞蓟宾脂质体在伤口愈合、抗衰老及其他方面的潜力。
