Tsichlis Ioannis, Manou Athanasia-Paraskevi, Manolopoulou Vasiliki, Matskou Konstantina, Chountoulesi Maria, Pletsa Vasiliki, Xenakis Aristotelis, Demetzos Costas
Section of Pharmaceutical Technology, Department of Pharmacy, School of Health Sciences, National and Kapodistrian University of Athens, Panepistimioupolis Zografou, 15771 Athens, Greece.
Institute of Chemical Biology, National Hellenic Research Foundation, 48 Vassileos Constantinou Avenue, 11635 Athens, Greece.
Materials (Basel). 2023 Aug 8;16(16):5509. doi: 10.3390/ma16165509.
The aim of the present study is the development, physicochemical characterization, and in vitro cytotoxicity evaluation of both empty and quercetin-loaded HSPC (hydrogenated soy phosphatidylcholine) liposomes, GMO (glyceryl monooleate) liquid crystalline nanoparticles, and PHYT (phytantriol) liquid crystalline nanoparticles. Specifically, HSPC phospholipids were mixed with different non-ionic surfactant molecules (Tween 80 and/or Span 80) for liposomal formulations, whereas both GMO and PHYT lipids were mixed with Span 80 and Tween 80 as alternative stabilizers, as well as with Poloxamer P407 in different ratios for liquid crystalline formulations. Subsequently, their physicochemical properties, such as size, size distribution, and ζ-potential were assessed by the dynamic and electrophoretic light scattering (DLS/ELS) techniques in both aqueous and biological medium with serum proteins. The in vitro biological evaluation of the empty nanosystems was performed by using the MTT cell viability and proliferation assay. Finally, the entrapment efficiency of quercetin was calculated and the differences between the two different categories of lipidic nanoparticles were highlighted. According to the results, the incorporation of the non-ionic surfactants yields a successful stabilization and physicochemical stability of both liposomal and liquid crystalline nanoparticles. Moreover, in combination with an appropriate biosafety in vitro profile, increased encapsulation efficiency of quercetin was achieved. Overall, the addition of surfactants improved the nanosystem's stealth properties. In conclusion, the results indicate that the physicochemical properties were strictly affected by the formulation parameters, such as the type of surfactant.
本研究的目的是对空白和载有槲皮素的氢化大豆磷脂酰胆碱（HSPC）脂质体、甘油单油酸酯（GMO）液晶纳米粒和植烷三醇（PHYT）液晶纳米粒进行开发、理化特性表征及体外细胞毒性评估。具体而言，将HSPC磷脂与不同的非离子表面活性剂分子（吐温80和/或司盘80）混合用于脂质体制剂，而将GMO和PHYT脂质与司盘80和吐温80作为替代稳定剂混合，以及与泊洛沙姆P407以不同比例混合用于液晶体制剂。随后，通过动态和电泳光散射（DLS/ELS）技术在含有血清蛋白的水性和生物介质中评估它们的理化性质，如尺寸、尺寸分布和ζ电位。通过MTT细胞活力和增殖测定对空白纳米系统进行体外生物学评估。最后，计算槲皮素的包封率，并突出两种不同类型脂质纳米粒之间的差异。根据结果，非离子表面活性剂的加入使脂质体和液晶纳米粒都成功实现了稳定化和理化稳定性。此外，结合适当的体外生物安全性，槲皮素的包封效率有所提高。总体而言，表面活性剂的加入改善了纳米系统的隐身性能。总之，结果表明理化性质受到制剂参数（如表面活性剂类型）的严格影响。
