Faculty of Pharmacy, University of Coimbra, Pólo das Ciências da Saúde, Azinhaga de Santa Comba, 3000-548 Coimbra, Portugal; Coimbra Chemistry Centre, Department of Chemistry, University of Coimbra, Coimbra, Portugal.
Faculty of Pharmacy, University of Coimbra, Pólo das Ciências da Saúde, Azinhaga de Santa Comba, 3000-548 Coimbra, Portugal; Centre for Neurosciences and Cell Biology (CNC), University of Coimbra, Rua Larga, Faculty of Medicine, Pólo I, 1st floor, 3004-504 Coimbra, Portugal.
Mater Sci Eng C Mater Biol Appl. 2019 Oct;103:109804. doi: 10.1016/j.msec.2019.109804. Epub 2019 May 30.
The therapeutic potential of essential oils is widely recognized since antiquity, due to their antibacterial, antifungal, anti-inflammatory and immuno-modulatory properties. In particular, their physicochemical characteristics, such as lipophilicity and permeation enhancement effect have sparked attention for the development of innovative lipid nanosystems. The present work aimed at developing a differentiated nanostructured lipid carrier (NLC) based formulation for topical application, using the Ridolfia segetum essential oil (REO), isolated by hydrodistillation from this Portuguese aromatic plant, with a dual key function, as active and simultaneously nanostructuring component of the nanoparticles. The incorporation of the essential oil in the solid lipid matrix, followed by the respective hot high-pressure homogenization, led to particles with a size of 143 ± 5 nm, along with a polydispersity index of 0.21, a zeta potential of -16.3 ± 0.6 mV, encapsulation efficacy of ca. 100% and loading capacity of 1.4%. A comprehensive physicochemical characterization of the lipid nanosystem, including morphology, structural, thermal and accelerated stability analysis confirmed its nanostructured nature. REO-NLC was further jellified for designing an appropriate semisolid topical dosage form. In vitro release, permeation and skin retention studies evidenced a sustained release behaviour and a reservoir-like effect, suitable for a prolonged topical delivery. Cytotoxicity studies, performed in fibroblasts and keratinocytes, revealed the biocompatibility of the developed formulations. This work highlights the critical role of REO as a multiaddressable compound, both as active pharmaceutical ingredient and nanostructuring agent, able to tailor the permeation enhancement profile of nanoparticles towards topical delivery purposes and concomitantly presenting a safety profile for cosmetic and/or pharmaceutical purposes.
由于具有抗菌、抗真菌、抗炎和免疫调节特性,精油的治疗潜力从古至今都得到广泛认可。特别是,其物理化学特性,如亲脂性和渗透增强作用,引起了人们对开发创新脂质纳米系统的关注。本工作旨在开发一种基于差异的纳米结构化脂质载体(NLC)的局部应用制剂,使用从这种葡萄牙芳香植物中通过水蒸气蒸馏分离得到的 Ridolfia segetum 精油(REO),其具有双重关键功能,既是活性成分,同时也是纳米颗粒的结构化成分。将精油掺入固体脂质基质中,然后进行相应的热高压匀化,得到粒径为 143±5nm、多分散指数为 0.21、Zeta 电位为-16.3±0.6mV、包封效率约为 100%和载药量为 1.4%的颗粒。对脂质纳米系统进行了全面的物理化学特性表征,包括形态、结构、热和加速稳定性分析,证实了其纳米结构的性质。REO-NLC 进一步凝胶化,用于设计合适的半固体局部剂型。体外释放、渗透和皮肤保留研究表明,具有持续释放行为和储库样效应,适用于延长局部递送。在成纤维细胞和角质细胞中进行的细胞毒性研究表明,所开发的制剂具有生物相容性。这项工作强调了 REO 作为一种多用途化合物的关键作用,既是活性药物成分,又是结构化剂,能够针对局部递送目的调整纳米颗粒的渗透增强特性,同时呈现出适用于化妆品和/或制药目的的安全性特征。