Bodnár Krisztina, Papp Boglárka, Sinka Dávid, Fehér Pálma, Ujhelyi Zoltán, Lekli István, Kajtár Richárd, Nacsa Fruzsina, Bácskay Ildikó, Józsa Liza
Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, 4032 Debrecen, Hungary.
Doctoral School of Pharmaceutical Sciences, University of Debrecen, 4032 Debrecen, Hungary.
Pharmaceutics. 2025 Jan 21;17(2):140. doi: 10.3390/pharmaceutics17020140.
BACKGROUND/OBJECTIVES: The present study focused on the formulation and evaluation of novel topical systems containing (sage), emphasizing their antioxidant and anti-inflammatory properties. Sage, rich in carnosol, offers considerable therapeutic potential, yet its low water solubility limits its effectiveness in traditional formulations. The aim of our experimental work was to improve the solubility and thus bioavailability of the active ingredient by developing self-nano/microemulsifying drug delivery systems (SN/MEDDSs) with the help of Labrasol and Labrafil M as the nonionic surfactants, Transcutol HP as the co-surfactant, and isopropyl myristate as the oily phase.
The formulations were characterized for droplet size, zeta potential, polydispersity index (PDI), encapsulation efficacy, and stability. The composition exhibiting the most favorable characteristics, with particle sizes falling within the nanoscale range, was incorporated into a cream and a gel, which were compared for their textural properties, carnosol penetration, biocompatibility and efficacy.
Release studies conducted using Franz diffusion cells demonstrated that the SNEDDS-based cream achieved up to 80% carnosol release, outperforming gels. The 2,2-diphenyl-1-picrylhydrazyl (DPPH) test and enzyme-linked immunosorbent assays (ELISA) showed strong efficacy, with an in vivo carrageenan-induced rat paw edema model revealing that the SNEDDS-based cream significantly reduced inflammation.
These findings highlight the potential of SNEDDS-enhanced topical formulations in improving therapeutic outcomes. Further research is warranted to confirm their long-term safety and efficacy.
背景/目的:本研究聚焦于含鼠尾草的新型局部给药系统的制备与评价,着重考察其抗氧化和抗炎特性。鼠尾草富含鼠尾草酸,具有相当大的治疗潜力,但其低水溶性限制了它在传统制剂中的有效性。我们实验工作的目的是借助Labrasol和Labrafil M作为非离子表面活性剂、Transcutol HP作为助表面活性剂以及肉豆蔻酸异丙酯作为油相,开发自纳米/微乳药物递送系统(SN/MEDDSs),以提高活性成分的溶解度及生物利用度。
对制剂的粒径、zeta电位、多分散指数(PDI)、包封率和稳定性进行表征。将具有最有利特性且粒径处于纳米级范围的组合物加入乳膏和凝胶中,比较它们的质地特性、鼠尾草酸渗透率、生物相容性和功效。
使用Franz扩散池进行的释放研究表明,基于SNEDDS的乳膏实现了高达80%的鼠尾草酸释放,优于凝胶。2,2-二苯基-1-苦基肼基(DPPH)试验和酶联免疫吸附测定(ELISA)显示出强大的功效,在体内角叉菜胶诱导的大鼠足肿胀模型中,基于SNEDDS的乳膏显著减轻了炎症。
这些发现凸显了SNEDDS增强型局部制剂在改善治疗效果方面的潜力。有必要进行进一步研究以确认其长期安全性和有效性。