Department of Pharmaceutics, Faculty of Pharmacy, South Valley University, Qena, Egypt.
Department of Pharmacology and Toxicology, Faculty of Pharmacy, South Valley University, Qena, Egypt.
Int J Nanomedicine. 2023 Mar 15;18:1259-1280. doi: 10.2147/IJN.S400604. eCollection 2023.
Ginger extract (GE) has sparked great interest due to its numerous biological benefits. However, it suffers from limited skin permeability, which challenges its transdermal application. The target of the current work was to develop transethosomes as a potential nanovehicle to achieve enhanced transdermal delivery of GE through the skin.
GE-loaded transethosomes were prepared by cold injection using different edge activators. The fabricated nanovesicles were evaluated for particle size, ζ-potential, encapsulation efficiency, and in vitro drug release. The selected formulation was then laden into the hydrogel system and evaluated for ex vivo permeability and in vivo anti-inflammatory activity in a carrageenan-induced rat-paw edema model.
The selected formulation comprised of sodium deoxycholate exhibited particle size of 188.3±7.66 nm, ζ-potential of -38.6±0.08 mV, and encapsulation efficiency of 91.0%±0.24%. The developed transethosomal hydrogel containing hydroxypropyl methylcellulose was homogeneous, pseudoplastic, and demonstrated sustained drug release. Furthermore, it exhibited improved flux (12.61±0.45 μg.cm/second), apparent skin permeability (2.43±0.008×10 cm/second), and skin deposition compared to free GE hydrogel. In vivo testing and histopathological examination revealed that the GE transethosomal hydrogel exhibited significant inhibition of edema swelling compared to free GE hydrogel and ketoprofen gel. The animals that were treated with ginger transethosome hydrogel showed a significant decrement in reactive oxygen species and prostaglandin E compared to untreated animals.
Transethosomes might be a promising new vehicle for GE for effective skin permeation and anti-inflammation. To the best of our knowledge, this work is the first utilization of transethosomes laden into hydrogel as a novel transdermal delivery system of GE.
姜提取物(GE)因其众多的生物学益处而引起了极大的兴趣。然而,它的皮肤渗透性有限,这对其经皮应用提出了挑战。目前的工作目标是开发转脂体作为一种潜在的纳米载体,通过皮肤实现 GE 的增强经皮传递。
使用不同的边缘活性剂通过冷注入法制备载有 GE 的转脂体。对所制备的纳米囊泡进行粒径、ζ-电位、包封效率和体外药物释放的评价。然后将选定的配方载入水凝胶系统,并在角叉菜胶诱导的大鼠足肿胀模型中评价其体外透皮性和体内抗炎活性。
选定的配方包含脱氧胆酸钠,其粒径为 188.3±7.66nm,ζ-电位为-38.6±0.08mV,包封效率为 91.0%±0.24%。含有羟丙基甲基纤维素的开发的转脂体水凝胶是均匀的、假塑性的,并表现出持续的药物释放。此外,与游离 GE 水凝胶相比,它表现出改善的通量(12.61±0.45μg·cm/sec)、表观皮肤渗透性(2.43±0.008×10cm/sec)和皮肤沉积。体内试验和组织病理学检查表明,与游离 GE 水凝胶和酮洛芬凝胶相比,GE 转脂体水凝胶对水肿肿胀具有显著的抑制作用。与未处理的动物相比,用姜转脂体水凝胶处理的动物的活性氧和前列腺素 E 显著减少。
转脂体可能是 GE 经皮渗透和抗炎的有前途的新载体。据我们所知,这是首次将载有转脂体的水凝胶用作 GE 的新型经皮递药系统。