Department of Chemical and Pharmaceutical Sciences, School of Life Sciences, Pharmacy and Chemistry, Kingston University, London, KT1 2EE, UK.
Department of Applied Pharmaceutical Sciences and Clinical Pharmacy, Faculty of Pharmacy, Isra University, Amman, 11622, Jordan.
AAPS PharmSciTech. 2024 Mar 27;25(4):69. doi: 10.1208/s12249-024-02781-2.
Thymoquinone (TQ) is a phytochemical compound present in Nigella sativa and has potential benefits for treating dermatological conditions such as psoriasis. However, its clinical use is limited due to its restricted bioavailability, caused mainly by its low solubility and permeability. To overcome this, a new transdermal drug delivery system is required. Nanoparticles are known to enhance material solubility and permeability, and hence, this study aimed to synthesize TQ-loaded L-arginine-based polyamide (TQ/Arg PA) nanocapsules incorporated into transdermal patches for prolonged delivery of TQ. To achieve this, Eudragit E polymer, plasticizers, and aloe vera as penetration enhancer were used to develop the transdermal patch. Furthermore, novel TQ/Arg-PA was synthesized via interfacial polymerization, and the resultant nanocapsules (NCs) were incorporated into the matrix transdermal patch. The Arg-PA NCs' structure was confirmed via NMR and FTIR, and optimal TQ/Arg-PA NCs containing formulation showed high entrapment efficiency of TQ (99.60%). Molecular and thermal profiling of TQ/Arg-PA and the transdermal patch revealed the effective development of spherical NCs with an average particle size of 129.23 ± 18.22 nm. Using Franz diffusion cells and synthetic membrane (STRAT M®), the in vitro permeation profile of the prepared patches demonstrated an extended release of TQ over 24 h, with enhanced permeation by 42.64% when aloe vera was employed. In conclusion, the produced formulation has a potential substitute for corticosteroids and other drugs commonly used to treat psoriasis due to its effectiveness, safety, and lack of the side effects typically associated with other drugs.
姜酮（TQ）是一种存在于黑种草中的植物化学物质，具有治疗银屑病等皮肤病的潜力。然而，由于其生物利用度低，主要是由于其溶解度和渗透性低，其临床应用受到限制。为了克服这一问题，需要一种新的经皮药物传递系统。纳米粒子已知可以提高物质的溶解度和渗透性，因此，本研究旨在合成负载姜酮的 L-精氨酸基聚酰胺（TQ/Arg PA）纳米胶囊，并将其纳入经皮贴剂中，以延长 TQ 的递送。为了实现这一目标，使用 Eudragit E 聚合物、增塑剂和芦荟作为渗透增强剂来开发经皮贴剂。此外，通过界面聚合合成了新型 TQ/Arg-PA，将所得纳米胶囊（NCs）纳入基质经皮贴剂中。通过 NMR 和 FTIR 确认了 Arg-PA NCs 的结构，最佳的 TQ/Arg-PA NCs 包含制剂显示出 TQ 的高包封效率（99.60%）。TQ/Arg-PA 和经皮贴剂的分子和热分析表明，有效开发了具有 129.23±18.22nm 平均粒径的球形 NCs。使用 Franz 扩散池和合成膜（STRAT M®），制备的贴剂的体外渗透曲线表明，TQ 在 24 小时内持续释放，当使用芦荟时，渗透增强了 42.64%。总之，由于其有效性、安全性和缺乏与其他药物相关的副作用，该制剂具有成为治疗银屑病的皮质类固醇和其他药物的潜在替代品的潜力。
