AAPS PharmSciTech ( IF 3.4 ) Pub Date : 2024-03-27 , DOI: 10.1208/s12249-024-02781-2 Eman Zmaily Dahmash 1 , Lama Murad Attiany 2 , Dalia Ali 3 , Shereen M Assaf 4 , Jamal Alkrad 2 , Hamad Alyami 5
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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.
Graphical Abstract
中文翻译：
使用新型百里醌-L-精氨酸聚酰胺纳米胶囊开发和表征透皮贴剂，用于治疗银屑病
百里醌 (TQ) 是存在于黑种草中的一种植物化学化合物，对治疗牛皮癣等皮肤病具有潜在益处。然而，由于其生物利用度有限，其临床应用受到限制，这主要是由于其溶解度和渗透性较低。为了克服这个问题，需要一种新的透皮给药系统。众所周知，纳米颗粒可以增强材料的溶解度和渗透性，因此，本研究旨在合成负载 TQ 的L -精氨酸聚酰胺 (TQ/Arg PA) 纳米胶囊，并将其纳入透皮贴剂中，以延长 TQ 的递送时间。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促进剂来开发透皮贴剂。此外，通过界面聚合合成了新型 TQ/Arg-PA，并将所得纳米胶囊 (NC) 纳入基质透皮贴剂中。 Arg-PA NCs 的结构通过 NMR 和 FTIR 得到证实，最佳的 TQ/Arg-PA NCs 配方显示出较高的 TQ 包封率（99.60%）。 TQ/Arg-PA 和透皮贴剂的分子和热分析揭示了平均粒径为 129.23 ± 18.22 nm 的球形 NC 的有效开发。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 的释放时间超过 24 小时，当使用芦荟时，渗透增强了 42.64%。总之，所生产的制剂具有皮质类固醇和其他常用于治疗牛皮癣的药物的潜在替代品，因为其有效性、安全性并且没有其他药物通常相关的副作用。
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