Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, El-Gomhoria Street, Mansoura, 35516, Dakahlia, Egypt.
Department of Biochemistry, Faculty of Pharmacy, Mansoura University, El-Gomhoria Street, Mansoura, 35516, Dakahlia, Egypt.
Drug Deliv Transl Res. 2023 Nov;13(11):2903-2929. doi: 10.1007/s13346-023-01360-5. Epub 2023 Jun 7.
Apocynin (APO), a well-known bioactive plant-based phenolic phytochemical with renowned anti-inflammatory and antioxidant pharmacological activities, has recently emerged as a specific nicotinamide adenine dinucleotide phosphate-oxidase (NADPH) oxidase inhibitor. As far as we know, no information has been issued yet regarding its topical application as a nanostructured-based delivery system. Herein, APO-loaded Compritol 888 ATO (lipid)/chitosan (polymer) hybrid nanoparticles (APO-loaded CPT/CS hybrid NPs) were successfully developed, characterized, and optimized, adopting a fully randomized design (3) with two independent active parameters (IAPs), namely, CPT amount (X) and Pluronic F-68 (PF-68) concentration (X), at three levels. Further in vitro-ex vivo investigation of the optimized formulation was performed before its incorporation into a gel base matrix to prolong its residence time with consequent therapeutic efficacy enhancement. Subsequently, scrupulous ex vivo-in vivo evaluations of APO-hybrid NPs-based gel (containing the optimized formulation) to scout out its momentous activity as a topical nanostructured system for beneficial remedy of rheumatoid arthritis (RA) were performed. Imperatively, the results support an anticipated effectual therapeutic activity of the APO-hybrid NPs-based gel formulation against Complete Freund's Adjuvant-induced rheumatoid arthritis (CFA-induced RA) in rats. In conclusion, APO-hybrid NPs-based gel could be considered a promising topical nanostructured system to break new ground for phytopharmaceutical medical involvement in inflammatory-dependent ailments.
白杨素（APO）是一种众所周知的具有抗炎和抗氧化药理学活性的植物源多酚类生物活性化合物，最近已成为一种特定的烟酰胺腺嘌呤二核苷酸磷酸氧化酶（NADPH）氧化酶抑制剂。据我们所知，目前尚无关于其作为基于纳米结构的递药系统的局部应用的信息。在此，成功开发了负载白杨素的 Compritol 888 ATO（脂质）/壳聚糖（聚合物）混合纳米粒（负载白杨素的 CPT/CS 混合 NPs），采用完全随机设计（3），两个独立的活性参数（IAP），即 CPT 量（X）和泊洛沙姆 F-68（PF-68）浓度（X），各有三个水平。在将优化的制剂掺入凝胶基质中以延长其滞留时间从而增强治疗效果之前，进一步进行了体外-体内研究。随后，对基于 APO 混合 NPs 的凝胶（包含优化的制剂）进行了严格的体外-体内评价，以探索其作为治疗类风湿关节炎（RA）的局部纳米结构系统的重要作用。至关重要的是，结果支持基于 APO 混合 NPs 的凝胶制剂对完全弗氏佐剂诱导的类风湿关节炎（CFA 诱导的 RA）大鼠具有预期的有效治疗活性。总之，APO 混合 NPs 凝胶可以被认为是一种很有前途的局部纳米结构系统，为植物药在炎症依赖性疾病中的医学应用开辟了新天地。
