牛皮癣是一种慢性炎症性疾病,正在变得普遍,并与许多其他严重疾病有关。本研究旨在开发一种装载甲氨蝶呤的杏仁油基纳米乳液制剂(MTXNE),用于局部给药。采用高剪切均质化技术制备载药纳米乳制剂。配方的稳定性,以及其他物理和化学特性,包括诱捕有效性,药物释放动力学,皮肤渗透性,皮肤刺激,和体内评估优化的配方,被评估。此外,采用咪喹莫特诱导的大鼠银屑病研究MTXNE对皮肤病的疗效。MTXNE制剂的粒径为18.74±9.748nm,多分散指数(PDI)为0.198±0.01,平均包封率为79.65±3.84%。释放动力学模型估计在24小时后pH5.5时药物释放为81.08%。表皮,通过优化的MTXNE配方成功地流化了真皮,如FTIR结果所示,最有可能增强药物保留和渗透性。然而,因为吐温80和PEG400是众所周知的渗透促进剂,它们的应用大大加速了这些效果。渗透数据表明,24小时后,甲氨蝶呤以76.83±4.98g/cm2的速率从纳米乳剂中释放,通量率为2.385±0.61µg/cm2/h。在兔皮肤上进行的体内研究显示,所制备的负载MTX的纳米乳液制剂的增强的皮肤渗透不引起角质层的细胞间脂质层中的任何结构修饰。在体内抗牛皮癣研究中使用的兔子证明MTXNE使PASI减少了95%。药代动力学特征显示Cmax,Tmax,t1/2值为8.63µg/mL,12.5h,17.77±2.21h,分别。这些发现表明,制剂MTXNE在治疗牛皮癣中是有效的,并且可以减轻牛皮癣症状。
Psoriasis is a chronic inflammatory disease that is becoming widespread and is associated with many kinds of additional severe diseases. The present study aimed to develop a methotrexate-loaded almond oil-based
nanoemulsion formulation (MTX NE) for topical administration. The drug-loaded
nanoemulsion formulation was prepared by high shear homogenization technique. The formulation\'s stability, as well as other physical and chemical characteristics, including entrapment effectiveness, drug release kinetics, skin permeability, skin irritation, and in vivo evaluation of the optimized formulation, was assessed. Additionally, imiquimod-induced psoriasis in rats was employed to investigate the efficacy of MTX NE against skin disorders. The MTX NE formulation was developed with a particle size of 18.74 ± 9.748 nm, a polydispersity index (PDI) of 0.198 ± 0.01, and an average entrapment efficiency of 79.65 ± 3.84%. The release kinetics model estimates 81.08% drug release at pH 5.5 after 24 h. The major layers of the skin, the epidermis, and dermis were successfully fluidized by the optimized MTX NE formulation, as shown by FTIR results, most likely enhancing drug retention and permeability. However, since Tween 80 and PEG 400 are well-known penetration enhancers, their application greatly accelerates these effects. Permeation data indicate that after 24 h, methotrexate was released from the nano-emulsion at 76.83 ± 4.98 g/cm2 with a flux rate of 2.385 ± 0.61 µg/cm2/h. The in vivo study conducted on rabbit skin showed that the enhanced skin penetration of the prepared MTX-loaded
nanoemulsion formulation does not cause any structural modifications in the inter-cellular lipid layers of the stratum corneum. Rabbits used in the in vivo anti-psoriatic investigation demonstrated that MTX NE produced a 95% reduction in PASI. The pharmacokinetic profile revealed that the Cmax, Tmax, and t1/2 values were 8.63 µg/mL, 12.5 h, and 17.77 ± 2.21 h, respectively. These findings suggest that the formulation MTX NE is effective in treating psoriasis and may reduce psoriasis symptoms.