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首页> 外文期刊>Journal of drug delivery science and technology >Cilnidipine loaded transfersomes for transdermal application: Formulation optimization, in-vitro and in-vivo study
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Cilnidipine loaded transfersomes for transdermal application: Formulation optimization, in-vitro and in-vivo study

机译：Cilnidipine负载转移转移透皮应用：配方优化，体外和体内研究

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摘要

Cilnidipine, a BCS class II drug is a widely prescribed antihypertensive with poor oral bioavailability. An approach to deliver the drug as flexible vesicles called transfersomes through the skin was adopted to optimise the drug delivery. A quadratic model of Box-Behnken design was used as QbD approach to analyze the effect of variables on formulation quality (example: vesicle size, entrapment efficiency and transdermal flux). The optimized composition showed small vesicle size (206.24 +/- 5.94 nm) with a good polydispersity index (0.302 +/- 0.034), sufficient drug entrapment (96.45 +/- 1.92%) and a good transdermal flux (27.72 +/- 3.55 mu g/cm(2)/h). Confocal laser scanning microscopy of rat skin treated with Rhodamine B loaded transfersomal formulation showed significantly deeper penetration compared to Rhodamine B dye solution. The optimized formulation was developed as a gel that exhibited higher drug release (81.52 +/- 9.01%) than the drug suspension (20.29 +/- 3.78%). Skin irritation study and histopathological examination of rat abdominal skin revealed that the gel formulation was safe, less irritant and well tolerable for transdermal delivery. Furthermore, the in vivo pharmacokinetic study showed improved bioavailability at a significant level (p < 0.001) than the drug suspension. Thus, it is concluded that cilnidipine loaded transfersomes are efficacious in treating hypertension.
机译：西兰迪普，BCS II类药物是一种广泛规定的抗高血压性，口服不良的生物利用度。采用一种将药物作为柔性囊泡作为柔性囊泡的方法，以优化药物递送。 Box-Behnken设计的二次模型被用作QBD方法，分析变量对配方质量的影响（例如：囊泡尺寸，咬血管效率和透皮通量）。优化的组合物显示出小的囊泡尺寸（206.24 +/- 5.94nm），具有良好的多分散性指数（0.302 +/- 0.034），足够的药物夹带（96.45 +/- 1.92％）和良好的透皮通量（27.72 +/- 3.55 mu g / cm（2）/ h）。用罗丹明B负载转杂甲醚制剂处理的大鼠皮肤的共聚焦激光扫描显微镜表现出与罗丹明B染料溶液相比显着更深的渗透。优化的制剂被开发为凝胶，其凝胶显示出比药物悬浮液更高的药物释放（81.52 +/- 9.01％）（20.29 +/- 3.78％）。皮肤刺激研究和大鼠腹部皮肤的组织病理学检查显示，凝胶配方是安全的，透明递送的刺激性较小，耐受性良好。此外，体内药代动力学研究表明，在显着水平（P <0.001）中的生物利用度高于药物悬浮液。因此，得出结论认为，西兰​​迪普载的转移素在治疗高血压方面是有效的。

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