Formulation and Evaluation of Transdermal Niosomal Gel for Antihyperlipidemic Agent

Pravin Patil, Priyanka Bhagwat, Pournima Sankpal, Sachinkumar Patil, Shashikant Dhawale
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Abstract

The current study aims to create a formulation of Fluvastatin sodium (FVS) loaded niosome for the treatment of antihyperlipidemia using thin film hydration. The developed formulations were statistically optimized by two factors, three levels by 3-level factorial design and were evaluated for vesicle size, entrapment efficiency, zeta potential, transmission electron microscopy, and invitro drug release. The optimized FVS niosome being transformed to gel formulation was likewise analyzed for in-vitro skin permeability study, lipase action, and stability study. The composition of an improved FVS niosome revealed vesicle size, entrapment effectiveness, zeta potential of 105.3 ± 12.4nm, 74.5 ± 0.86% and -36.2±7mV, respectively, with spherical morphology. The FVS Niosomal gel demonstrated improved skin permeation compared to Orlistat. Furthermore, lipase activity showed better activity when compared with standard Orlistat drugs. Niosomal particles were discovered as a reliable nanovesicular carrier for the transdermal administration of FVS.
抗高血脂药物透皮鼻腔凝胶的配制与评估
目前的研究旨在利用薄膜水合技术制备一种载入氟伐他汀钠(FVS)的niosome制剂,用于治疗高脂血症。通过 3 级因子设计,对所开发的配方进行了 2 因子、3 级统计优化,并对囊泡大小、夹持效率、ZETA 电位、透射电子显微镜和体外药物释放进行了评估。将优化后的 FVS niosome 转化为凝胶制剂后,同样进行了体外皮肤渗透性研究、脂肪酶作用和稳定性研究。改进后的 FVS niosome 的囊泡大小、夹持效果和 zeta 电位分别为 105.3 ±12.4nm, 74.5 ± 0.86% 和 -36.2±7mV,呈球形。与奥利司他相比,FVS Niosomal 凝胶的皮肤渗透性更好。此外,与标准奥利司他药物相比,脂肪酶活性更高。研究发现,Niosomal 颗粒是经皮给药 FVS 的一种可靠的纳米颗粒载体。
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