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Investigating superiority of novel bilosomes over niosomes in the transdermal delivery of diacerein: In vitro characterization, ex vivo permeation and in vivo skin deposition study
Journal of Liposome Research ( IF 3.6 ) Pub Date : 2018-02-06 , DOI: 10.1080/08982104.2018.1430831
Diana E Aziz 1 , Aly A Abdelbary 1, 2 , Abdelhalim I Elassasy 1
Affiliation  

Abstract Skin is considered the most accessible organ of the body because of its underlying capillary network. However, stratum corneum (SC), the upper most layer of skin, represents major diffusional barrier for most drugs. Hence, the use of edge activators (EAs) in designing novel elastic vesicles is hypothesized to impart their lipid bilayer with ultra-flexibility to trespass SC by high self-optimizing deformability. To confirm this hypothesis, this work aimed at developing novel bilosomes by modulating conventional niosomal composition using different bile salts as EAs and investigating their superiority over niosomes for transdermal delivery of diacerein (DCN), as model drug. Bilosomes were prepared by thin film hydration (TFH) technique according to full 31.22 factorial design to select the optimal formulation using Design-Expert® software. The optimal bilosomes (B6) showed nanosized vesicles (301.65 ± 17.32 nm) and 100.00 ± 0.00 % entrapment efficiency. Ex vivo permeation studies and in vivo evaluation revealed that B6 exhibited superior permeation and drug retention capacity compared to the conventional niosomal formulation and drug suspension. Furthermore, B6 was subjected to in vivo histopathological study using male Wistar rats which ensured its safety for topical application. Overall, the results confirmed the hypothesized superiority of bilosomes over niosomes for enhancing DCN flux across the skin.

中文翻译:

在双醋瑞因的透皮递送中研究新型胆汁体优于 niosomes 的优势:体外表征、离体渗透和体内皮肤沉积研究

摘要 皮肤因其底层的毛细血管网络而被认为是人体最容易接近的器官。然而,皮肤的最上层角质层 (SC) 是大多数药物的主要扩散屏障。因此,假设在设计新型弹性囊泡中使用边缘激活剂 (EA) 可以通过高自优化变形性赋予其脂质双层超柔韧性以侵入 SC。为了证实这一假设,这项工作旨在通过使用不同的胆汁盐作为 EA 调节传统的 niosomes 组成来开发新的胆汁体,并研究它们在作为模型药物的双醋瑞因 (DCN) 经皮递送方面优于 niosomes 的优势。根据完整的 31.22 因子设计,通过薄膜水合 (TFH) 技术制备胆汁体,以使用 Design-Expert® 软件选择最佳配方。最佳胆汁体 (B6) 显示出纳米级囊泡 (301.65 ± 17.32 nm) 和 100.00 ± 0.00 % 的包埋效率。体外渗透研究和体内评估表明,与传统的 niosomal 制剂和药物悬浮液相比,B6 表现出优异的渗透和药物保留能力。此外,使用雄性 Wistar 大鼠对 B6 进行了体内组织病理学研究,确保了其局部应用的安全性。总体而言,结果证实了 bilosomes 在增强皮肤上 DCN 通量方面优于 niosomes 的假设优势。体外渗透研究和体内评估表明,与传统的 niosomal 制剂和药物悬浮液相比,B6 表现出优异的渗透和药物保留能力。此外,使用雄性 Wistar 大鼠对 B6 进行了体内组织病理学研究,确保了其局部应用的安全性。总体而言,结果证实了 bilosomes 在增强皮肤上 DCN 通量方面优于 niosomes 的假设优势。体外渗透研究和体内评估表明,与传统的 niosomal 制剂和药物悬浮液相比,B6 表现出优异的渗透和药物保留能力。此外,使用雄性 Wistar 大鼠对 B6 进行了体内组织病理学研究,确保了其局部应用的安全性。总体而言,结果证实了 bilosomes 在增强皮肤上 DCN 通量方面优于 niosomes 的假设优势。
更新日期:2018-02-06
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