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采用纳米囊泡系统增强昂丹司琼经皮传递:制备、表征、优化及体外渗透研究-Box-Cox 变换实例。

Enhanced transdermal delivery of ondansetron using nanovesicular systems: Fabrication, characterization, optimization and ex-vivo permeation study-Box-Cox transformation practical example.

机构信息

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Egypt.

Department of Analytical Chemistry, Faculty of Pharmacy, Cairo University, Egypt.

出版信息

Eur J Pharm Sci. 2018 Mar 30;115:352-361. doi: 10.1016/j.ejps.2018.01.044. Epub 2018 Jan 31.

Abstract

This study aimed to formulate suitable nanovesicles (NVs) for transdermal delivery of Ondansetron. It also illustrated a practical example for the importance of Box-Cox transformation. A 2 full factorial design was used to enable testing transfersomes, ethosomes, and transethosomes of Ondansetron simultaneously. The independent variables (IVs) studied were sodium taurocholate amount, ethanol volume in hydration medium and sonication time. The studied dependent variables (DVs) were: particle size (PS), zeta potential (ZP) and entrapment efficiency (EE). Polynomial equations were used to study the influence of IVs on each DV. Numerical multiple response optimization was applied to select an optimized formula (OF) with the goals of minimizing PS and maximizing ZP absolute value and EE. Box-Cox transformation was adopted to enable modeling PS raised to the power of 1.2 with an excellent prediction R of 1.000. ZP and EE were adequately represented directly with prediction R of 0.9549 and 0.9892 respectively. Response surface plots helped in explaining the influence of IVs on each DV. Two-sided 95% prediction interval test and percent deviation of actual values from predicted ones proved the validity of the elucidated models. The OF was a transfersomal formula with desirability of 0.866 and showed promising results in ex-vivo permeation study.

摘要

本研究旨在为昂丹司琼的透皮给药构建合适的纳米囊(NVs)。它还说明了 Box-Cox 变换的重要性的实际示例。采用 2 全因子设计来同时测试昂丹司琼的传递体、醇质体和转醇质体。研究的自变量(IVs)为牛磺胆酸钠的量、水合介质中的乙醇体积和超声时间。研究的因变量(DVs)为:粒径(PS)、Zeta 电位(ZP)和包封效率(EE)。多项式方程用于研究 IVs 对每个 DV 的影响。数值多响应优化用于选择具有最小 PS 和最大 ZP 绝对值和 EE 的目标的优化配方(OF)。采用 Box-Cox 变换来对 PS 进行 1.2 次幂建模,具有出色的预测 R 为 1.000。ZP 和 EE 可以直接通过预测 R 为 0.9549 和 0.9892 来充分表示。响应面图有助于解释 IVs 对每个 DV 的影响。双向 95%预测区间测试和实际值与预测值的百分比偏差证明了所阐明模型的有效性。OF 是一种传递体配方,其适宜性为 0.866,并在体外渗透研究中显示出有希望的结果。

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