a Pharmaceutics and Industrial Pharmacy Department, Faculty of Pharmacy , Cairo University , Cairo , Egypt.
b Pharmaceutics Department , Damanhour University , Damanhour , Egypt.
Drug Dev Ind Pharm. 2018 Dec;44(12):2013-2025. doi: 10.1080/03639045.2018.1508220.
The study aims to elaborate novel self-assembled liquid crystalline nanoparticles (LCNPs) of resveratrol which has neuro-protective, anti-aging, and anticancer activity. Resveratrol loaded LCNPs fabrication and optimization for transdermal delivery was assessed via a quality by design approach based on 2 full factorial designs. The cubic phase of LCNPs was successfully prepared using GMO (glyceryl monooleate) via the emulsification technique. Based on the factorial design, the independent operating variables significantly affected the five dependent responses. The cubosomes and hexosomes hydrodynamic diameters were in the nanometer range (135-256 nm) with narrow particle size distribution, high negative zeta potential ≥ -27.9 mV, and entrapment efficiency ≥73.5%. The LCNPs succeeded in sustaining resveratrol release for almost 24 h, following a non-fickian transport of drug diffusion mechanism. Ex-vivo study revealed a significant enhancement up to six folds in the transdermal permeation of resveratrol-loaded LCNPs compared to its suspension. The selected LCNPs exhibited a high physical stability while retaining the cubic structure for at least 3 months. Quality by design approach successfully accomplished a predictable mathematical model permitting the development of novel LCNPs for sustained transdermal delivery of resveratrol.
本研究旨在阐述具有神经保护、抗衰老和抗癌活性的白藜芦醇新型自组装液晶纳米颗粒（LCNP）。通过基于 2 个完全因子设计的质量源于设计方法，评估了用于透皮递送的载白藜芦醇 LCNP 的制备和优化。通过乳化技术成功地使用 GMO（甘油单油酸酯）制备立方相 LCNP。基于因子设计，独立操作变量显著影响五个依赖响应。立方囊泡和六方囊泡的水动力学直径在纳米范围内（135-256nm），具有较窄的粒径分布、高的负 zeta 电位（≥-27.9mV）和包封效率（≥73.5%）。LCNP 成功地实现了白藜芦醇的持续释放，几乎达到 24 小时，遵循药物扩散机制的非菲克扩散。离体研究表明，与悬浮液相比，负载白藜芦醇的 LCNP 的透皮渗透显著提高了六倍。所选的 LCNP 表现出高物理稳定性，至少 3 个月内保持立方结构。质量源于设计方法成功地完成了可预测的数学模型，从而开发了用于白藜芦醇持续透皮递送的新型 LCNP。
