College of Pharmacy, Al Ain University, Abu Dhabi 112612, United Arab Emirates.
College of Pharmacy, Al Ain University, Abu Dhabi 112612, United Arab Emirates.
J Pharm Sci. 2021 Dec;110(12):3907-3918. doi: 10.1016/j.xphs.2021.08.014. Epub 2021 Aug 14.
Nano-colloidal systems formulated from amphiphilically-modified polysaccharides (degree of modification 16.6%) are focus of prominent study due to their potential to augment active penetration across the skin. Here we report the synthesis of amphiphilically-modified guar gum (GBE-GG) prepared by grafting with glycidol butyl ether (GBE), which were subsequently formed into nanocarriers and loaded with α-arbutin (22.3% loading). The monodispersed and close-to-spherical nanocarriers (size range 239-297 nm) formed via cross-linking were adequately stable mainly at low temperature (4 °C) under physiological pH condition. α-arbutin was released from GBE-GG NPs in a more sustained manner and the release profiles can be accurately represented by the 1 order kinetic model. In-vitro interactions on immortalised human keratinocytes (HaCaT) cells revealed an increase in biological membrane permeability as well as the absence of cellular toxicity at application pertinent concentrations. No substantial haemolytic activity appeared and flow cytometry analysis revealed effective cellular uptake, suggesting their potential as promising nanocarriers for percutaneous delivery that warrants further comprehensive research.
由于具有增强活性物质经皮渗透的潜力，由两亲改性多糖（修饰度 16.6%）制成的纳米胶体系统是当前研究的重点。本研究报告了通过与缩水甘油丁醚（GBE）接枝合成的两亲改性瓜尔胶（GBE-GG）的合成，随后将其制成纳米载体并负载α-熊果苷（载药量 22.3%）。通过交联形成的单分散且近球形的纳米载体（粒径范围 239-297nm）在低温（4°C）和生理 pH 条件下主要保持足够稳定。α-熊果苷从 GBE-GG NPs 中的释放更持续，释放曲线可以通过 1 级动力学模型准确表示。在永生化人角质形成细胞（HaCaT）细胞上的体外相互作用表明，生物膜通透性增加，在应用相关浓度下没有细胞毒性。几乎没有出现明显的溶血活性，流式细胞术分析显示有效的细胞摄取，这表明它们具有作为经皮给药有前途的纳米载体的潜力，值得进一步进行全面研究。
