Hu Xixi, Tian Shuang, Wang Jiao, Luo Weixi, Yao Jiangli, Zhu Rui, Dai Yiyuan, Li Hongyun, Ma Yuhua, Liu Chen, Wang Wenping
College of Chinese Materia Medica, Yunnan University of Chinese Medicine, Kunming, Yunnan, China.
Key Laboratory for Tibet Plateau Phytochemistry of Qinghai Province, School of Pharmacy, Qinghai Nationalities University, Xining, Qinghai, China.
Front Bioeng Biotechnol. 2025 May 2;13:1589865. doi: 10.3389/fbioe.2025.1589865. eCollection 2025.
The study aimed to develop a supramolecular hydrogel of asiaticoside (AS) via self-assembly and evaluate its potential for enhanced transdermal delivery.
AS was dissolved in dimethyl sulfoxide (DMSO) and dispersed into a glycerol-water mixture (3:7 v/v) via ultrasonication to induce gelation. The critical gelation concentration (CGC) was determined through macroscopic and microscopic evaluation. Morphological analysis was performed using various microscopy techniques. Physicochemical properties were assessed using differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), Fourier-transform infrared (FTIR) spectroscopy, and UV-VIS spectroscopy. Molecular dynamics (MD) simulations with general AMBER force field (GAFF) parameters were used to analyze assembly dynamics. Rheological behavior and transdermal performance were tested using a rheometer and Franz diffusion cells, respectively.
The hydrogel formed at a CGC of 0.5% w/v, exhibiting pH-responsive gelation and a nanofibrous architecture. MD simulations revealed hydrogen bonding and π-π stacking as the dominant drivers of assembly, supported by FTIR peak shifts. The hydrogel demonstrated shear-thinning behavior (G' > G″) and thermal stability below 70°C. Compared to the AS suspension, the hydrogel enhanced transdermal flux by 1.73-fold and skin retention by 2.04-fold, attributed to supersaturated drug molecules and sustained release from the nanofiber network.
This work pioneers the use of AS as a natural supramolecular gelator, addressing its bioavailability challenges through nanostructured self-assembly. The hydrogel's dual functionality (pH-responsive gelation and enhanced permeation) offers a sustainable platform for the transdermal delivery of hydrophobic phytochemicals, bridging phytochemistry and nanobiotechnology. This strategy expands the application of plant-derived saponins in advanced drug delivery systems.
本研究旨在通过自组装开发积雪草苷（AS）的超分子水凝胶，并评估其增强透皮给药的潜力。
将AS溶解于二甲基亚砜（DMSO）中，通过超声分散到甘油 - 水混合物（3:7 v/v）中以诱导凝胶化。通过宏观和微观评估确定临界凝胶化浓度（CGC）。使用各种显微镜技术进行形态分析。使用差示扫描量热法（DSC）、粉末X射线衍射（PXRD）、傅里叶变换红外（FTIR）光谱和紫外 - 可见光谱评估物理化学性质。使用具有通用琥珀色力场（GAFF）参数的分子动力学（MD）模拟来分析组装动力学。分别使用流变仪和弗兰兹扩散池测试流变行为和透皮性能。
水凝胶在0.5% w/v的CGC下形成，表现出pH响应性凝胶化和纳米纤维结构。MD模拟揭示氢键和π - π堆积是组装的主要驱动力，FTIR峰位移支持了这一点。水凝胶表现出剪切变稀行为（G' > G″）且在70°C以下具有热稳定性。与AS悬浮液相比，水凝胶使透皮通量提高了1.73倍，皮肤滞留量提高了2.04倍，这归因于过饱和药物分子和从纳米纤维网络的持续释放。
本研究率先将AS用作天然超分子凝胶剂，通过纳米结构自组装解决其生物利用度挑战。水凝胶的双重功能（pH响应性凝胶化和增强渗透）为疏水性植物化学物质的透皮给药提供了一个可持续的平台，架起了植物化学与纳米生物技术之间的桥梁。该策略扩展了植物源皂苷在先进药物递送系统中的应用。
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