Bai Jie, Lu Yang, Li Peng-yue, Liu Cong-min, Wu Hui-chao, Wen Ran, Du Shou-ying
Department of Industrial Pharmacy, School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing, China.
Pak J Pharm Sci. 2014 Mar;27(2):369-75.
Current work aimed to develop and evaluate a transdermal delivery system of hydrogel patch for ferulic acid to treat skin damage induced by UV radiation. VISCOMATE(TM) NP700, dihydroxy aluminium aminoacetate, glycerine, tartaric acid were used in combination in different ratios to design the hydrogel patch. In vitro release rate was selected as an index to optimize the formulation. The formulated hydrogel patch was evaluated by several parameters like tacking strength, cohesive strength, peeling strength, residuals after peeling and drug content determination. The in vitro penetration was determined by Franz diffusion technology with hairless mouse skin as permeability media. Different kinetics models were employed to simulate the release and penetrate patterns of ferulic acid from patches in order to investigate the drug transport mechanism. The residual drugs in the patch and skin were determined after the penetration experiment. The optimized preparation was dihydroxy aluminium aminoacetate: NP700: glycerine: ferulic acid as a ratio of 0.02:0.4:1.5:1.25:0.25. The cumulative percentage of release was 60.4465±1.7679% for 24h, which results from a combination of diffusion effect and polymer erosion effect. For the barrier of stratum corneum, the cumulative penetrate rate was only 1.3156±0.3588% and the release mechanism turn out to be the effect of erosion of polymer surface. The residual drugs in the patch were 97.5949±1.4932%. The in vitro data revealed that it was easy for ferulic acid to release from the paste while difficult to permeate through the skin barrier, which resulted in most of drugs residued in the paste. Hence, further experiments will be necessary for finding the penetration enhancer in ferulic acid transdermal delivery.
当前的工作旨在开发和评估一种用于阿魏酸的水凝胶贴剂透皮给药系统,以治疗紫外线辐射引起的皮肤损伤。使用VISCOMATE(TM) NP700、甘羟铝、甘油、酒石酸按不同比例组合来设计水凝胶贴剂。选择体外释放速率作为优化制剂的指标。通过诸如粘着强度、内聚强度、剥离强度、剥离后残留量和药物含量测定等多个参数对所制备的水凝胶贴剂进行评估。采用Franz扩散技术,以无毛小鼠皮肤作为渗透介质来测定体外渗透率。采用不同的动力学模型来模拟阿魏酸从贴剂中的释放和渗透模式,以研究药物转运机制。渗透实验后测定贴剂和皮肤中的残留药物。优化后的制剂中甘羟铝:NP700:甘油:阿魏酸的比例为0.02:0.4:1.5:1.25:0.25。24小时的累积释放百分比为60.4465±1.7679%,这是扩散效应和聚合物侵蚀效应共同作用的结果。对于角质层屏障,累积渗透率仅为1.3156±0.3588%,释放机制为聚合物表面的侵蚀作用。贴剂中的残留药物为97.5949±1.4932%。体外数据表明,阿魏酸易于从贴剂中释放,但难以透过皮肤屏障,这导致大部分药物残留在贴剂中。因此,有必要进一步开展实验以寻找阿魏酸透皮给药的渗透促进剂。