Hung Wan-Hsuan, Chen Ping-Kang, Fang Chih-Wun, Lin Ying-Chi, Wu Pao-Chu
Divison of Pharmacy, Zuoying Branch of Kaohsiung Armed Forces General Hospital, Kaohsiung City 81342, Taiwan.
School of Pharmacy, College of Pharmacy, Kaohsiung Medical University, Kaohsiung City 80708, Taiwan.
Pharmaceutics. 2021 Mar 19;13(3):410. doi: 10.3390/pharmaceutics13030410.
The aim of this study was to design oil in water (O/W) microemulsion formulations for the topical administration of azelaic acid. The permeability of azelaic acid through rat skin and the anti-inflammatory activities of the formulations were conducted to examine the efficacy of the designed formulations. Skin irritation and stability tests were also performed. The permeability of azelaic acid was significantly increased by using O/W microemulsions as carriers. The edema index of ear swelling percentage was significantly recovered by the 5% drug-loaded formulation and a 20% commercial product, demonstrating that the experimental formulation possessed comparable effect with the commercial product on the improvement of inflammation. The experimental formulation did not cause significant skin irritation compared to the negative control group. Moreover, the drug-loaded formulation also showed thermodynamic stability and chemical stability after storage for 30 days. In conclusion, the O/W microemulsion was a potential drug delivery carrier for azelaic acid topical application.
本研究的目的是设计用于壬二酸局部给药的水包油(O/W)微乳制剂。通过大鼠皮肤测定壬二酸的渗透率,并对制剂的抗炎活性进行检测,以考察所设计制剂的疗效。还进行了皮肤刺激性和稳定性试验。以O/W微乳为载体可显著提高壬二酸的渗透率。含5%药物的制剂和一种20%的市售产品能显著降低耳部肿胀百分比的水肿指数,表明实验制剂在改善炎症方面与市售产品具有相当的效果。与阴性对照组相比,实验制剂未引起明显的皮肤刺激。此外,含药制剂在储存30天后还表现出热力学稳定性和化学稳定性。总之,O/W微乳是壬二酸局部应用潜在的药物递送载体。