Wang Yu, Yue Yan, Jia Ruoyang, Liu Xinyi, Cheng Zhiqing, Cheng Yongfeng, Xu Yinxiang, Xie Zili, Xia Hongmei
College of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012, China.
Clinical College of Anhui Medical University, Hefei 230031, China.
Gels. 2023 Mar 5;9(3):198. doi: 10.3390/gels9030198.
Paeonol (PAE) is a hydrophobic drug. In this study, we encapsulated paeonol in a lipid bilayer of liposomes (PAE-L), which delayed drug release and increased drug solubility. When PAE-L was dispersed in gels (PAE-L-G) based on a poloxamer matrix material for local transdermal delivery, we observed amphiphilicity, reversible thermal responsiveness, and micellar self-assembly behavior. These gels can be used for atopic dermatitis (AD), an inflammatory skin disease, to change the surface temperature of the skin. In this study, we prepared PAE-L-G at an appropriate temperature for the treatment of AD. We then assessed the gel's relevant physicochemical properties, in vitro cumulative drug release, and antioxidant properties. We found that PAE-loaded liposomes could be designed to increase the drug effect of thermoreversible gels. At 32 °C, PAE-L-G could change from solution state to gelatinous state at 31.70 ± 0.42 s, while the viscosity was 136.98 ± 0.78 MPa.S and the free radical scavenging rates on DPPH and HO were 92.24 ± 5.57% and 92.12 ± 2.71%, respectively. Drug release across the extracorporeal dialysis membrane reached 41.76 ± 3.78%. In AD-like mice, PAE-L-G could also relieve skin damage by the 12th day. In summary, PAE-L-G could play an antioxidant role and relieve inflammation caused by oxidative stress in AD.
丹皮酚(PAE)是一种疏水性药物。在本研究中,我们将丹皮酚包裹在脂质体的脂质双层中(PAE-L),这延缓了药物释放并提高了药物溶解度。当PAE-L分散在基于泊洛沙姆基质材料的凝胶中(PAE-L-G)用于局部透皮给药时,我们观察到其具有两亲性、可逆热响应性和胶束自组装行为。这些凝胶可用于治疗特应性皮炎(AD)这种炎症性皮肤病,以改变皮肤表面温度。在本研究中,我们制备了适合治疗AD的PAE-L-G。然后我们评估了该凝胶的相关物理化学性质、体外累积药物释放和抗氧化性能。我们发现负载PAE的脂质体可以设计成增强热可逆凝胶的药物效果。在32℃时,PAE-L-G可在31.70±0.42秒内从溶液状态转变为凝胶状态,此时粘度为136.98±0.78MPa·S,对DPPH和HO的自由基清除率分别为92.24±5.57%和92.12±2.71%。药物透过体外透析膜的释放率达到41.76±3.78%。在类AD小鼠中,PAE-L-G在第12天时也可减轻皮肤损伤。总之,PAE-L-G可发挥抗氧化作用并减轻AD中氧化应激引起的炎症。