Bin Jardan Yousef A, Ahad Abdul, Raish Mohammad, Al-Jenoobi Fahad I
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.
Pharmaceutics. 2023 Sep 27;15(10):2391. doi: 10.3390/pharmaceutics15102391.
Sinapic acid (SA) is a bioactive phenolic acid; its diverse properties are its anti-inflammatory, antioxidant, anticancer, and antibacterial activities. The bioactive compound SA is poorly soluble in water. Our goal was to formulate SA-transethosomes using thin-film hydration. The prepared formulations were examined for various parameters. In addition, the optimized formulation was evaluated for surface morphology, in-vitro penetration studies across the Strat M, and its antioxidant activity. The optimized formulation (F5) exhibited 74.36% entrapment efficacy. The vesicle size, zeta potential, and polydispersity index were found to be 111.67 nm, -7.253 mV, and 0.240, respectively. The surface morphology showed smooth and spherical vesicles of SA-transethosomes. In addition, the prepared SA-transethosomes exhibited enhanced antioxidant activity. The SA-transethosomes demonstrated considerably greater penetration across the Strat M membrane during the study. The flux of SA and SA-transethosomes through the Strat M membrane was 1.03 ± 0.07 µg/cm/h and 2.93 ± 0.16 µg/cm/h. The enhancement ratio of SA-transethosomes was 2.86 ± 0.35 compared to the control. The SA-transethosomes are flexible nano-sized vesicles and are able to penetrate the entrapped drug in a higher concentration. Hence, it was concluded that SA-transethosome-based approaches have the potential to be useful for accentuating the penetrability of SA across the skin.
芥子酸（SA）是一种具有生物活性的酚酸；其多种特性包括抗炎、抗氧化、抗癌和抗菌活性。生物活性化合物SA在水中的溶解度很低。我们的目标是通过薄膜水化法制备SA-转质体。对制备的制剂进行了各种参数检测。此外，还对优化后的制剂进行了表面形态、跨Strat M的体外渗透研究及其抗氧化活性评估。优化后的制剂（F5）包封率为74.36%。发现囊泡大小、zeta电位和多分散指数分别为111.67 nm、-7.253 mV和0.240。表面形态显示SA-转质体的囊泡光滑且呈球形。此外，制备的SA-转质体表现出增强的抗氧化活性。在研究过程中，SA-转质体在跨Strat M膜时表现出显著更高的渗透性。SA和SA-转质体通过Strat M膜的通量分别为1.03±0.07 μg/cm/h和2.93±0.16 μg/cm/h。与对照相比，SA-转质体的增强倍数为2.86±0.35。SA-转质体是灵活的纳米级囊泡，能够以更高的浓度包封药物。因此，可以得出结论，基于SA-转质体的方法有可能用于增强SA在皮肤中的渗透性。
