School of Pharmacy, University of Nottingham Malaysia, Semenyih, Malaysia.
School of Pharmacy, Monash University Malaysia, Bandar Sunway, Malaysia.
Pharm Dev Technol. 2021 Feb;26(2):243-251. doi: 10.1080/10837450.2020.1860087. Epub 2020 Dec 15.
Tocotrienol (TRF) ethosomes were developed and evaluated for potential transdermal delivery against melanoma. The optimised TRF ethosomal size ranged between 64.9 ± 2.2 nm to 79.6 ± 3.9 nm and zeta potential (ZP) between -53.3 mV to -62.0 ± 2.6 mV. Characterisation of the ethosomes by ATR-FTIR indicated the successful formation of TRF-ethosomes. Scanning electron microscopy (SEM) images demonstrated the spherical shape of ethosomes, and the entrapment efficiencies of all the formulations were above 66%. permeation studies using full-thickness human skin showed that the permeation of gamma-T3 from the TRF ethosomal formulations was significantly higher ( < 0.05) than from the control. The cumulative amount of gamma-T3 permeated from TRF ethosome after 48 hours was 1.03 ± 0.24 µg cm with a flux of 0.03 ± 0.01 µg cm h. Furthermore, the flux of gamma-T3 across the Strat-M and the epidermal membrane was significantly higher than that across full-thickness human skin ( < 0.05). cytotoxicity studies on HaCat cells showed significantly higher cell viability than the pure drug solution ( < 0.05). The enhanced skin permeation and high cell viability associated with this formulation suggest a promising carrier for transdermal delivery.
生育三烯酚（TRF）醇质体被开发并评估用于潜在的经皮传递治疗黑素瘤。优化的 TRF 醇质体大小范围在 64.9±2.2nm 至 79.6±3.9nm 之间，Zeta 电位（ZP）在-53.3mV 至-62.0±2.6mV 之间。ATR-FTIR 对醇质体的特征分析表明成功形成了 TRF-醇质体。扫描电子显微镜（SEM）图像显示醇质体的球形形状，所有制剂的包封效率均高于 66%。使用全厚人皮肤进行的渗透研究表明，γ-T3 从 TRF 醇质体制剂中的渗透明显更高（<0.05）。经过 48 小时后，TRF 醇质体中渗透的γ-T3 累积量为 1.03±0.24µg cm，通量为 0.03±0.01µg cm h。此外，γ-T3 穿过 Strat-M 和表皮膜的通量明显高于穿过全厚人皮肤的通量（<0.05）。在 HaCat 细胞上进行的细胞毒性研究显示细胞活力明显高于纯药物溶液（<0.05）。这种制剂与皮肤渗透增强和高细胞活力相关，表明其是一种有前途的经皮传递载体。
