Department of Pharmacy, First Hospital of Lanzhou University, Lanzhou 730000, China.
Arch Pharm Res. 2012 Jan;35(1):109-17. doi: 10.1007/s12272-012-0112-0. Epub 2012 Feb 2.
The aim of this study was to compare the skin permeation of ethosomes, binary ethosomes and transfersomes of Terbinafine Hydrochloride (TH) under non-occlusive conditions. These lipid vesicles were prepared and characterized for shape, size, zeta-potential and entrapment efficiency. Franz diffusion cells and confocal laser scanning microscopy (CLSM) were used for the percutaneous absorption studies. The quantity of drug in the skin from ethosomes, binary ethosomes (the weight ratio of ethanol to propylene glycol 7:3, ethanol-PG = 7:3, w/w), and transfersomes was 1.26, 1.51 (p <0.05), 1.56 (p <0.01) times higher than that of TH from traditional liposomes (control). The skin deposition of the applied dose (DD%) of TH from ethosomes, binary ethosomes, and transfersomes was 3.34 (p < 0.05), 9.88 (p < 0.01), 2.52 times higher than that of TH from control. The results of CLSM experiments showed that penetration depth and fluorescence intensity of Rhodamine B from binary ethosomes was much greater than that from ethosomes and transfersomes. These results indicated the binary ethosomes (ethanol-PG = 7:3, w/w) most effectively permitted drug penetration through skin; transfersomes made drug easiest to accumulate in the skin. Ethosomes improved drug delivery with greater improvement in skin permeation than improvement in skin deposition.
本研究旨在比较特比萘芬盐酸盐（TH）的醇质体、二元醇质体和传递体在非密闭条件下的皮肤渗透情况。这些脂质体在形状、大小、Zeta 电位和包封效率方面进行了制备和特征描述。Franz 扩散池和共聚焦激光扫描显微镜（CLSM）用于经皮吸收研究。与传统脂质体（对照）相比，醇质体、二元醇质体（乙醇与丙二醇重量比为 7:3，乙醇-PG = 7:3，w/w）和传递体中的药物在皮肤中的量分别提高了 1.26、1.51（p <0.05）和 1.56（p <0.01）倍。醇质体、二元醇质体和传递体中 TH 的应用剂量（DD%）在皮肤中的沉积分别是对照的 3.34（p <0.05）、9.88（p <0.01）和 2.52 倍。CLSM 实验结果表明，二元醇质体中 Rhodamine B 的穿透深度和荧光强度明显大于醇质体和传递体。这些结果表明，二元醇质体（乙醇-PG = 7:3，w/w）最有效地允许药物穿透皮肤；传递体使药物最容易在皮肤中积累。醇质体改善了药物传递，皮肤渗透的改善程度大于皮肤沉积的改善程度。
