Fang Jia-You, Leu Yann-Lii, Hwang Tsong-Long, Cheng Hsiao-Chin
Graduate Institute of Natural Products, Chang Gung University, Kweishan, Taoyuan, Taiwan.
Biol Pharm Bull. 2004 Nov;27(11):1819-25. doi: 10.1248/bpb.27.1819.
The purpose of this study was to evaluate the essential oils from sweet basil (Ocimum basilicum, OB) as skin permeation enhancers to promote the percutaneous absorption of drugs. The in vitro and in vivo irritancy of the essential oils was also examined. Terpenes with various carbon numbers (mono-, sesqui-, di-, and tri-) were identified in both the lower-polarity fraction (OB-1) and higher-polarity fraction (OB-2). In vitro skin permeation and deposition of indomethacin were significantly enhanced after treatment with OB essential oils. The enhancing effect of OB-1 was greater than that of OB-2 in the in vitro permeation and in vivo cutaneous microdialysis analyses as well as in the plasma concentration of indomethacin. On the other hand, the in vivo study showed that OB-2 had a greater ability to retain the drug within the skin than did OB-1. Enhancement of the skin permeation of drugs by OB essential oils might be mainly due to improvement in the partitioning of the drugs to the stratum corneum. Both in vitro cell cultures (keratinocytes and skin fibroblasts) and in vivo transepidermal water loss showed no or only negligible irritation to skin by OB essential oils.
本研究的目的是评估甜罗勒(Ocimum basilicum,OB)精油作为皮肤渗透促进剂对药物经皮吸收的促进作用。同时还检测了该精油的体外和体内刺激性。在低极性组分(OB-1)和高极性组分(OB-2)中均鉴定出了具有不同碳原子数的萜类化合物(单萜、倍半萜、二萜和三萜)。用OB精油处理后,吲哚美辛的体外皮肤渗透和沉积显著增强。在体外渗透、体内皮肤微透析分析以及吲哚美辛的血浆浓度方面,OB-1的增强作用大于OB-2。另一方面,体内研究表明,OB-2在皮肤内保留药物的能力比OB-1更强。OB精油对药物皮肤渗透的增强作用可能主要归因于药物在角质层中分配的改善。体外细胞培养(角质形成细胞和皮肤成纤维细胞)和体内经表皮水分流失均显示,OB精油对皮肤无刺激或仅有可忽略不计的刺激。