Takeuchi Y, Yasukawa H, Yamaoka Y, Morimoto Y, Nakao S, Fukumori Y, Fukuda T
Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Kobe-Gakuin University, Japan.
Chem Pharm Bull (Tokyo). 1992 Feb;40(2):484-7. doi: 10.1248/cpb.40.484.
Whole skin lipid bio-liposomes (skin bio-liposomes), in size ranging from 2 to 8 microns, were prepared by a reverse phase evaporation technique using rat full thickness skin. Leakage of an encapsulated fluorescence probe, ANTS (delta-amino-1,3,6-naphthalene-trisulfonate), was measured by adding transdermal penetration enhancers (penetrants) into the medium where the skin bio-liposomes were present. Oleylamine induced a fast release of ANTS from the liposomes compared to lauryl-amine which showed a weak action. With these penetrants, the degree of ANTS release from the prepared bio-liposomes was found to correlate well with the results of frequency changes in the CH-asymmetric stretching band near 2920 cm-1 in the rat stratum corneum. The penetrant which caused relatively strong leakage of ANTS induced the significantly large shift of the peak toward the higher wave-numbers due to the perturbation in the structure of lipids of the stratum corneum. The skin bio-liposomes prepared from the rat full thickness skin could be useful in evaluating the penetrants.
采用大鼠全层皮肤,通过反相蒸发技术制备了粒径范围为2至8微米的全皮肤脂质生物脂质体(皮肤生物脂质体)。通过向存在皮肤生物脂质体的介质中添加透皮渗透促进剂(渗透剂)来测量包封的荧光探针ANTS(δ-氨基-1,3,6-萘三磺酸盐)的泄漏情况。与作用较弱的月桂胺相比,油胺能使ANTS从脂质体中快速释放。使用这些渗透剂时,发现制备的生物脂质体中ANTS的释放程度与大鼠角质层中2920 cm-1附近CH不对称伸缩带频率变化的结果密切相关。由于角质层脂质结构受到扰动,导致ANTS相对较强泄漏的渗透剂会使峰向更高波数显著移动。由大鼠全层皮肤制备的皮肤生物脂质体可用于评估渗透剂。