Quantitative assessment of the transport of elastic and rigid vesicle components and a model drug from these vesicle formulations into human skin in vivo
Quantitative assessment of the transport of elastic and rigid vesicle components and a model drug from these vesicle formulations into human skin in vivo
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DOI：
10.1111/j.0022-202x.2004.23441.x
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发表时间：
2004-11-01
影响因子：
6.5
通讯作者：
Bouwstra, JA
中科院分区：
文献类型：
--
作者：
Honeywell-Nguyen, PL;Gooris, GS;Bouwstra, JA
本研究的目的是定量评估弹性和刚性水泡材料在人体皮肤中的分布情况。此外，还考察了模型药物酮咯酸在这些囊泡剂中的分布情况。在这些囊泡中掺入一种标记了氚的磷脂，作为囊泡材料的标记。囊泡中装入饱和浓度的酮咯酸。将水泡溶液非闭塞地涂抹在皮肤上，并按顺序剥离治疗部位。用衰减全反射傅里叶变换红外光谱分析胶条中的囊泡物质，并通过提取胶条和高压液相色谱来分析酮咯酸。获得了弹性囊泡材料和刚性囊泡材料以及酮咯酸在角质层(SC)的分布情况。这些分布表明，弹性囊泡材料可以迅速进入SC的更深层，并可以到达几乎可存活的SC-表皮连接处。然而，硬泡材料并没有深入到SC中。此外，弹性囊泡在促进酮咯酸在人体SC中的转运方面优于刚性囊泡。然而，酮咯酸在SC深层的分布与囊泡物质的分布不同。这表明，一旦弹性囊泡进入SC，酮咯酸就从囊泡中释放出来。无论是在囊泡进入SC的运输方面，还是在作为皮肤输送载体的治疗潜力方面，弹性囊泡都优于刚性囊泡。
The aim of this study was to quantitatively assess the distribution profiles of elastic and rigid vesicle material in human skin in vivo. Furthermore, the distribution profiles of the model drug ketorolac applied in these vesicle formulations was investigated. A deuterium-labelled phospholipid was incorporated into these vesicles to serve as a marker for the vesicle material. The vesicles were loaded with ketorolac at saturated concentrations. Vesicle solutions were applied non-occlusively onto the skin and the treated site was sequentially tape-stripped. Tape-strips were analyzed for vesicle material using attenuated total reflectance-Fourier transform infrared spectroscopy and for ketorolac by extraction of the tape-strips followed by high pressure liquid chromatography. Distribution profiles in the stratum corneum (SC) were obtained for the elastic and rigid vesicle material and for the ketorolac. These profiles have suggested that elastic vesicle material can rapidly enter the deeper layers of the SC and can reach almost the SC-viable epidermal junction. Rigid vesicle material, however, did not penetrate deep into the SC. Furthermore, the elastic vesicles were better than the rigid vesicles in the enhancement of ketorolac transport into human SC. The distribution profile of ketorolac in the deeper SC layers was, however, different from that of the vesicle material. This suggests that once the elastic vesicles partition into the SC, the ketorolac is released from the vesicles. The elastic vesicles are superior to the rigid vesicles both in terms of vesicular transport into the SC and in terms of therapeutic potential as a skin delivery vehicle.