Permeant lipophilicity and vehicle composition influence accumulation of dyes in hair follicles of human skin
Permeant lipophilicity and vehicle composition influence accumulation of dyes in hair follicles of human skin
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DOI：
10.1016/s0928-0987(03)00035-6
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发表时间：
2003-04-01
影响因子：
4.6
通讯作者：
Bouwstra, JA
中科院分区：
文献类型：
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作者：
Grams, YY;Alaruikka, S;Bouwstra, JA
在皮肤和毛发研究中，以毛囊为靶点的药物引起了极大的兴趣。因此，使用共聚焦激光扫描显微镜（CLSM）检查了渗透性亲脂性和溶媒组成对局部蓄积的影响。制备用俄勒冈州格林488（（R））Bodipy（（R））FL C-5或Bodipy（（R））564/570 C-5饱和的制剂。将染料施加在柠檬酸缓冲液、柠檬酸缓冲液中的8%（w/v）表面活性剂或柠檬酸缓冲液中的8%（w/v）表面活性剂/20%（w/v）丙二醇中。用新鲜的人头皮皮肤进行流通扩散实验，之后使用CLSM对皮肤进行成像。扩散研究表明，与表面活性剂相比，俄勒冈州格林488（低亲脂性）在柠檬酸缓冲液中应用时具有更高的通量。相比之下，更亲脂的染料（Bodipy（（R））FL C-5和Bodipy（（R））564/570 C-5）的通量当在表面活性剂/丙二醇中应用时最高。CLSM研究表明，卵泡积累增加与（i）亲脂性染料和（ii）应用亲脂性染料的表面活性剂-丙二醇。因此，我们得出结论，通过使用亲脂性药物与表面活性剂溶液和丙二醇的组合，可以增加对毛囊的靶向。(C)2003 Elsevier Science B. V.保留所有权利。
In skin and hair research drug targeting to the hair follicle is of great interest. Therefore the influence of permeant lipophilicity and vehicle composition on local accumulation has been examined using confocal laser scanning microscopy (CLSM). Formulations saturated with either Oregon Greene 488((R)) Bodipy((R)) FL C-5 or Bodipy((R)) 564/570 C-5 were prepared. The dyes were applied in citric acid buffer, 8% (w/v) surfactants in citric acid buffer or 8% (w/v) surfactants/20% (w/v) propylene glycol in citric acid buffer. Flow-through diffusion experiments were performed with fresh human scalp skin, after which the skin was imaged using CLSM. Diffusion studies showed for Oregon Greene 488 (low lipophilicity) a higher flux when applied in citric acid buffer compared to surfactants. In contrast the fluxes of the more lipophilic dyes (Bodipy((R)) FL C-5 and Bodipy((R)) 564/570 C-5) are highest when applied in surfactants/propylene glycol. CLSM studies revealed that follicular accumulation increased with (i) a lipophilic dye and (ii) application of lipophilic dyes in surfactants-propylene glycol. Therefore we conclude that targeting to the hair follicle can be increased by the use of lipophilic drugs in combination with surfactant solutions and propylene glycol. (C) 2003 Elsevier Science B.V. All rights reserved.