Grams Ylva Y, Alaruikka Soile, Lashley Lisa, Caussin Julia, Whitehead Lynne, Bouwstra Joke A
Leiden/Amsterdam Center for Drug Research, Department of Pharmaceutical Technology, Leiden University, P.O. Box 9502, Einsteinweg 55, 2300 RA Leiden, The Netherlands.
Eur J Pharm Sci. 2003 Apr;18(5):329-36. doi: 10.1016/s0928-0987(03)00035-6.
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 Green 488, Bodipy FL C(5) or Bodipy 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 Green 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 FL C(5) and Bodipy 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.
在皮肤和毛发研究中，靶向毛囊的药物备受关注。因此，使用共聚焦激光扫描显微镜（CLSM）研究了渗透剂亲脂性和载体组成对局部蓄积的影响。制备了用俄勒冈绿488、Bodipy FL C(5)或Bodipy 564/570 C(5)饱和的制剂。染料分别应用于柠檬酸缓冲液、含8%（w/v）表面活性剂的柠檬酸缓冲液或含8%（w/v）表面活性剂/20%（w/v）丙二醇的柠檬酸缓冲液中。对新鲜的人头皮皮肤进行流通扩散实验，之后用CLSM对皮肤成像。扩散研究表明，对于俄勒冈绿488（亲脂性低），与表面活性剂相比，应用于柠檬酸缓冲液时通量更高。相反，对于亲脂性更强的染料（Bodipy FL C(5)和Bodipy 564/570 C(5)），应用于表面活性剂/丙二醇时通量最高。CLSM研究表明，（i）亲脂性染料和（ii）在表面活性剂 - 丙二醇中应用亲脂性染料时，毛囊蓄积增加。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联合使用，可以增加对毛囊的靶向性。
