Innovative liposomes as a transfollicular drug delivery system: Penetration into porcine hair follicles

Innovative liposomes as a transfollicular drug delivery system: Penetration into porcine hair follicles
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DOI:
10.1038/sj.jid.5700323
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发表时间:
2006-08-01
影响因子:
6.5
通讯作者:
Lademann, Juergen
Lademann, Juergen
中科院分区:
医学1区
文献类型:
--
作者:
Jung, Sascha;Otberg, Nina;Lademann, Juergen

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脂质体在过去曾被广泛用于药物输送。在本研究中,五种不同的脂质体被用作猪耳皮肤的毛囊给药系统。脂质体主要在球径、脂类组成和表面电荷方面有所不同。一类新型的两性脂质体的电荷行为与已有的阴离子和阳离子脂质体进行了比较。将两种不同的荧光染料--亲水性羧基荧光素或亲脂性姜黄素包裹在脂质体中,作为模型药物。荧光染料也被应用在标准配方中以供参考。用激光扫描显微镜在组织切片上测量染料的穿透深度。分别于用药后1小时、3天、5天和7天取材,纵向切片测量毛囊的穿透深度。与标准制剂相比,脂质体具有更高的渗透深度。在整个观察期内,标准配方中使用的染料的相对渗透深度平均为整个毛囊长度的30%,而脂质体配方对毛囊的渗透要深得多。两性和阳离子脂质体的平均相对渗透深度约为整个毛囊长度的70%。
Liposomes had been widely used for drug delivery in the past. In this study, five different liposomes were used as a follicular delivery system in pig ear skin. The liposomes mainly differed in their sphere diameter, lipid composition, and surface charge. A novel class of liposomes being amphoteric in their charge behavior are compared to established anionic and cationic liposomes. Two different fluorescent dyes, hydrophilic carboxyfluoresceine or lipophilic curcumin, were enclosed in the liposomes and used as model drugs. The fluorescent dyes were also applied in a standard formulation for reference. The penetration depth of the dyes was measured by laser scanning microscopy in histological sections. One hour, 3, 5, and 7 days after application, biopsies were taken and the penetration depth into the hair follicle was measured in longitudinal sections. The liposomes showed a higher penetration depth compared to the standard formulation. The relative penetration depth of the dyes, applied in the standard formulation, averaged 30% of the full follicle length during the whole observation period, whereas the liposomal formulations penetrated considerably deeper into the hair follicles. Amphoteric and cationic liposomes reached an average relative penetration depth of approximately 70% of the full hair follicle length.