Pena-Rodríguez Eloy, Lajarin-Reinares Maria, Mata-Ventosa Aida, Pérez-Torras Sandra, Fernández-Campos Francisco
Topical & Oral Development R+D Reig Jofre Laboratories, 08970 Barcelona, Spain.
Molecular Pharmacology and Experimental Therapeutics, Department of Biochemistry and Molecular Biomedicine, Institute of Biomedicine (IBUB), University of Barcelona, 08028 Barcelona, Spain.
Pharmaceutics. 2021 Apr 11;13(4):533. doi: 10.3390/pharmaceutics13040533.
Follicular targeting has gained more attention in recent decades, due to the possibility of obtaining a depot effect in topical administration and its potential as a tool to treat hair follicle-related diseases. Lipid core ethyl cellulose lipomers were developed and optimized, following which characterization of their physicochemical properties was carried out. Dexamethasone was encapsulated in the lipomers (size, 115 nm; polydispersity, 0.24; zeta-potential (Z-potential), +30 mV) and their in vitro release profiles against dexamethasone in solution were investigated by vertical diffusion Franz cells. The skin biodistribution of the fluorescent-loaded lipomers was observed using confocal microscopy, demonstrating the accumulation of both lipomers and fluorochromes in the hair follicles of pig skin. To confirm this fact, immunofluorescence of the dexamethasone-loaded lipomers was carried out in pig hair follicles. The anti-inflammatory (via TNFα) efficacy of the dexamethasone-loaded lipomers was demonstrated in vitro in an HEK001 human keratinocytes cell culture and the in vitro cytotoxicity of the nanoformulation was investigated.
近几十年来，毛囊靶向受到了更多关注，这是因为在局部给药中有可能获得长效缓释效果，并且它作为治疗毛囊相关疾病的工具具有潜力。脂质核乙基纤维素脂质体得到了开发和优化，随后对其理化性质进行了表征。将地塞米松包封在脂质体中（尺寸为115纳米；多分散性为0.24；ζ电位（Z电位）为+30毫伏），并通过垂直扩散弗兰兹细胞研究其相对于溶液中地塞米松的体外释放曲线。使用共聚焦显微镜观察了负载荧光的脂质体在皮肤中的生物分布，证明脂质体和荧光染料在猪皮肤的毛囊中积累。为了证实这一事实，在猪毛囊中进行了负载地塞米松脂质体的免疫荧光实验。在HEK001人角质形成细胞培养物中体外证明了负载地塞米松脂质体的抗炎（通过肿瘤坏死因子α）功效，并研究了该纳米制剂的体外细胞毒性。
