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Mussel-Inspired Polydopamine Coating Enhances the Intracutaneous Drug Delivery from Nanostructured Lipid Carriers Dependently on a Follicular Pathway.
Molecular Pharmaceutics ( IF 4.5 ) Pub Date : 2020-03-13 , DOI: 10.1021/acs.molpharmaceut.9b01240
Yang Chen 1 , Xun Feng 2 , Yan Zhao 1 , Xu Zhao 3 , Xiaoyu Zhang 4
Affiliation  

Inspired by the structure and function of the mussel adhesive protein, a facile strategy involving oxidative polymerization of dopamine was proposed for surface modification of nanostructured lipid carriers (NLCs) to promote drug delivery in the skin. The formation of a polydopamine (PDA) layer rounding the surface of NLCs was confirmed by the X-ray photoelectron spectroscopy and the Fourier transform infrared spectroscopy studies. Using terbinafine (TBF) as a model drug, the in vitro permeation study revealed that the PDA coating significantly enhanced the delivery of TBF from NLCs to the deep skin layers, where the follicular pathway played an essential role as suggested by the hair follicle blocking and differential tape stripping experiments, as well as the laser scanning confocal microscopy study by using Nile red as the fluorescent probe. The cellular investigation indicated that the PDA coating led to a higher cellular uptake of nanoparticles in human immortalized keratinocytes (HaCaT) without causing additional cytotoxicity. Using endocytic inhibitors, it was found that the lipid raft/caveolae-mediated endocytosis was strongly involved in the internalization of both the PDA modified and unmodified NLCs. Our results suggested that surface modification of NLCs with PDA coating improved the intracutaneous drug delivery mainly via the follicular pathway, which provided an avenue for the development of potential drug delivery carriers for dermal use.

中文翻译:

贻贝启发的聚多巴胺涂层依赖于卵泡途径增强了从纳米结构脂质载体的皮内药物递送。

受贻贝粘附蛋白的结构和功能的启发,提出了一种涉及多巴胺氧化聚合的简便策略,用于纳米结构脂质载体(NLC)的表面修饰,以促进药物在皮肤中的递送。X射线光电子能谱和傅里叶变换红外光谱研究证实了围绕NLC表面的聚多巴胺(PDA)层的形成。使用特比萘芬(TBF)作为模型药物,在体外渗透研究表明,PDA涂层显着增强了从NLC到深层皮肤的TBF传递,其中毛囊阻塞和差异化胶带剥离实验以及激光扫描共聚焦显微镜表明,卵泡途径起着至关重要的作用。使用尼罗红作为荧光探针进行研究。细胞研究表明,PDA涂层导致人类永生化角质形成细胞(HaCaT)中纳米颗粒的细胞摄取更高,而不会引起额外的细胞毒性。使用内吞抑制剂,发现脂质筏/小窝介导的内吞作用强烈参与了PDA修饰的和未修饰的NLC的内在化。
更新日期:2020-04-24
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