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基于脂质和聚合物的纳米结构用于姜黄素的经皮传递。

Lipid- and Polymer-Based Nanostructures for Cutaneous Delivery of Curcumin.

机构信息

Laboratório de Controle de Qualidade, Programa de Pós-Graduação em Farmácia, Departamento de Ciências Farmacêuticas, Universidade Federal de Santa Catarina (UFSC), Campus Universitário, Trindade, 88040-900, Florianópolis, SC, Brazil.

Laboratório de Farmacotécnica e Cosmetologia, Programa de Pós-Graduação em Farmácia, Departamento de Ciências Farmacêuticas, Universidade Federal de Santa Catarina (UFSC), Campus Universitário, Trindade, 88040-900, Florianópolis, SC, Brazil.

出版信息

AAPS PharmSciTech. 2017 Apr;18(3):920-925. doi: 10.1208/s12249-016-0554-7. Epub 2016 May 26.

Abstract

It is well-known that nanoencapsulation may overcome biopharmaceutical limitations of curcumin (CUR), but studies regarding the contribution of the vesicular nature of CUR-loaded nanoparticles on skin permeation are still scarce. Therefore, the effect of three colloidal systems (solid lipid nanoparticles (SLN), nanoemulsion (NE), and polymeric nanoparticles (NP)) on the control of cutaneous permeation of CUR was investigated in porcine ear skin/Franz diffusion cells. Colloidal suspensions were designed to present a similar particle size (±170 nm), narrow size distribution (PdI < 0.2), and high entrapment efficiency (>99%). Zeta potential values were -0.13, -9.68 and -36.7 mV for the CUR-loaded NP, SLN and NE, respectively. Nanoencapsulation resulted in a cumulative amount of CUR in the more superficial layers of the skin. NP significantly enhanced the compound retention in the epidermis, which was approximately 2.49- and 3.32-fold more than SLN and NE, respectively. The CUR levels into the dermis were significantly increased after treatment with NE, which may be associated with repulsion phenomena in surface skin. Therefore, a more superficial or deeper action of CUR on the skin may be obtained depending on nanostructure type. While NPs are more effective in upper skin layers, NE should be prioritized when a dermal action for the CUR is required.

摘要

众所周知,纳米封装可以克服姜黄素(CUR)的生物制药局限性,但关于载有 CUR 的纳米粒子的囊泡性质对皮肤渗透的贡献的研究仍然很少。因此,在猪耳朵皮肤/Franz 扩散细胞中研究了三种胶体系统(固体脂质纳米粒子(SLN)、纳米乳液(NE)和聚合物纳米粒子(NP))对 CUR 经皮渗透的控制作用。胶体悬浮液的设计旨在具有相似的粒径(±170nm)、较窄的粒径分布(PdI<0.2)和高包封效率(>99%)。载有 CUR 的 NP、SLN 和 NE 的 Zeta 电位值分别为-0.13、-9.68 和-36.7mV。纳米封装导致 CUR 在皮肤更浅层的累积量增加。NP 显著增加了化合物在表皮中的保留量,分别比 SLN 和 NE 高约 2.49 倍和 3.32 倍。经 NE 处理后,CUR 进入真皮的水平显著增加,这可能与表面皮肤的排斥现象有关。因此,根据纳米结构类型,CUR 对皮肤的作用可能更表浅或更深。虽然 NPs 在较浅层皮肤中更有效,但当需要 CUR 对真皮的作用时,应优先考虑 NE。

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