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用于局部给药的基于硅酮和表面活性剂的系统的设计与表征

Design and Characterization of Silicone and Surfactant Based Systems for Topical Drug Delivery.

作者信息

Oyafuso Márcia Helena, Carvalho Flávia Chiva, Chiavacci Leila Aparecida, Gremião Maria Palmira Daflon, Chorilli Marlus

出版信息

J Nanosci Nanotechnol. 2015 Jan;15(1):817-26. doi: 10.1166/jnn.2015.9181.

DOI:10.1166/jnn.2015.9181
PMID:26328446
Abstract

Nanotechnology offers advantages for new drug delivery design by providing drug targeting while minimizing the side effects. Polyoxyethylene 20 cetyl alcohol (CETETH-20) is a surfactant that may form nanostructured systems, such as liquid crystals, when in contact with water/oil, which are structurally similar to biological membranes and may improve skin interaction. The aim of this study was to develop and characterize CETETH 20-based nanostructured systems by combining CETETH-20 with water and different oily phases, including PEG-12-dimethicone for topical drug administration. The systems were characterized by polarized light microscopy (PLM), small-angle X-ray scattering (SAXS), rheology, texture profile analyses (TPA), in vitro cytotoxicity and histopathological analyses of rabbits' skin. Lamellar, hexagonal and cubic phases were identified and their viscoelastic moduli varied according to each phase. The stiffness of the cubic phase was 3-fold higher and twice more adhesive than the hexagonal phase. The formulations did not affect the normal macrophages cells, neither promoted skin irritation. They were spontaneously obtained by simply mixing the components, which corroborates for an ease scaled-up. These results suggest that systems composed of CETETH 20, PEG-12-dimethicone and water are a promising new approach for designing nanostructured topical drug delivery systems.

摘要

纳米技术通过实现药物靶向并将副作用降至最低,为新型药物递送设计带来了优势。聚氧乙烯20鲸蜡醇(CETETH - 20)是一种表面活性剂,当与水/油接触时,它可能形成纳米结构体系,如液晶,其结构与生物膜相似,可能改善与皮肤的相互作用。本研究的目的是通过将CETETH - 20与水和不同的油相(包括用于局部给药的PEG - 12 - 二甲基硅氧烷)相结合,开发并表征基于CETETH 20的纳米结构体系。通过偏光显微镜(PLM)、小角X射线散射(SAXS)、流变学、质地剖面分析(TPA)、体外细胞毒性以及兔皮肤组织病理学分析对这些体系进行了表征。鉴定出了层状、六方和立方相,并且它们的粘弹性模量根据各相而有所不同。立方相的硬度比六方相高3倍,粘性是六方相的两倍。这些制剂既不影响正常巨噬细胞,也不会引起皮肤刺激。它们通过简单混合各组分即可自发获得,这证实了其易于放大生产。这些结果表明,由CETETH 20、PEG - 12 - 二甲基硅氧烷和水组成的体系是设计纳米结构局部药物递送系统的一种有前景的新方法。

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