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脂质纳米粒作为辛甲氧肉桂酸的载体:体外经皮吸收和光稳定性研究。

Lipid nanoparticles as carrier for octyl-methoxycinnamate: in vitro percutaneous absorption and photostability studies.

机构信息

Dipartimento di Scienze del Farmaco, Facoltà di Farmacia, Università di Catania, 95125 Catania, Italy.

出版信息

J Pharm Sci. 2012 Jan;101(1):301-11. doi: 10.1002/jps.22741. Epub 2011 Sep 8.

Abstract

The aim of the present study was the evaluation of lipid nanoparticles (solid lipid nanoparticles, SLN, and nanostructured lipid carriers, NLC) as potential carriers for octyl-methoxycinnamate (OMC). The release pattern of OMC from SLN and NLC was evaluated in vitro, determining its percutaneous absorption through excised human skin. Additional in vitro studies were performed in order to evaluate, after UVA radiation treatment, the spectral stability of OMC-loaded lipid nanoparticles. From the obtained results, ultrasonication method yielded both SLN and NLC in the nanometer range with a high active loading and a particle shape close to spherical. Differential scanning calorimetry data pointed out the key role of the inner oil phase of NLC in stabilizing the particle architecture and in increasing the solubility of OMC as compared with SLN. In vitro results showed that OMC, when incorporated in viscosized NLC dispersions (OMC-NLC), exhibited a lower flux with respect to viscosized SLN dispersions (OMC-SLN) and two reference formulations: a microemulsion (OMC-ME) and a hydroalcoholic gel (OMC-GEL). Photostability studies revealed that viscosized NLC dispersions were the most efficient at preserving OMC from ultraviolet-mediated photodegradation.

摘要

本研究旨在评估脂质纳米粒(固体脂质纳米粒,SLN 和纳米结构化脂质载体,NLC)作为辛基甲氧基肉桂酸(OMC)的潜在载体。通过体外评估 OMC 从 SLN 和 NLC 中的释放模式,测定其经皮吸收。还进行了额外的体外研究,以评估经 UVA 辐射处理后,载有 OMC 的脂质纳米粒的光谱稳定性。从获得的结果来看,超声法在纳米范围内得到了 SLN 和 NLC,具有高活性负载和接近球形的颗粒形状。差示扫描量热法数据指出,NLC 的内油相在稳定颗粒结构和增加 OMC 的溶解度方面起着关键作用,与 SLN 相比。体外结果表明,与增粘 SLN 分散体(OMC-SLN)和两种参考制剂:微乳液(OMC-ME)和水醇凝胶(OMC-GEL)相比,载有 OMC 的增粘 NLC 分散体的通量较低。光稳定性研究表明,增粘 NLC 分散体在保护 OMC 免受紫外介导的光降解方面最为有效。

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