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含神经酰胺的固体脂质纳米粒和纳米乳剂:制备及理化特性研究

Solid lipid nanoparticles and nanoemulsions containing ceramides: preparation and physicochemical characterization.

作者信息

Deli Georgia, Hatziantoniou Sophia, Nikas Yorgos, Demetzos Costas

机构信息

Department of Pharmaceutical Technology, School of Pharmacy, University of Athens, Athens, Greece.

出版信息

J Liposome Res. 2009;19(3):180-8. doi: 10.1080/08982100802702046.

Abstract

Nanoemulsions (NEs) and solid lipid nanoparticles (SLNs) are widely used colloidal carriers for bioactive compounds. They are used in therapeutic, diagnostic, and cosmetic formulations. Ceramides are main components of the stratum corneum and are essential for the efficient barrier function. Their very high lipophilicity renders them difficult to incorporate in an acceptable formulation. The aim of this work was to investigate the possibility of using the benefits of nanotechnology in the efficient topical delivery of ceramides formulated as NEs or SLNs. The physicochemical characteristics of such carriers incorporating ceramides were investigated and their stability over time was assessed. Their morphology was examined under a scanning electron microscope and the interactions of their components were studied by differential scanning calorimetry. The results showed that the nanoemulsions can incorporate a high percentage (48.4% of total lipids by weight) of ceramides giving more homogeneous particle distributions of spherical-shaped nanoparticles and they maintained their characteristics over time. On the contrary, SLNs' incorporation of ceramide higher than 10.8% of total lipids by weight led to the formation of rod-like nanoparticles deteriorating the homogeneity of the particle distribution, as depicted on the high polydispersity indexes of the corresponding formulations. The results demonstrate that NEs may be the more suitable carrier, compared to SLNs.

摘要

纳米乳剂(NEs)和固体脂质纳米粒(SLNs)是生物活性化合物广泛使用的胶体载体。它们用于治疗、诊断和化妆品配方中。神经酰胺是角质层的主要成分,对于有效的屏障功能至关重要。其极高的亲脂性使其难以纳入可接受的配方中。这项工作的目的是研究利用纳米技术的优势实现神经酰胺以纳米乳剂或固体脂质纳米粒形式高效局部递送的可能性。研究了包含神经酰胺的此类载体的物理化学特性,并评估了它们随时间的稳定性。在扫描电子显微镜下检查其形态,并通过差示扫描量热法研究其成分之间的相互作用。结果表明,纳米乳剂可以包含高百分比(按重量计占总脂质的48.4%)的神经酰胺,使球形纳米颗粒的颗粒分布更均匀,并且它们随时间保持其特性。相反,固体脂质纳米粒中神经酰胺的掺入量高于按重量计占总脂质的10.8%会导致形成棒状纳米颗粒,从而恶化颗粒分布的均匀性,如相应配方的高多分散指数所示。结果表明,与固体脂质纳米粒相比,纳米乳剂可能是更合适的载体。

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