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首页> 外文期刊>Journal of Controlled Release: Official Journal of the Controlled Release Society >Lipid nanoparticles for skin penetration enhancement-correlation to drug localization within the particle matrix as determined by fluorescence and parelectric spectroscopy
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Lipid nanoparticles for skin penetration enhancement-correlation to drug localization within the particle matrix as determined by fluorescence and parelectric spectroscopy

机译：脂质纳米颗粒，用于皮肤渗透增强，与药物在颗粒基质内的定位相关（通过荧光和电镜确定）

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With topical treatment of skin diseases, the requirement of a high and reproducible drug uptake often still is not met. Moreover, drug targeting to specific skin strata may improve the use of agents which are prone to cause local unwanted effects. Recent investigations have indicated that improved uptake and skin targeting may become feasible by means of nanoparticular systems such as solid lipid nanoparticles (SLN), nanostructured lipid carriers (NLC) and nanoemulsions (NE). Here we describe techniques to characterize drug loading to carrier systems and skin penetration profiles by using the lipophilic dye nile red as a model agent. Since the mode of drug association with the particle matrix may strongly influence the efficiency of skin targeting, parelectric spectroscopy (PS) was used to differentiate between matrix incorporation and attachment to the particle surface and fluorescence spectroscopy (FS) to solve dye distribution within NLC particles. Nile red was incorporated into the lipid matrix or the covering tensed shell, respectively, of SLN and NLC with all the lipids studied (Compritol, Precirol, oleic acid, Miglyol). In NLC, the dye was enriched in the liquid phase. Next, nile red concentrations were followed by image analysis of vertical sections of pigskin treated with dye-loaded nanoparticular dispersions and an oil-in-water cream for 4 and 8 h in vitro. Following the SLN dispersions, dye penetration increased about fourfold over the uptake obtained following the cream. NLC turned out less potent (< threefold increase) and penetration appeared even reduced when applying a NE. In contrast to previous studies with glucocorticoids attached to the surface of SLN, a targeting effect was not detected here. Therefore, drug targeting appears to be more strictly related to the mode of interaction of drug and particle than penetration enhancement. (c) 2005 Elsevier B.V. All rights reserved.
机译：通过皮肤疾病的局部治疗，常常仍不能满足对高且可再现的药物吸收的要求。而且，针对特定皮肤层的药物靶向可改善易于引起局部不良作用的药物的使用。最近的研究表明，借助于纳米颗粒系统，例如固体脂质纳米颗粒（SLN），纳米结构脂质载体（NLC）和纳米乳剂（NE），改善摄取和靶向皮肤可能变得可行。在这里，我们描述了通过使用亲脂性染料尼罗红作为模型剂来表征载药到载体系统和皮肤渗透曲线的技术。由于药物与颗粒基质缔合的模式可能会强烈影响皮肤靶向的效率，因此使用了介电谱（PS）来区分基质掺入和与颗粒表面的附着以及荧光光谱（FS），以解决NLC颗粒内的染料分布。将尼罗红与所有研究过的脂质（Compritol，Precirol，油酸，Miglyol）分别掺入SLN和NLC的脂质基质或覆盖张紧的壳中。在NLC中，染料在液相中富集。接下来，在尼罗红浓度之后，对用染料加载的纳米颗粒分散体和水包油乳膏处理的猪皮的垂直切片进行体外4和8小时的图像分析。在SLN分散液之后，染料渗透率比乳霜后的吸收率高出约四倍。当使用NE时，NLC的效力降低（<三倍增加），渗透力甚至降低。与先前将糖皮质激素附着在SLN表面的研究相比，此处未检测到靶向作用。因此，靶向药物似乎比渗透增强更严格地与药物和颗粒的相互作用方式相关。 （c）2005 Elsevier B.V.保留所有权利。

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