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首页> 外文期刊>International Journal of Pharmaceutics >Optimization of linalool-loaded solid lipid nanoparticles using experimental factorial design and long-term stability studies with a new centrifugal sedimentation method
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Optimization of linalool-loaded solid lipid nanoparticles using experimental factorial design and long-term stability studies with a new centrifugal sedimentation method

机译：用实验阶乘设计和长期稳定性研究用新型离心沉降法优化Linalool加载的固体脂质纳米粒子

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摘要

Linalool (C10H18O), also known as 3, 7-dimethyl-1, 6-octadien-3-ol, is the most common acyclic monoterpene tertiary alcohol present in essential oils of several aromatic plant species. Previous studies indicate that linalool is a valuable compound with a wide range of therapeutic properties. The promising therapeutic effects of linalool are however limited by its poor water solubility and volatility. Recently, the encapsulation of linalool in drug delivery systems, such as solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) has demonstrated to overcome linalool physicochemical limitations.The present study aimed the production and optimization of linalool encapsulation in SLN applying the experimental full factorial design. The estimation of the long-term stability of the produced linalool-loaded SLN was carried out using a new centrifugal sedimentation method, LUMiSizer?. SLN dispersions were produced by the hot high pressure homogenization (HPH) method. The influence of the independent variables, surfactant and lipid concentrations on linalool-loaded SLN particle size, polydispersity index (PI) and zeta potential (ZP) was evaluated by a 22factorial design composed of 2 variables which were set at 2-levels each. For each of the three dependent variables, analysis of the variance (ANOVA) was performed using a 95% confidence interval. The concentration of surfactant, as well as, the interaction between the different concentrations of lipid and surfactant, hada statistically significant effect on the particle size and PI. Experimental factorial design has been successfully employed to develop an optimal SLN dispersion, requiring a minimum of performed experiments. Based on the obtained results, the optimal linalool-loaded SLN dispersion was composed of 1% (w/v) linalool 2% (w/v) of solid lipid and 5% (w/v) of surfactant. Furthermore, the stability analysis revealed that the produced linalool-loaded SLN dispersions have limited storage stability which can be easily overcome through the assembly of a polymeric coating on the SLN surface. LUMiSizer? has been successfully used in the kinetic analysis of linalool-SLN during accelerated storage time.
机译：Linalool（C10H18O），也称为3,7-二甲基-1,6-十八碳基-3-醇，是存在于几种芳香植物物种的精油中的最常见的无循环单萜叔醇。以前的研究表明，Linalool是一种有价值的化合物，具有各种治疗性质。然而，LINALOOL的有希望的治疗效果受其不良水溶解度和挥发性的限制。最近，在药物递送系统中的LINALOOL封装，例如固体脂质纳米颗粒（SLN）和纳米结构脂质载体（NLC）已经证明克服LILLOOL物理化学限制。目前的研究旨在应用实验的SLN中的LINALOOL封装的生产和优化完整的因素设计。使用新的离心沉降法，Lumisizer估算所生产的裂解机加载的SLN的长期稳定性的估计。通过热高压均化（HPH）方法产生SLN分散体。由22因素设计评估了独立变量，表面活性剂和脂质浓度对Linalool负载的SLN粒度，多分散性指数（PI）和Zeta电位（ZP）的影响，由2个变量组成，每个设计组成，每个设计都设置为2级。对于三个相关变量中的每一个，使用95％置信区间进行方差（ANOVA）的分析。表面活性剂的浓度，以及不同浓度的脂质和表面活性剂之间的相互作用，对粒径和Pi的统计显着作用。实验阶乘设计已成功用于开发最佳的SLN色散，需要最小的执行实验。基于所得到的结果，最佳的芳樟醇加载的SLN分散液由1％（W / V）芳樟醇2％（W ​​/ V）的固体脂质和5％的（重量/体积）表面活性剂。此外，稳定性分析表明，所产生的Linalool负载的SLN分散体具有有限的储存稳定性，该储存稳定性通过组装在SLN表面上的聚合物涂层可以容易地克服。 Lumisizer？已成功用于加速储存时间的LINALOOL-SLN的动力学分析。

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