Department of Pharmaceutical Technology, National Research Center , Cairo , Egypt .
Pharm Dev Technol. 2014 May;19(3):304-14. doi: 10.3109/10837450.2013.778872. Epub 2013 Mar 26.
OBJECTIVE: The aim of this study was to develop nanostructured lipid carriers (NLCs) as well as solid lipid nanoparticles (SLNs) and evaluate their potential in the topical delivery of meloxicam (MLX). MATERIALS AND METHODS: The effect of various compositional variations on their physicochemical properties was investigated. Furthermore, MLX-loaded lipid nanoparticles-based hydrogels were formulated and the gels were evaluated as vehicles for topical application. RESULTS AND DISCUSSION: The results showed that NLC and SLN dispersions had spherical shapes with an average size between 215 and 430 nm. High entrapment efficiency was obtained ranging from 61.94 to 90.38% with negatively charged zeta potential in the range of -19.1 to -25.7 mV. The release profiles of all formulations exhibited sustained release characteristics over 48 h and the release rates increased as the amount of liquid lipid in lipid core increased. Finally, Precirol NLC with 50% Miglyol® 812 and its corresponding SLN were incorporated in hydrogels. The gels showed adequate pH, non-Newtonian flow with shear-thinning behavior and controlled release profiles. The biological evaluation revealed that MLX-loaded NLC gel showed more pronounced effect compared to MLX-loaded SLN gel. CONCLUSION: It can be concluded that lipid nanoparticles represent promising particulate carriers for topical application.
目的:本研究旨在开发纳米结构化脂质载体(NLC)和固体脂质纳米粒(SLN),并评估其在局部递送美洛昔康(MLX)中的潜力。
材料和方法:研究了各种组成变化对其物理化学性质的影响。此外,还制备了载有 MLX 的基于脂质纳米粒子的水凝胶,并将其作为局部应用的载体进行了评估。
结果与讨论:结果表明,NLC 和 SLN 分散体具有球形形状,平均粒径在 215 至 430nm 之间。包封效率高,范围为 61.94%至 90.38%,带负电荷的 Zeta 电位在-19.1 至-25.7mV 范围内。所有制剂的释放曲线均表现出 48 小时以上的持续释放特征,随着脂质核中液体脂质含量的增加,释放速率增加。最后,将含有 50%Precirol NLC 和 50%Miglyol®812 的 NLC 及其相应的 SLN 掺入水凝胶中。凝胶具有合适的 pH 值、非牛顿流动和剪切稀化行为以及控制释放曲线。生物学评价表明,载有 MLX 的 NLC 凝胶的效果比载有 MLX 的 SLN 凝胶更为明显。
结论:可以得出结论,脂质纳米粒是一种很有前途的局部应用的微粒载体。
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