Section of Pharmaceutical Technology, Department of Drug Sciences, University of Catania, Catania, Italy.
Section of Pharmacology and Biochemistry, Department of Clinical and Molecular Biomedicine, School of Medicine, University of Catania, Catania, Italy.
Int J Pharm. 2014 Aug 15;470(1-2):133-40. doi: 10.1016/j.ijpharm.2014.04.061. Epub 2014 May 2.
Addition of one or more surfactant agents is often necessary for the production of nanostructured lipid and polymeric systems. The removal of residual surfactants is a required step for technological and toxicological reasons, especially for peculiar applications, such as the ophthalmic field. This study was planned to assess the technological properties of some surfactants, commonly used for the production of lipid nanoparticles, as well as their ocular safety profile. Stable and small-size solid lipid nanoparticles were obtained using Dynasan(®) 114 as the lipid matrix and all the tested surfactants. However, from a toxicological point of view, the nanocarriers produced using Kolliphor(®) P188 were the most valuable, showing no irritant effect on the ocular surface up to the highest tested surfactant concentration (0.4%, w/v). The SLN produced using Cremophor(®) A25 and Lipoid(®) S100 were tolerated up to a surfactant concentration of 0.2% by weight, while for Tween(®) 80 and Kolliphor(®) HS 15 a maximum concentration of 0.05% can be considered totally not-irritant.
添加一种或多种表面活性剂通常是生产纳米结构脂质和聚合物系统所必需的。出于技术和毒理学原因，特别是对于特殊应用，如眼科领域，去除残留的表面活性剂是必需的步骤。本研究旨在评估一些常用于生产脂质纳米粒子的表面活性剂的技术特性及其眼部安全性特征。使用 Dynasan®114 作为脂质基质和所有测试的表面活性剂，均获得了稳定且粒径较小的固体脂质纳米粒子。然而，从毒理学角度来看，使用 Kolliphor®P188 制备的纳米载体最有价值，在测试的最高表面活性剂浓度（0.4%，w/v）下，对眼表面没有刺激性作用。Cremophor®A25 和 Lipoid®S100 制备的 SLN 在重量为 0.2%的表面活性剂浓度下可耐受，而 Tween®80 和 Kolliphor®HS15 的最大浓度为 0.05%，可认为完全无刺激性。
