Center for Pharmaceutical Studies, Faculty of Pharmacy, University of Coimbra, Pólo das Ciências da Saúde, Coimbra, Portugal.
Colloids Surf B Biointerfaces. 2011 May 1;84(1):117-30. doi: 10.1016/j.colsurfb.2010.12.024. Epub 2010 Dec 24.
This study aimed to investigate the role of different factors affecting the size of solid lipid nanoparticles (SLN), prepared by the emulsification-solvent evaporation method. A double factorial design was conducted so as to cover a wide range of sizes, highlighting zones with different behaviour with respect to changes in the controlled variables: lipid concentration, solvent:lipid ratio and emulsifier concentration. The solvent:lipid ratio constituted the main factor influencing particle size. Increasing the amount of solvent induced a decrease in the size. This was a general trend, essentially independent from solvent and lipid type. The amount of emulsifier had a non-trivial impact on size, depending on whether systems were located below, above or close to the optimal surface coverage. The amount of lipid had a limited influence upon particle size, being more relevant for lower lipid concentrations. An optimal formulation was selected for intermediate levels of the three variables. Sonication reduced both particle size and polydispersity. These particles were also tested as drug carriers using simvastatin as a model of lipophilic drug. SLN were able to entrap a high amount of simvastatin, with little effect upon size and zeta potential, constituting a promising carrier for lipophilic drugs.
本研究旨在探讨影响固体脂质纳米粒(SLN)大小的不同因素的作用,这些纳米粒是通过乳化-溶剂蒸发法制备的。采用双因素设计,以便涵盖广泛的粒径范围,突出不同行为区域相对于控制变量变化的行为:脂质浓度、溶剂:脂质比和乳化剂浓度。溶剂:脂质比对粒径有主要影响。增加溶剂的量会导致粒径减小。这是一种普遍趋势,基本上与溶剂和脂质类型无关。乳化剂的量对粒径有重要影响,这取决于系统是位于最佳表面覆盖层以下、以上还是接近最佳表面覆盖层。脂质的量对粒径的影响有限,对于较低的脂质浓度更为相关。选择了一个用于三个变量中间水平的最佳配方。超声处理降低了粒径和多分散性。还使用辛伐他汀作为亲脂性药物的模型来测试这些颗粒作为药物载体的能力。SLN 能够包封大量的辛伐他汀,对粒径和 Zeta 电位几乎没有影响,是一种有前途的亲脂性药物载体。