Department of Pharmacy Sciences, School of Pharmacy & Health Professions, Creighton University, 2500 California Plaza, Omaha, NE 68178, USA.
Nanomedicine (Lond). 2012 Dec;7(12):1863-76. doi: 10.2217/nnm.12.49. Epub 2012 Jun 18.
The objective of this study was to investigate the influence of the high-pressure homogenization (HPH) process and stabilizers on the physicochemical properties of glycerol monooleate (GMO)/chitosan nanostructures using curcumin as a model hydrophobic drug.
MATERIALS & METHODS: The oil-in-water nanoemulsion of the GMO/chitosan system was prepared by sonication and HPH techniques using two different stabilizers (polyvinyl alcohol [PVA] and poloxamer 407). The particle size (PS), ζ-potential (ZP) and physical stability of the nanoemulsion were investigated. These nanoemulsions were lyophilized and characterized for PS, ZP, surface morphology, moisture content and physical form of the drug in the nanostructures. The in vitro release and the uptake of curcumin in Caco-2 cells were evaluated using an ultra-performance liquid chromatography method.
Three cycles of HPH produced a 50-65% reduction in the PS of the nanoemulsion. A change in stabilizer, from PVA to poloxamer, did not affect the PS, physical stability, moisture content or the physical form of the drug in the formulation. However, there was a significant change in the ZP, surface morphology, in vitro release rate and cellular uptake from the two formulations.
The process of HPH effectively reduces the PS of the GMO/chitosan nanoemulsions loaded with the hydrophobic drug. The type of stabilizer used affects several physicochemical properties of the GMO/chitosan nanostructures. Compared with PVA, poloxamer 407 is a more effective stabilizer for stabilizing the GMO/chitosan system containing a hydrophobic drug nanoemulsion at low concentrations.
本研究旨在研究高压均质(HPH)工艺和稳定剂对甘油单油酸酯(GMO)/壳聚糖纳米结构的物化性质的影响,所用模型疏水性药物为姜黄素。
采用超声和 HPH 技术,使用两种不同稳定剂(聚乙烯醇[PVA]和泊洛沙姆 407)制备 GMO/壳聚糖体系的油包水纳米乳液。考察纳米乳液的粒径(PS)、ζ-电位(ZP)和物理稳定性。对纳米乳液进行冷冻干燥,并对冻干物的 PS、ZP、表面形态、药物在纳米结构中的水分含量和物理形式进行表征。采用超高效液相色谱法评价姜黄素的体外释放和在 Caco-2 细胞中的摄取。
HPH 处理 3 个循环可使纳米乳液的 PS 降低 50%-65%。改变稳定剂从 PVA 变为泊洛沙姆 407 并不影响 PS、物理稳定性、水分含量或制剂中药物的物理形式。然而,两种制剂的 ZP、表面形态、体外释放速率和细胞摄取均发生了显著变化。
HPH 工艺可有效降低载有疏水性药物的 GMO/壳聚糖纳米乳液的 PS。所使用的稳定剂类型会影响 GMO/壳聚糖纳米结构的几种物化性质。与 PVA 相比,泊洛沙姆 407 是一种更有效的稳定剂,可在低浓度下稳定含有疏水性药物纳米乳液的 GMO/壳聚糖体系。