Department of Pharmacy Sciences, School of Pharmacy & Health Professions, Creighton University, 2500 California Plaza, Omaha, NE 68178, USA.
Nanomedicine (Lond). 2011 Oct;6(8):1397-412. doi: 10.2217/nnm.11.57.
The present research focuses on the development of the surface modified solid lipid nanoparticulate (SLN) system for enhancing the stability and sustaining the release of a model hydrophilic drug ifosfamide.
MATERIALS & METHODS: SLNs consisting of glyceryl monooleate (GMO) and chitosan were prepared by double emulsion technique, crosslinked with sodium tripolyphosphate, followed by lyophilization under two different vacuum conditions. The physicochemical characterization of SLNs included evaluation of surface morphology, particle size and surface charge, moisture content and physical state of the drug in the delivery system. The in vitro drug release and the stability were evaluated using high-performance liquid chromatography and liquid chromatography/mass spectrometry, respectively. Cellular permeability and subcellular localization studies were performed using Caco-2 cells.
Different chamber pressures during lyophilization produced SLNs with different morphologies and moisture contents. SLNs demonstrated high encapsulation efficiency, sustained release, and enhanced stability of ifosfamide with a high cellular uptake and permeability for Caco-2 cells.
GMO and chitosan SLNs could be successfully used for enhancing the stability, sustaining the release, enhancing the targeting and permeability characteristics of ifosfamide.
本研究专注于开发表面改性固体脂质纳米粒（SLN）系统，以提高模型亲水性药物异环磷酰胺的稳定性和持续释放。
采用双重乳液技术制备由甘油单油酸酯（GMO）和壳聚糖组成的 SLN，用三聚磷酸钠交联，然后在两种不同的真空条件下冷冻干燥。通过评估表面形态、粒径和表面电荷、水分含量以及药物在输送系统中的物理状态，对 SLN 进行理化特性表征。采用高效液相色谱法和液质联用技术分别评估体外药物释放和稳定性。使用 Caco-2 细胞进行细胞通透性和亚细胞定位研究。
冷冻干燥过程中不同的腔室压力会产生具有不同形态和含水量的 SLN。SLN 表现出高包封效率、持续释放和增强的异环磷酰胺稳定性，对 Caco-2 细胞具有高细胞摄取和通透性。
GMO 和壳聚糖 SLN 可成功用于提高异环磷酰胺的稳定性、持续释放、靶向和通透性特性。
