Pharmacokinetics, Nanotechnology and Gene Therapy Group, School of Pharmacy, University of the Basque Country UPV/EHU, Vitoria-Gasteiz, Spain.
Int J Pharm. 2013 Oct 1;454(2):775-83. doi: 10.1016/j.ijpharm.2013.05.017. Epub 2013 May 18.
The challenge for the treatment of inflammatory bowel disease (IBD) is the delivery of the drug to the site of inflammation. Because nanoparticles have the ability to accumulate in inflamed regions, the aim of the present study was to evaluate nanostructured lipid carriers (NLCs) as nanoparticulate drug delivery systems for the treatment of IBD. Budesonide (BDS) was chosen as a candidate anti-inflammatory drug. BDS-loaded NLCs (BDS-NLC) produced by high-pressure homogenization had a size of 200 nm and a negative zeta potential. BDS-NLCs reduced the TNF-α secretion by activated macrophages (J774 cells). BDS-NLCs were more active in a murine model of dextran sulfate-induced colitis when compared with Blank-NLCs or a BDS suspension: BDS-NLCs decreased neutrophil infiltration, decreased the levels of the pro-inflammatory cytokines IL-1β and TNF-α in the colon and improved the histological scores of the colons. These data suggest that NLCs could be a promising alternative to polymeric nanoparticles as a targeted drug delivery system for IBD treatment.
治疗炎症性肠病(IBD)的挑战在于将药物递送到炎症部位。由于纳米颗粒具有在炎症区域聚集的能力,本研究旨在评估纳米结构脂质载体(NLC)作为治疗 IBD 的纳米药物递送系统。布地奈德(BDS)被选为候选抗炎药物。高压均质法制备的载布地奈德 NLC(BDS-NLC)的粒径为 200nm,zeta 电位为负。BDS-NLC 可降低活化巨噬细胞(J774 细胞)分泌的 TNF-α。与空白 NLC 或 BDS 混悬剂相比,BDS-NLC 在葡聚糖硫酸钠诱导的结肠炎小鼠模型中更具活性:BDS-NLC 可减少中性粒细胞浸润,降低结肠中促炎细胞因子 IL-1β 和 TNF-α的水平,并改善结肠的组织学评分。这些数据表明,NLC 可能是聚合物纳米颗粒的有前途的替代品,作为治疗 IBD 的靶向药物递送系统。