SN38 is the active metabolite of irinotecan with 1000-fold greater cytotoxicity compared to the parent drug. Despite the potential, its application as a drug is still seriously limited due to its stability concerns and low solubility in acceptable pharmaceutical solvents. To address these drawbacks here nanostructured lipid carrier (NLC) containing SN38 was prepared and its cytotoxicity against U87MG glioblastoma cell line was investigated. The formulations were prepared using hot ultrasonication and solvent evaporation/emulsification methods. NLCs with a mean size of 140 nm and particle size distribution (PDI) of 0.25 were obtained. The average loading efficiency was 9.5% and its entrapment efficiency was 81%. In order to obtain an accurate determination of released amount of SN38 a novel medium and extraction method was designed, which lead to an appropriate in vitro release profile of the drug from the prepared NLCs. The MTT test results revealed the significant higher cytotoxicity of NLCs on U87MG human glioblastoma cell line compared with the free drug. The confocal microscopy images confirmed the proper penetration of the nanostructures into the cells within the first 4 h. Consequently, the results indicated promising potentials of the prepared NLCs as a novel treatment for glioblastoma.

SN38 是伊立替康的活性代谢物，与母体药物相比，其细胞毒性高 1000 倍。尽管具有潜力，但由于其稳定性问题和在可接受的药物溶剂中的低溶解度，其作为药物的应用仍然受到严重限制。为了解决这些缺点，本文制备了含有 SN38 的纳米结构脂质载体 (NLC)，并研究了其对 U87MG 胶质母细胞瘤细胞系的细胞毒性。使用热超声处理和溶剂蒸发/乳化方法制备制剂。获得了平均粒径为 140 nm 且粒径分布 (PDI) 为 0.25 的 NLC。平均装载效率为 9.5%，其包封效率为 81%。为了准确测定SN38的释放量，设计了一种新的培养基和提取方法，这导致药物从制备的 NLC 中的适当体外释放曲线。MTT 测试结果显示，与游离药物相比，NLC 对 U87MG 人胶质母细胞瘤细胞系的细胞毒性显着更高。共聚焦显微镜图像证实了纳米结构在前 4 小时内正确渗透到细胞中。因此，结果表明所制备的 NLC 作为胶质母细胞瘤的新型治疗方法具有广阔的前景。