Objective To preparation folic acid-conjugated cis-platin nanomedicine that can transport cisplatin by folate receptor-mediated endocytosis,and to investigate the therapy effect of this medicine for nasopharyngeal carcinoma ( NPC) cells. Methods Cis-platin loaded nanomedicine was prepared by co-precipitation method using sodium alginate as modification material. Folic acid linked nanoparticles (FA-MNP-CDDP) was synthesized through PEG (NH2)2. Capacity of FA-MNP-CDDP for targeted drug delivery and inhibitory effects on human NPC cells was evaluated hy Prussian Staining and MTT assay. Results CDDP content in CDDP-MNP-FA suspension was ( 1.6 ± 0.1 )mg/mL. An average core size of ( 10.1 ± 1.5)nm was found by transmission electronic microscopy (TEM). By comparing with CNE-2 cells, HNE-1 cells had a higher uptake for FA-MNP-CDDP. This nanomedicine had strong inhibitory effects on HNE-1 cells . the IC5o of it [ ( 1.300 ± 0.10) μg/mL] was 40％ lower than CDDP [ (2.161± .085) μg/mL]. Conclusion FA-MNP-CDDP nanomedicine show promise for targeted drug delivery and therapy effect in folate receptor over-expressing NPC cells.%目的:制备连接叶酸分子的顺铂纳米药物,并研究该药物对人鼻咽癌细胞的体外靶向治疗作用.方法:采用化学共沉淀法制备顺铂纳米药物并通过聚乙二醇二胺连接叶酸分子合成叶酸-顺铂纳米药物(FA-MNP-CDDP)并对其进行表征.将人鼻咽癌细胞HNE-1和CNE-2与FA-MNP-CDDP体外共培养,采用普鲁士蓝染色法测定细胞摄取纳米药物的情况,采用MTT法测定纳米药物的细胞毒性.结果:合成FA-MNPCDDP纳米药物顺铂含量为(1.6 ±0.1)mg/mL,药物粒子平均直径为(10.1 ±1.5)nm.表达叶酸受体的HNE-1细胞对该纳米药物摄取能力显著强于不表达叶酸受体的CNE-2细胞.FA-MNP-CDDP对HNE-1细胞的体外抑制效果明显,IC50[(1.300±0.10)μg/mL]较单纯顺铂[(2.161±0.85)μg/mL]降低约40%.结论:叶酸-顺铂纳米药物具有针对鼻咽癌细胞的靶向载药和抑制增殖的能力.
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