自旋探针α-苯基-N-4-丁基硝酮纳米粒的制备及其对肝肿瘤细胞的亲和性研究

采用薄膜分散-超声法制备、优化自旋捕捉剂α-苯基-N-4-丁基硝酮(N-tert-butyl-α-phenylnitrone，PBN)脂质体，并研究其相关性质。以人肝肿瘤细胞SMMC-7721为实验对象，采用反相高效液相法(RP-HPLC)测定细胞内PBN的浓度，以此评价PBN脂质体对细胞的亲和性；考察了PBN脂质体对细胞生长的影响。结果显示，采用正交设计优化得到PBN脂质体的平均粒径137.5 nm，包封率71.52%，多分散系数0.286。PBN脂质体可稳定进入癌细胞内，同游离的PBN相比，PBN脂质体对肝肿瘤细胞更具亲和性，转染后癌细胞坏死率更高。表明自旋捕捉剂脂质体对肝肿瘤细胞具有较好的亲和性并能明显抑制其生长。为研究肿瘤自旋靶向性干预提供了实验依据。

Preparation of the spin trapping probe, N-tert-butyl-α-phenylnitrone,nanoparticle and its affinity to hepatoma cells

This article describes the preparation of the N-tert-butyl-alpha-phenylnitrone (PBN) liposomes and their related characteristics. The PBN liposomes were prepared by film dispersion-supersonic method and the formula of liposomes was optimized by orthogonal uniform design. RP-HPLC was used to qualify the amount of PBN that entered into the hepatoma cells. Necrosis rate was also investigated by fluorescence activated cell sorter (FACS) after PBN liposomes transfection. Result showed that the mean particle size, entrapment efficiency, and polydispersity of the resulting PBN-liposome were 137.5 nm, 71.52% and 0.286, respectively. PBN liposomes can enter into the tumor cell stably and they have higher affinity to hepatoma cell compared with free PBN resulting in a higher necrosis rate after transfection. These results provide a potential method for early diagnosis and treatment of cancer using specific spin trapping probe targeting tumor cells.