Objective To prepare immunonanospheres containing sorafenib[HAb18-HSA(SAF)-NS] a-gainst human liver cancer and evaluate its immunoreactivity and effects on cancer. Methods HAb18-HAS (SAF)-NS was prepared by intermolecular cross-linking the monoclonal antibody HAb18 with human serum albumin nanospheres containing SAF [HAS (SAF)-NS]via a new heterobifunctional cross-linker SPDP. Con-densation test and immunofluorescence assay were used to evaluate the immunoreactivity, and the specific binding of HAb18-HSA (SAF)-NS with liver cancer cell line SMMC-7721 was observed by microscope and electron-microscope. The specific cytotoxic effects on target cells were evaluated in vitro by MTT assay. HAb18-HSA(SAF)-NS, HSA(SAF)-NS and SAF were separately injected into nude mice bearing human liv-er carcinoma to observe the inhibitory activity of HAb18-HSA(SAF)-NS in vivo. Results The immunoreac-tivity of HAb18-HSA (SAF)-NS was well preserved. Under electron-microscope, HAb18-HSA (SAF)-NS could bind SMMC-7721 cells specifically. IC50 value for HAb18-HSA(SAF)-NS on SMMC-7721 cells was 42.4μg/mL, which was lower than that of HSA (SAF)-NS (368.9 μg/mL) and SAF (377.5 μg/mL). The in-hibitory rate of HAb18-HSA (SAF)-NS on the growth of liver cancer xenografts was significantly higher than that of HSA (SAF)-NS or SAF (P<0.001). Conclusion HAb18-HSA (SAF)-NS has immunoreactivity and specific targeting to the liver cancer cells. The anticancer ability of HAb18-HSA (SAF)-NS is significantly higher than that of HSA(SAF)-NS and SAF.%目的：制备抗人肝癌抗体与索拉非尼偶联免疫毫微球，观察其特性及抗肝癌效果。方法通过异型双功能交联剂SPDP，将抗人肝癌单克隆抗体HAb18与索拉非尼（sorafenib, SAF）人血清白蛋白毫微球[HSA（SAF）-NS]偶联，制成抗人肝癌抗体与索拉非尼偶联免疫毫微球HAb18-HSA（SAF）-NS，使用凝集试验检测其活性，光镜和电镜下观察其与人肝癌细胞株SMMC-7721特异性结合。MTT法检测该免疫毫微球的体外杀伤性。于人肝癌裸鼠模型上分别使用HAb18-HSA （SAF）-NS、HSA （SAF）-NS及SAF，检测三者的肿瘤抑制率。结果 HAb18-HSA（SAF）-NS具有单抗活性，能与肝癌细胞特异结合；其体外杀伤SMMC-7721细胞IC 50值为42.4μg/mL，与HSA （SAF）-NS （368.9μg/mL）及SAF （377.5μg/mL）相比，明显降低；体内肿瘤抑制率比HSA（SAF）-NS及SAF显著增强（P<0.001）。结论 HAb18-HSA （SAF）-NS具有免疫活性，对肝癌细胞有主动靶向性，体内外均具有比HSA（SAF）-NS及SAF更强的抗癌效果。
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