Objective To investigate and analyze the cell targeting of tumor targeting vector. Methods Source selection to 293T cells and H460 cells as experimental samples, experimental sites were selected in the laboratory of our hospital for February 2016 to 2016 March, SP5 52, doxorubicin, the 4th generation of polyamide amine, ultra filtration centrifuge tube, fluorescence isothiocyanate fluorescein, and summarize and discuss the tumor target to drugs with cell targeting. Results U-under the conditions of conventional pharmaceutical formulations against tumor new drug target to support system develop-ment, and improve the drug in the carrier of metabolic dynamics characteristics, can make the drug to enriched to drug site of tumors and tumor cells aggregation, ensure curative effect to improve, toxic side effect decreases gradually, detection con-centration range cell survival rate of over 80%, which G4 - Ac toxicity is 90%, G4 - Ac - FITC as 87%, and G4 - Ac -FITC -SP5 52 cytotoxicity was 97%;the difference is statistically significant(P<0.05). Conclusion Under the influence of the continuous development of science and technology and progress, form of anticancer drugs work started towards the tar-get, efficient, intelligent direction, ideal of pharmaceutical dosage forms with controlled and sustained release, targeted de-velopment prospect is broad, it is in;clinical application of use and promotion.%目的：探讨和分析肿瘤靶向物载体的细胞靶向性。方法选择293T细胞和H460细胞作为实验标本，实验地点选择该院实验室，时间为2016年2—3月，选择合成的SP5-52、阿霉素、第4代聚酰胺—胺、超滤离心管、荧光分子异硫氰酸荧光素等，并总结和探讨肿瘤靶向性药物所具有的细胞靶向性。结果在常规药物制剂的条件下对抗肿瘤药物新型靶向载体系统进行发展，并且改善药物在载体内部的代谢动力学相关特征，能够让药物向富集到肿瘤药部位、肿瘤细胞内部聚集，保证疗效得到提升，毒副作用逐渐减小，检测浓度范围之内细胞存活率超过80%，其中G4-Ac毒性为90%、G4-Ac-FITC为87%、而G4-Ac-FITC-SP5-52细胞毒性为97%，差异具有统计学意义(P<0.05)。结论在科学技术不断发展和进步的影响下，抗癌药物剂型的研究工作开始朝着靶向、高效、智能化方向发展，理想药物剂型具有控释、缓释、靶向发展前景较为广阔，值得在；临床运用上进行使用和推广。
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