重组高密度脂蛋白-紫杉醇对结肠癌的靶向性研究

目的：制备重组高密度脂蛋白-紫杉醇复合物（γHDL-PTX），研究其对结肠癌的靶向作用。方法：薄膜分散法制备γHDL-PTX，采用HPLC法定量考察结肠癌细胞HT-29对γHDL-PTX的摄取作用；采用MTT法测定研究γHDL-PTX对HT-29细胞的增殖抑制作用；采用HPLC法测定γHDL-PTX在荷瘤鼠中的组织分布情况；构建rHDL-DiR并采用裸鼠活体成像法观察载体在荷瘤鼠的分布情况。结果：细胞试验表明HT-29细胞对γHDL-PTX摄取高于对PTX溶液、γHDL-PTX核的摄取，IC₅₀显著低于其他两种剂型（P < 0.01）。组织分布及裸鼠活体成像试验表明γHDL-PTX在肿瘤组织的分布较其他两种剂型有所提高。结论：γHDL作为抗肿瘤药物载体对结肠癌具有较好的靶向性能，具有较为广阔的应用前景。

Targeting effect of reconstituted high density lipoprotein loaded paclitaxel to colon cancer

OBJECTIVE To prepare reconstituted high density lipoprotein loaded paclitaxel ((γHDL-PTX), and evaluate the targeting effects to colon cancer.METHODS γHDL-PTX was prepared using thin-film dispersion method. The cellular uptakes of γHDL-PTX in vivo were detected by HPLC. MTT assay was used to evaluate the anti-proliferation efficiency of γHDL-PTX. The distribution of PTX in tumor-bearing mice was detected using HPLC. in vivo imaging system was used to detect the targeting efficiency in the tumor-bearing nude mice.RESULTS The cellular uptake of γHDL-PTX was significantly higher than PTX solution and the core of γHDL-PTX, IC₅₀ of rHDL-PTX was significantly lower than the other dosage forms. γHDL-PTX exhibited remarkable tumor targeting efficiency by distribution test in tumor-bearing mice and in vivo imaging.CONCLUSION γHDL shows well tumor targeting efficiency to colon cancer, and it will be a promising drug delivery system for anti-cancer drugs.