维生素A-姜黄素脂质体的制备及细胞毒性研究

孟路华 赵怡 潘黎军 王驰

中国药学杂志 ›› 2011, Vol. 46 ›› Issue (14) : 1104-1107.

PDF(660 KB)
PDF(660 KB)
中国药学杂志 ›› 2011, Vol. 46 ›› Issue (14) : 1104-1107.
论著

维生素A-姜黄素脂质体的制备及细胞毒性研究

  • 孟路华,赵怡,潘黎军,王驰*
作者信息 +

Study on Preparation of Vitamin A-Curcumin Liposome and Its Cytotoxicity

  • MENG Lu-hua, ZHAO Yi, PAN Li-jun, WANG Chi*
Author information +
文章历史 +

摘要

目的 制备肝星状细胞靶向维生素A-姜黄素脂质体(VA-CUR-L),并进行体外细胞毒性实验。方法 采用逆相蒸发法制备VA-CUR-L,测定其包封率及VA结合率;脂质体分别在4,25 ℃下密闭放置30d,以包封率、VA结合率及过氧化值为指标考察其稳定性;以视黄醇结合蛋白受体高表达的鼠肝星状细胞HSC-T6和无视黄醇结合蛋白受体表达的人食管癌细胞A-549为细胞模型,采用MTT法考察该脂质体的细胞毒性及靶向性。结果 脂质体平均包封率为89.32%,VA结合率为61.34%;脂质体于4 ℃贮存较稳定;细胞实验显示,游离姜黄素、姜黄素脂质体及VA-CUR-L对HSC-T6的IC50值分别为31.53,14.95和8.28 μg·mL-1 ,姜黄素脂质体和VA-CUR-L对A-549细胞作用相当。结论 在最佳工艺条件下制得的VA-CUR-L包封率高、稳定性好,且可特异性靶向作用于肝星状细胞,提高药物疗效。

Abstract

OBJECTIVE To prepare Hepatic stellate cell targeting Vitamin A-curcumin liposome and to investigate its cytotoxicity in vitro. METHODS Reverse phase evaporation was used to prepare VA-curcumin liposome and the entrapment efficiency and the VA binding rate was determined. Entrapment efficiency, VA binging rate and peroxide value were determined to evaluate the stability of liposome at 4 and 25 ℃ for 30 d. MTT assay was used to investigate the cytotoxicity and targeting ability of the liposome in rat hepatic stellate cells HSC-T6 with high expression of retinol binding protein and human esophageal cancer cells A-549 without expression of retinol binding protein. RESULTS The average entrapment efficiency for curcumin was 89.32%, and binding rate for VA was 61.34%. The liposome stored at 4 ℃ was stable. The RESULTS of MTT assay showed that IC50 of curcumin, curcumin liposome, and VA-curcumin liposome in HSC-T6 cell were 31.53, 14.95 and 8.28 μg·mL-1, respectively. Curcumin liposome and VA-curcumin liposome had same cytotoxic effects in A-549 cell. CONCLUSION The optimized conditions were obtained with high entrapment efficiency and good stability. VA-curcumin liposome could specifically target HSC and promote therapeutic effect of curcumin.

关键词

肝星状细胞 / 姜黄素 / 维生素A / 脂质体 / 细胞毒作用 / 靶向性

Key words

hepatic stellate cell / curcumin / vitamin A / liposome / cytotoxic effect / targeting ability

引用本文

导出引用
孟路华 赵怡 潘黎军 王驰. 维生素A-姜黄素脂质体的制备及细胞毒性研究[J]. 中国药学杂志, 2011, 46(14): 1104-1107
MENG Lu-hu;ZHO Yi;PN Li-jun;WNG Chi. Study on Preparation of Vitamin A-Curcumin Liposome and Its Cytotoxicity[J]. Chinese Pharmaceutical Journal, 2011, 46(14): 1104-1107

参考文献


[1] CHENG Y, PING J, LIU C, et al.Study on effect of extracts from salvia miltiorrhiza and curcuma longa in inhibiting phosphorylated extracellular signal regulated kinase expression in rats Hepatic stellate cell[J].Chin J Integr Med, 2006, 12(3): 207-211.
[2] SUNDARAM M, SIVAPRASADARO A, DESOUSA M M, et al. The transfer of retinol from serum retinol-binding protein to cellular retinol-binding protein is mediated by a membrane receptor[J].J Biol Chem, 1998, 273(6):3336-3342.
[3] SATO Y, MURASE K, KATO J, et al.Resolution of liver cirrhosis using vitamin A-coupled liposomes to deliver siRNA against a collagen-specific chaperone[J].Nat Biotechnol, 2008, 26(4):431-442.
[4] FRIENDMAN S L.Targeting siRNA to arrest fibrosis[J].Nat Biotechnol, 2008, 26(4):399-400.
[5] BRUCK R, ASHKENAZI M, WEISS S, et al.Prevention of liver cirrhosis in rats by curcumin[J].Liver Int, 2007, 27(3):373-383.
[6] LI Y, YANG L X, LI Y D, et al.Progress in anti-fibrosis effects of curcumin[J].J Beijing Univ Trad Chin Med(北京中医药大学学报), 2008, 31(6):408-411.
PDF(660 KB)

72

Accesses

0

Citation

Detail

段落导航
相关文章

/