Antibody fragment-armed mesoporous silica nanoparticles for the targeted delivery of bevacizumab in ovarian cancer cells

作者：Zhang Ying; Guo Jing; Zhang Xiao Ling; Li Da Peng; Zhang Ting Ting; Gao Fu Feng; Liu Nai Fu; Sheng Xiu Gui^*

来源：International Journal of Pharmaceutics, 2015, 496(2): 1026-1033.

DOI：10.1016/j.ijpharm.2015.10.080

• Antibody
• Bevacizumab
• Mesoporous silica nanoparticles
• Apoptosis
• Ovarian cancer

In order to enhance the therapeutic efficacy and intracellular concentration of bevacizumab (BVC), we have designed a novel tumor endothelial marker 1 (TEM1)/endosialin (Ab-/scFv)-conjugated mesoporous silica nanoparticles (MSN) to target ovarian cancer cell. The Ab-/scFv-conjugated MSN were prepared by the conjugation of amine functional group of antibody of the carboxyl group of MSN. The resultant MSN was nanosized, spherical shaped, and exhibited a controlled release phenomenon in pH 7.4 conditions. Furthermore, BMSN/Ab was found to increase the cellular uptake and intracellular distribution of BVC in OVCAR-5 cancer cells. The Ab- conjugated MSN exhibited a superior anticancer effect with profound apoptosis in cancer cells in a time- and concentration dependent manner. Consistently, BMSN/Ab effectively inhibited the colony formation in transwell plate. Finally, BMSN/Ab showed a notable increase in the proportion of cells in G2/M phase of cell cycle indicating promising anticancer efficacy profile. Overall, Ab-/scFv-conjugated MSN might provide an effective strategy for the therapeutic management of ovarian cancers.

• 出版日期2015-12-30
• 单位山东省医学科学院; 济南大学