Aptavalve-gated Mesoporous Carbon Nanospheres image Cellular Mucin and provide On-demand Targeted Drug Delivery

Chengyi Li¹, Min Qian¹, Shanshan Wang¹, Huilin Jiang¹, Yilin Du¹, Jianxin Wang¹, Weiyue Lu¹, Niren Murthy², Rongqin Huang^1✉

1. Department of pharmaceutics, School of Pharmacy, Key Laboratory of Smart Drug Delivery, Ministry of Education, Fudan University, Shanghai 201203, P. R. China.
2. Department of Bioengineering, University of California, Berkeley, California 94720, USA.

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Citation:
Li C, Qian M, Wang S, Jiang H, Du Y, Wang J, Lu W, Murthy N, Huang R. Aptavalve-gated Mesoporous Carbon Nanospheres image Cellular Mucin and provide On-demand Targeted Drug Delivery. Theranostics 2017; 7(13):3319-3325. doi:10.7150/thno.18692. Available from https://www.thno.org/v07p3319.htm

Abstract

In this report, we present a mesoporous carbon nanosphere that can target drugs to tumors and image tumor biomarkers. A single-strand DNA (P₀ aptamer) aptavalve was capped on the surface of doxorubicin-loaded oxide mesoporous carbon nanospheres (Dox-OMCN-P₀) through π-π stacking for real-time imaging-guided on-demand targeting drug delivery. The Dox-OMCN-P₀ could not only realize the detection of MUC1 tumor marker with a wide linear range (0.1 - 10.6 μmol/L) and a low detection limit (17.5 nmol) based on different apparatuses, but also achieve in-situ targeting imaging of cellular MUC1 concentration in vitro and in vivo via “off-on” fluorescence biosensing. Much attractively, as a real-time feedback of the diagnostic/imaging outcomes, Dox-OMCN-P₀ accomplished the on-demand targeting drug delivery in quantitative response to MUC1. Controllable chemotherapy with sustained release and pH-sensitiveness, together with the potential photothermal therapy, were also clearly demonstrated. This is a simple but advanced platform, which could well achieve the real-time switchable imaging of cellular mucin for targeting cancer therapy.

Keywords: MCN, aptavalve, real-time imaging, on-demand, targeting delivery