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New drug carrier and delivery systems have been investigated using DNA origami structures. Initially, a fluorescence‐labeled DNA origami was added to cultured cells, and the efficiency of cellular uptake was investigated. Ding and coworkers created a DNA origami structure as a drug carrier containing the anticancer drug doxorubicin (Dox) (Figure 1.15a) [108]. The DNA origami structures carrying a high concentration of drug were efficiently incorporated into cells, and remarkable cytotoxicity was observed. Furthermore, delivery using DNA origami is being studied for living organisms. DNA origami has been used to investigate tumor targeting in mice and drug persistence at the tumor site [112]. DNA origami showed tumor‐specific accumulation, and by introducing the anticancer drug Dox into the DNA origami structure, it showed delivery to the tumor and a remarkable antitumor effect.

Figure 1.14 (a) DNA origami channel structure. Tubular pores (dark gray), main body (light gray), cholesterol moieties (gray) at the bottom of the main body, and TEM image. (b) The DNA channel is bound to the lipid bilayer membrane via cholesterol, and the pore domain penetrates the lipid membrane. TEM image of origami channels bound to a liposome.

Source: Langecker et al. [103]/with permission of Springer Nature.

(c) Precise control of liposome size using DNA origami templates. DNA‐DOPE conjugates were placed inside the ring via hybridization, then extra lipid was supplied, and the formed vesicle was dialyzed. Finally, the size‐controlled liposome was released from the ring template. (d) TEM images of size‐controlled liposomes.

Source: Yang et al. [104]/with permission of Springer Nature.

Figure 1.15 Delivery of DNA origami structures to cells and functional control. (a) The prepared DNA origami structure is intercalated with the anticancer drug doxorubicin (Dox) and introduced into the cells.

Source: Jiang et al. [108]/with permission of American Chemical Society.

(b) Control the binding amount and release rate of Dox using DNA origami structures with different pitches (10.5 and 12 base pairs).

Source: Zhao et al. [109].

(c) Retention of DNA nanodevice in mouse (after two hours). Left: No coating. Accumulated in the bladder. Right: With coating. Distributed throughout the body.

Source: Perrault and Shih [110].

(d) Coating of the structure with PEG‐conjugated cationic polymer (polylysine K10‐PEG5K).

Source: Ponnuswamy et al. [111]/Springer Nature/CC BY 4.0.

In addition, tumor growth was suppressed by incorporating siRNA into the DNA origami structure [113]. A DNA origami structure carrying Bcl2 siRNA that suppresses apoptosis was prepared and introduced into the host cells. Using this structure, Bcl2 expression was suppressed by RNA interference resulting in suppression of tumor growth.