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Abstract

This paper describes the design of alendronate-conjugated nanodiamonds (Alen-NDs) and evaluation of their feasibility for bone-targeted delivery. Alen-NDs exhibited a high affinity to hydroxyapatite (HAp, the mineral component of bone) due to the presence of Alen. Unlike NDs (without Alen), Alen-NDs were preferentially taken up by MC3T3-E1 osteoblast-like cells, compared to NIH3T3 and HepG2 cells, suggesting their cellular specificity. In addition, NDs itself increased ALP activity of MC3T3-E1 cells, compared to control group (osteogenic medium) and Alen-NDs exhibited more enhanced ALP activity. In addition, an in vivo study revealed that Alen-NDs effectively accumulated in bone tissues after intravenous tail vein injection. These results confirm the superior properties of Alen-NDs with advantages of high HAp affinity, specific uptake for MC3T3-E1 cells, positive synergistic effect for ALP activity, and in vivo bone targeting ability. The Alen-NDs can potentially be employed for osteoporosis treatment by delivering both NDs and Alen to bone tissue. 

Author information

Ryu TK1, Kang RH1, Jeong KY1, Jun DR1, Koh JM2, Kim D3, Bae SK3, Choi SW4.​

1Department of Biotechnology, The Catholic University of Korea, 43 Jibong-ro Wonmi-gu, Bucheon-si, Gyeonggi-do 420-743, Republic of Korea.

2Division of Endocrinology and Metabolism, Asan Medical Center, University of Ulsan College of Medicine, 88 Olympic-ro 43-gil, Songpa-gu, Seoul 138-736, Republic of Korea.

3College of Pharmacy, The Catholic University of Korea, 43 Jibong-ro Wonmi-gu, Bucheon-si, Gyeonggi-do 420-743, Republic of Korea.

4Department of Biotechnology, The Catholic University of Korea, 43 Jibong-ro Wonmi-gu, Bucheon-si, Gyeonggi-do 420-743, Republic of Korea. Electronic address: choisw@catholic.ac.kr.