Department of Biotechnology, The Catholic University of Korea, 43 Jibong-ro Wonmi-gu, Bucheon-si, Gyeonggi-do 420-743, Republic of Korea.
Division 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.
J Control Release. 2016 Jun 28;232:152-60. doi: 10.1016/j.jconrel.2016.04.025. Epub 2016 Apr 17.
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.
本文描述了阿仑膦酸钠偶联纳米金刚石（Alen-NDs）的设计及其用于骨靶向递药的可行性评估。由于存在 Alen，Alen-NDs 对羟基磷灰石（HAp，骨的矿物质成分）表现出高亲和力。与 NIH3T3 和 HepG2 细胞相比，不同于 NDs（无 Alen），Alen-NDs 优先被 MC3T3-E1 成骨样细胞摄取，表明其具有细胞特异性。此外，与对照组（成骨培养基）相比，NDs 本身增加了 MC3T3-E1 细胞的碱性磷酸酶（ALP）活性，而 Alen-NDs 表现出更高的 ALP 活性。此外，体内研究表明，静脉尾静脉注射后，Alen-NDs 能有效地在骨组织中蓄积。这些结果证实了 Alen-NDs 的优越性能，具有高 HAp 亲和力、对 MC3T3-E1 细胞的特异性摄取、对 ALP 活性的积极协同作用以及体内骨靶向能力的优势。Alen-NDs 可通过将 NDs 和 Alen 递送到骨组织中，用于骨质疏松症的治疗。
