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<p>Nitrogen-containing bisphosphonates (BPs) are widely used in the treatment of osteoporosis (OP); however, their administration can lead to severe complications, such as bisphosphonate-related osteonecrosis of the jaw, causing significant pain in patients. In this study, we synthesized carbon dots (CDs) from alendronate, ibandronate, risedronate, and zoledronate, which are drugs used in OP treatment. These bisphosphonate-containing CDs (BP-CDs) exhibited excellent biocompatibility, fluorescence properties, and a strong affinity for calcium-based biomaterials. Moreover, the BP-CDs effectively inhibited the differentiation of RAW 264.7 cells, a type of macrophages, into osteoclasts (OCs). Importantly, all the BP-CDs demonstrated an inhibitory effect on osteoclast differentiation comparable to that of alendronate. In addition, compared to alendronate, the BP-CDs exhibited reduced cytotoxic effects on RAW 264.7 cells, which are precursors of OCs, as well as on MC3T3-e1 cells, which are precursors of osteoblasts. These findings suggest that BP-CDs are a promising therapeutic option for OP and are capable of inhibiting the differentiation and maturation processes of OCs.</p>

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Nitrogen-Containing Bisphosphonate Carbon Dots with High Affinity to Calcium-Based Biomaterials for Suppression of Osteoclasts

  • 期刊论文

  • 发表日期：

    2025年1月20日

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  • Kyung Kwan Lee,
  • Hongki Kim,
  • Chang-Soo Lee

摘要

Nitrogen-containing bisphosphonates (BPs) are widely used in the treatment of osteoporosis (OP); however, their administration can lead to severe complications, such as bisphosphonate-related osteonecrosis of the jaw, causing significant pain in patients. In this study, we synthesized carbon dots (CDs) from alendronate, ibandronate, risedronate, and zoledronate, which are drugs used in OP treatment. These bisphosphonate-containing CDs (BP-CDs) exhibited excellent biocompatibility, fluorescence properties, and a strong affinity for calcium-based biomaterials. Moreover, the BP-CDs effectively inhibited the differentiation of RAW 264.7 cells, a type of macrophages, into osteoclasts (OCs). Importantly, all the BP-CDs demonstrated an inhibitory effect on osteoclast differentiation comparable to that of alendronate. In addition, compared to alendronate, the BP-CDs exhibited reduced cytotoxic effects on RAW 264.7 cells, which are precursors of OCs, as well as on MC3T3-e1 cells, which are precursors of osteoblasts. These findings suggest that BP-CDs are a promising therapeutic option for OP and are capable of inhibiting the differentiation and maturation processes of OCs.