2. Academic Validation
  3. Hexapeptide-conjugated calcitonin for targeted therapy of osteoporosis

Hexapeptide-conjugated calcitonin for targeted therapy of osteoporosis

  • J Control Release. 2019 Jun 28:304:39-50. doi: 10.1016/j.jconrel.2019.04.042.
Yanpeng Liu 1,  Peng Yu 1,  Xu Peng 2,  Qin Huang 1,  Mingming Ding 1,  Yantao Chen 3,  Ruitao Jin 1,  Jing Xie 1,  Changsheng Zhao 1,  Jianshu Li 4
Affiliations

Affiliations

  • 1 College of Polymer Science and Engineering, State Key Laboratory of Polymer Materials Engineering, Sichuan University, Chengdu 610065, China.
  • 2 Laboratory Animal Center of Sichuan University, Chengdu 610041, China.
  • 3 Shenzhen Key Laboratory of Environmental Chemistry and Ecological Remediationering, College of Chemistry and Environmental Engineering, Shenzhen University, Shenzhen 518060, China.
  • 4 College of Polymer Science and Engineering, State Key Laboratory of Polymer Materials Engineering, Sichuan University, Chengdu 610065, China. Electronic address: jianshu_li@scu.edu.cn.
PMID: 31054990 DOI: 10.1016/j.jconrel.2019.04.042
Abstract

The high level of bone metabolism associated with osteopenia and multifocal skeletal fracture remains a challenging clinical problem in osteoporosis patients. Salmon Calcitonin (sCT), as a peptide medicine, is able to inhibit osteoclast activity and stimulate osteoblast growth. However, Calcitonin receptors (CTRs) are widely distributed in vivo, limiting the specificity and therapeutic effects. Here, we report a bone-seeking hexapeptide (Asp6)-conjugated sCT (sCT-Mal-Asp6) for the targeted treatment of osteoporosis. The sCT-Mal-Asp6 was synthesized via a disulfide re-bridge reaction with high specificity and purity. It was demonstrated that the adsorption of sCT-Mal-Asp6 on hydroxyapatite (HA) was about 5.4 times higher than that of sCT. It was demonstrated a prolonged circulation time and 3-fold higher femur tissue accumulation of sCT-Mal-Asp6. In ovariectomized (OVX) models, sCT-Mal-Asp6 significantly increased the ability to attenuate hypercalcemia and reconstruct the trabecula. Our work provides an efficient approach to targeted and effective osteoporosis treatment.

Keywords

Bioconjugate; Bone-targeting; Hexapeptide; Osteoporosis; Salmon calcitonin.

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