The controlled release of a novel thiolated icariin for enhanced osteoporotic bone regeneration
The regeneration of bone defects in osteoporotic patients presents a big challenge. Icariin (Ica), which is the main active component of traditional Chinese medicine - herba epimedii, has been widely loaded to scaffolds for the treatment of bone fracture and osteoporosis. To increase drug loading ca...
| Main Authors: | , , , , , , , , |
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| Format: | Article |
| Language: | English |
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Elsevier
2021-02-01
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| Series: | Materials & Design |
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| Online Access: | http://www.sciencedirect.com/science/article/pii/S0264127521000216 |
| _version_ | 1819160565678866432 |
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| author | Zhaocong Luo Xuening Chen Minjun Liu Yuyi Wang Dongxiao Li Xiangfeng Li Yumei Xiao Yan Wang Xingdong Zhang |
| author_facet | Zhaocong Luo Xuening Chen Minjun Liu Yuyi Wang Dongxiao Li Xiangfeng Li Yumei Xiao Yan Wang Xingdong Zhang |
| author_sort | Zhaocong Luo |
| collection | DOAJ |
| description | The regeneration of bone defects in osteoporotic patients presents a big challenge. Icariin (Ica), which is the main active component of traditional Chinese medicine - herba epimedii, has been widely loaded to scaffolds for the treatment of bone fracture and osteoporosis. To increase drug loading capacity, and meanwhile achieve a stable and safe drug delivery, in present study, a novel icariin derivative - thiolated icariin (Ica-SH) molecule with good cytocompatibility and bioactivity was incorporated into biphasic calcium phosphate (BCP) ceramic scaffold through Ica-SH intermolecular disulfide bonds (abbr., Ica-SH/BCP) to form film coating. Compared with Ica-loaded BCP scaffolds via physical adsorption (abbr., Ica/BCP), the formation of Ica-SH intermolecular disulfide bonds in Ica-SH/BCP scaffolds led to a decreased real-time drug release concentration, and a reduced drug release rate. The released drug from Ica-SH/BCP scaffolds could promote the proliferation, migration, and osteoblastic differentiation of ovariectomized rat bone mesenchymal stem cells (OVX-rBMSCs), and up-regulate the angiogenic gene expression in human umbilical vein endothelial cells (HUVECs) in vitro. The OVX-rat femoral condyle defect model also demonstrated that Ica-SH/BCP scaffolds promoted a superior bone regeneration in osteoporotic animals than BCP ones. These findings suggest that Ica-SH is a promising drug, which can be facilely incorporated into a variety of scaffolds for repairing bone defects of patients, in particular the ones with osteoporosis. |
| first_indexed | 2024-12-22T16:58:28Z |
| format | Article |
| id | doaj.art-1afabd0db0e343328470ab279c79c998 |
| institution | Directory Open Access Journal |
| issn | 0264-1275 |
| language | English |
| last_indexed | 2024-12-22T16:58:28Z |
| publishDate | 2021-02-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Materials & Design |
| spelling | doaj.art-1afabd0db0e343328470ab279c79c9982022-12-21T18:19:23ZengElsevierMaterials & Design0264-12752021-02-01200109468The controlled release of a novel thiolated icariin for enhanced osteoporotic bone regenerationZhaocong Luo0Xuening Chen1Minjun Liu2Yuyi Wang3Dongxiao Li4Xiangfeng Li5Yumei Xiao6Yan Wang7Xingdong Zhang8National Engineering Research Center for Biomaterials, Sichuan University, Chengdu 61004, Sichuan, ChinaNational Engineering Research Center for Biomaterials, Sichuan University, Chengdu 61004, Sichuan, ChinaNational Engineering Research Center for Biomaterials, Sichuan University, Chengdu 61004, Sichuan, ChinaNational Engineering Research Center for Biomaterials, Sichuan University, Chengdu 61004, Sichuan, ChinaSichuan Academy of Chinese Medicine Science, Chengdu, Sichuan, ChinaNational Engineering Research Center for Biomaterials, Sichuan University, Chengdu 61004, Sichuan, ChinaNational Engineering Research Center for Biomaterials, Sichuan University, Chengdu 61004, Sichuan, China; Corresponding authors.Sichuan Academy of Medical Sciences & Sichuan Provincial People's Hospital, Chengdu, Sichuan, China; Corresponding authors.National Engineering Research Center for Biomaterials, Sichuan University, Chengdu 61004, Sichuan, ChinaThe regeneration of bone defects in osteoporotic patients presents a big challenge. Icariin (Ica), which is the main active component of traditional Chinese medicine - herba epimedii, has been widely loaded to scaffolds for the treatment of bone fracture and osteoporosis. To increase drug loading capacity, and meanwhile achieve a stable and safe drug delivery, in present study, a novel icariin derivative - thiolated icariin (Ica-SH) molecule with good cytocompatibility and bioactivity was incorporated into biphasic calcium phosphate (BCP) ceramic scaffold through Ica-SH intermolecular disulfide bonds (abbr., Ica-SH/BCP) to form film coating. Compared with Ica-loaded BCP scaffolds via physical adsorption (abbr., Ica/BCP), the formation of Ica-SH intermolecular disulfide bonds in Ica-SH/BCP scaffolds led to a decreased real-time drug release concentration, and a reduced drug release rate. The released drug from Ica-SH/BCP scaffolds could promote the proliferation, migration, and osteoblastic differentiation of ovariectomized rat bone mesenchymal stem cells (OVX-rBMSCs), and up-regulate the angiogenic gene expression in human umbilical vein endothelial cells (HUVECs) in vitro. The OVX-rat femoral condyle defect model also demonstrated that Ica-SH/BCP scaffolds promoted a superior bone regeneration in osteoporotic animals than BCP ones. These findings suggest that Ica-SH is a promising drug, which can be facilely incorporated into a variety of scaffolds for repairing bone defects of patients, in particular the ones with osteoporosis.http://www.sciencedirect.com/science/article/pii/S0264127521000216Thiolated icariinControlled releaseHigh loading capacityOsteoporotic bone regenerationBCP ceramic |
| spellingShingle | Zhaocong Luo Xuening Chen Minjun Liu Yuyi Wang Dongxiao Li Xiangfeng Li Yumei Xiao Yan Wang Xingdong Zhang The controlled release of a novel thiolated icariin for enhanced osteoporotic bone regeneration Materials & Design Thiolated icariin Controlled release High loading capacity Osteoporotic bone regeneration BCP ceramic |
| title | The controlled release of a novel thiolated icariin for enhanced osteoporotic bone regeneration |
| title_full | The controlled release of a novel thiolated icariin for enhanced osteoporotic bone regeneration |
| title_fullStr | The controlled release of a novel thiolated icariin for enhanced osteoporotic bone regeneration |
| title_full_unstemmed | The controlled release of a novel thiolated icariin for enhanced osteoporotic bone regeneration |
| title_short | The controlled release of a novel thiolated icariin for enhanced osteoporotic bone regeneration |
| title_sort | controlled release of a novel thiolated icariin for enhanced osteoporotic bone regeneration |
| topic | Thiolated icariin Controlled release High loading capacity Osteoporotic bone regeneration BCP ceramic |
| url | http://www.sciencedirect.com/science/article/pii/S0264127521000216 |
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