Recent Advancements in Drug Delivery of Sinomenine, A Disease-Modifying Anti-Rheumatic Drug
Sinomenine (SIN) is a benzyltetrahydroisoquinoline-type alkaloid isolated from the dried plant root and stem of <i>Sinomenium acutum</i> (Thumb.) Rehd.et Wils, which shows potent anti-inflammatory and analgesic effects. As a transforming disease-modifying anti-rheumatic drug, SIN has bee...
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-12-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/14/12/2820 |
| _version_ | 1827637275905753088 |
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| author | Xin Chen Chengcheng Lu Yanwen Duan Yong Huang |
| author_facet | Xin Chen Chengcheng Lu Yanwen Duan Yong Huang |
| author_sort | Xin Chen |
| collection | DOAJ |
| description | Sinomenine (SIN) is a benzyltetrahydroisoquinoline-type alkaloid isolated from the dried plant root and stem of <i>Sinomenium acutum</i> (Thumb.) Rehd.et Wils, which shows potent anti-inflammatory and analgesic effects. As a transforming disease-modifying anti-rheumatic drug, SIN has been used to treat rheumatoid arthritis over twenty-five years in China. In recent years, SIN is also in development for use against other disorders, including colitis, pain, traumatic brain injury, and uveitis. However, its commercial hydrochloride (SIN-HCl) shows low oral bioavailability and certain allergic reactions in patients, due to the release of histamine. Therefore, a large number of pharmaceutical strategies have been explored to address these liabilities, such as prolonging release behaviors, enhancing skin permeation and adsorption for transdermal delivery, targeted SIN delivery using new material or conjugates, and co-amorphous technology. This review discusses these different delivery strategies and approaches employed to overcome the limitations of SIN for its efficient delivery, in order to achieve improved bioavailability and reduced side effects. The potential advantages and limitations of SIN delivery strategies are elaborated along with discussions of potential future SIN drug development strategies. |
| first_indexed | 2024-03-09T15:57:48Z |
| format | Article |
| id | doaj.art-d5d1de00894d4bc9b573c17c1e6dbd8b |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-09T15:57:48Z |
| publishDate | 2022-12-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-d5d1de00894d4bc9b573c17c1e6dbd8b2023-11-24T17:22:35ZengMDPI AGPharmaceutics1999-49232022-12-011412282010.3390/pharmaceutics14122820Recent Advancements in Drug Delivery of Sinomenine, A Disease-Modifying Anti-Rheumatic DrugXin Chen0Chengcheng Lu1Yanwen Duan2Yong Huang3Xiangya International Academy of Translational Medicine, Central South University, Changsha 410013, ChinaXiangya International Academy of Translational Medicine, Central South University, Changsha 410013, ChinaXiangya International Academy of Translational Medicine, Central South University, Changsha 410013, ChinaXiangya International Academy of Translational Medicine, Central South University, Changsha 410013, ChinaSinomenine (SIN) is a benzyltetrahydroisoquinoline-type alkaloid isolated from the dried plant root and stem of <i>Sinomenium acutum</i> (Thumb.) Rehd.et Wils, which shows potent anti-inflammatory and analgesic effects. As a transforming disease-modifying anti-rheumatic drug, SIN has been used to treat rheumatoid arthritis over twenty-five years in China. In recent years, SIN is also in development for use against other disorders, including colitis, pain, traumatic brain injury, and uveitis. However, its commercial hydrochloride (SIN-HCl) shows low oral bioavailability and certain allergic reactions in patients, due to the release of histamine. Therefore, a large number of pharmaceutical strategies have been explored to address these liabilities, such as prolonging release behaviors, enhancing skin permeation and adsorption for transdermal delivery, targeted SIN delivery using new material or conjugates, and co-amorphous technology. This review discusses these different delivery strategies and approaches employed to overcome the limitations of SIN for its efficient delivery, in order to achieve improved bioavailability and reduced side effects. The potential advantages and limitations of SIN delivery strategies are elaborated along with discussions of potential future SIN drug development strategies.https://www.mdpi.com/1999-4923/14/12/2820rheumatoid arthritissinomeninehalf-lifeside effectdrug deliverydrug release behaviors |
| spellingShingle | Xin Chen Chengcheng Lu Yanwen Duan Yong Huang Recent Advancements in Drug Delivery of Sinomenine, A Disease-Modifying Anti-Rheumatic Drug Pharmaceutics rheumatoid arthritis sinomenine half-life side effect drug delivery drug release behaviors |
| title | Recent Advancements in Drug Delivery of Sinomenine, A Disease-Modifying Anti-Rheumatic Drug |
| title_full | Recent Advancements in Drug Delivery of Sinomenine, A Disease-Modifying Anti-Rheumatic Drug |
| title_fullStr | Recent Advancements in Drug Delivery of Sinomenine, A Disease-Modifying Anti-Rheumatic Drug |
| title_full_unstemmed | Recent Advancements in Drug Delivery of Sinomenine, A Disease-Modifying Anti-Rheumatic Drug |
| title_short | Recent Advancements in Drug Delivery of Sinomenine, A Disease-Modifying Anti-Rheumatic Drug |
| title_sort | recent advancements in drug delivery of sinomenine a disease modifying anti rheumatic drug |
| topic | rheumatoid arthritis sinomenine half-life side effect drug delivery drug release behaviors |
| url | https://www.mdpi.com/1999-4923/14/12/2820 |
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