Journal
PHARMACEUTICS
Volume 14, Issue 12, Pages -Publisher
MDPI
DOI: 10.3390/pharmaceutics14122820
Keywords
rheumatoid arthritis; sinomenine; half-life; side effect; drug delivery; drug release behaviors
Categories
Funding
- National Natural Science Foundation of China
- Chinese Ministry of Education 111 Project
- science and technology innovation Program of Hunan Province
- Hunan Provincial Natural Science Foundation of China
- Fundamental Research Funds for the Central Universities of Central South University
- [82173688]
- [BP0820034]
- [2021RC4067]
- [2021JJ30791]
- [2021zzts1006]
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Sinomenine is a benzyltetrahydroisoquinoline-type alkaloid with potent anti-inflammatory and analgesic effects, used for over 25 years in China to treat rheumatoid arthritis. However, its commercial hydrochloride form has low oral bioavailability and allergic reactions, requiring pharmaceutical strategies to improve delivery efficiency and reduce side effects.
Sinomenine (SIN) is a benzyltetrahydroisoquinoline-type alkaloid isolated from the dried plant root and stem of Sinomenium acutum (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.
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