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Newswise — Xiao et al reported on the natural product sinomenine (SIN), which is a traditional Chinese medicine for treating osteoporosis via its modulation of autophagy; however, SIN was dissolved in dimethyl sulfoxide prior to administration, which is not conducive to the development of clinical injectables. By comparing solubilization techniques, including amorphisation, emulsification, micellisation, nano-crystallisation and host-guest inclusion, we found that the solubilization of SIN by host-guest inclusion can enhance solubility and improve stability and has an increased release rate and enhanced bioavailability. Therefore, we conclude that host-guest inclusion holds promise for SIN solubilization. To solubilise SIN, we selected β-cyclodextrin as the host agent considering its excellent biocompatibility, efficient encapsulation ability, mature preparation process and adequate drug stability. If the prerequisites of SIN-β-cyclodextrin complexes in terms of safety, efficacy, stability and the relevant laws and regulations are met, its clinical application for the treatment of osteoporosis may be achieved.

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Core Tip: Sinomenine (SIN) inhibits phosphorylation processes in the phosphatidylinositol 3-kinase/protein kinase B/mammalian target of the rapamycin pathway, increases autophagic capacity and promotes osteogenic differentiation, hence effectively treating osteoporosis. Nevertheless, the insolubility of SIN is a limitation to its clinical application. Here, we proposed the use of host-guest inclusion instead of dimethyl sulfoxide (DMSO) to solubilise SIN by preparing SIN-β-cyclodextrin complexes. Compared with direct dissolution in DMSO, the SIN-β-cyclodextrin complexes circumvent the safety concerns associated with DMSO, providing higher water solubility, improved drug stability, lower toxicity and side effects and optimal drug release properties. We conclude the clinical application of SIN-β-cyclodextrin complexes to treat osteoporosis may be achieved.

• Citation: Guo MQ, Hu P, Huang ZW. Cyclodextrin host-guest complex to facilitate sinomenine-based osteoporosis therapy. World J Stem Cells 2025; 17(3): 101376
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