Cyclodextrin host-guest complex to facilitate sinomenine-based osteoporosis therapy.

Abstract

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.