A comparative study on stevioside- and rubusoside-assisted micellar solubilization of clofazimine for physicochemical and in vitro release properties

Fuente: PubMed "agrofood sustainability"
Int J Pharm X. 2025 Oct 24;10:100424. doi: 10.1016/j.ijpx.2025.100424. eCollection 2025 Dec.ABSTRACTThis study compares the micellization and encapsulation abilities of stevioside (STE) and rubusoside (RUB) for enhancing the solubility, stability, and bioavailability of clofazimine (CFZ), a poorly water-soluble antibiotic. CFZ-loaded micelles were prepared and characterized by FT-IR, XRD, DSC, SEM, and NMR. RUB showed a lower critical micelle concentration and significantly improved CFZ solubility (up to 2.06 mg/mL) compared to STE. CFZ-RUB complexes offered greater protection against UV and oxidative degradation. In vitro release tests indicated sustained and enhanced CFZ release in simulated gastrointestinal fluids. CFZ-RUB also showed higher permeability across Caco-2 cell monolayers (62.5 %) and reduced cytotoxicity versus free CFZ. These results suggest that RUB's amphiphilic structure facilitates stable micelle formation and efficient drug loading. Overall, RUB presents a promising natural solubilizer and oral delivery vehicle for lipophilic bioactives in food and pharmaceutical applications, providing new insights into the structure-function roles of steviol glycosides.PMID:41230037 | PMC:PMC12603695 | DOI:10.1016/j.ijpx.2025.100424