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• W3142092103 endingPage "115511" @default.
• W3142092103 startingPage "115511" @default.
• W3142092103 abstract "Hesperetin (HSP) has excellent biological activities with poor water solubility which limits its clinical development. In this study, we successfully prepared a novel, self-assembled micelle based on Rebaudioside A (RA) for oral delivery of HSP with improved bioavailability and therapeutic effects. We found that RA and HSP could be formylated into nanomicelles with particle sizes of 4.541 nm ± 0.048 nm. HSP was readily encapsulated into RA micelles and this improved its water solubility (to 12.74 mg/mL ± 0.28 mg/mL). The MTT results showed that RA-HSP enhanced the cytotoxicity, the clonal formation inhibitory activity, and cell migration inhibitory activity of HSP in human breast cancer MDA-MB-231 cells. The mechanism results showed that RA-HSP induced cell apoptosis by inducing the production of reactive oxygen species (ROS), destroying the mitochondrial membrane potential (MMP), and inhibiting the PI3K/Akt signaling pathway. Moreover, RA-HSP enhanced the anticancer activity, increased the oral bioavailability and tissue distribution of HSP in vivo. Moreover, the mechanism studies in vivo found that HSP inhibited PI3K/Akt signaling pathway with low side effects. These findings indicate that RA micelle formulations have great potential in oral drug delivery systems for the delivery of hydrophobic drugs." @default.
• W3142092103 created "2021-04-13" @default.
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• W3142092103 date "2021-05-01" @default.
• W3142092103 modified "2023-10-16" @default.
• W3142092103 title "Improved bioavailability and anticancer efficacy of Hesperetin on breast cancer via a self-assembled rebaudioside A nanomicelles system" @default.
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• W3142092103 doi "https://doi.org/10.1016/j.taap.2021.115511" @default.
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