Metformin hydrochloride (MET) is commonly used in diabetes treatment. Recently, it has gained interest for its anticancer potential against a wide range of cancers. Owing to its hydrophilic nature, the delivery and clinical actions of MET are limited. Therefore, the present work aims to develop MET-encapsulated NLCs using the hot-melt emulsification and probe-sonication method. The optimization was accomplished by 3 BB design wherein lipid ratio, surfactant concentration, and sonication time were independent variables while the PS (nm), PDI, and EE (%) were dependent variables. The PS, PDI, % EE and ZP of optimized MET-NLCs were found to be 114.9 ± 1.32 nm, 0.268 ± 0.04 %, 60.10 ± 2.23 %, and ZP - 15.76 mV, respectively. The morphological features, DSC and PXRD, and FTIR analyses suggested the confirmation of formation of the NLCs. Besides, optimized MET-NLCs showed up to 88 % MET release in 24 h. Moreover, MET-NLCs showed significant cell cytotoxicity against KB oral cancer cells compared with MET solution as shown by the reduction of IC values. Additionally, MET-NLCs displayed significantly increased intracellular ROS levels suggesting the MET-NLCs induced cell death in KB cells. MET-NLCs can therefore be explored to deliver MET through different routes of administration for the effective treatment of oral cancer.

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http://dx.doi.org/10.1016/j.chemphyslip.2022.105256DOI Listing

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