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Nanostructured lipid carrier-loaded metformin hydrochloride: Design, optimization, characterization, assessment of cytotoxicity and ROS evaluation
Chemistry and Physics of Lipids ( IF 3.4 ) Pub Date : 2022-11-11 , DOI: 10.1016/j.chemphyslip.2022.105256
Meghanath B Shete 1 , Ashwini S Deshpande 2 , Pravin K Shende 3
Affiliation  

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 33 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 GMSMET-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 GMSMET-NLCs showed up to 88 % MET release in 24 h. Moreover, GMSMET-NLCs showed significant cell cytotoxicity against KB oral cancer cells compared with MET solution as shown by the reduction of IC50 values. Additionally, GMSMET-NLCs displayed significantly increased intracellular ROS levels suggesting the GMSMET-NLCs induced cell death in KB cells. GMSMET-NLCs can therefore be explored to deliver MET through different routes of administration for the effective treatment of oral cancer.



中文翻译:

纳米结构脂质载体负载二甲双胍盐酸盐:设计、优化、表征、细胞毒性评估和 ROS 评估

盐酸二甲双胍 (MET) 常用于糖尿病治疗。最近,它因其对多种癌症的抗癌潜力而受到关注。由于其亲水性,MET 的递送和临床作用受到限制。因此,目前的工作旨在使用热熔乳化和探针超声法开发 MET 包封的 NLC。优化是通过 3 3 BB 设计完成的,其中脂质比率、表面活性剂浓度和超声处理时间是自变量,而 PS (nm)、PDI 和 EE (%) 是因变量。优化后的GMS的 PS、PDI、% EE 和 ZPMET-NLC 被发现分别为 114.9 ± 1.32 nm、0.268 ± 0.04 %、60.10 ± 2.23 % 和 ZP − 15.76 mV。形态学特征、DSC 和 PXRD 以及 FTIR 分析表明已确认 NLC 的形成。此外,优化的GMS MET-NLCs 在 24 小时内显示出高达 88% 的 MET 释放。此外,与 MET 溶液相比, GMS MET-NLC 显示出对 KB 口腔癌细胞的显着细胞毒性,如 IC 50值的降低所示。此外,GMS MET-NLCs 显示细胞内 ROS 水平显着增加,表明GMS MET-NLCs 诱导 KB 细胞死亡。全球管理系统因此,可以探索 MET-NLCs 通过不同的给药途径递送 MET,以有效治疗口腔癌。

更新日期:2022-11-11
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