Shete Meghanath B, Deshpande Ashwini S, Shende Pravin K
School of Pharmacy & Technology Management, SVKM'S NMIMS, Shirpur, Maharashtra, India; Department of Pharmaceutical Quality Assurance, R C Patel Institute of Pharmaceutical Education and Research, Shirpur, Dist., Dhule 425405, Maharashtra, India.
School of Pharmacy & Technology Management, SVKM'S NMIMS, Polepally SEZ, TSIIC Jadcherla, Hyderabad 509301, India.
Chem Phys Lipids. 2023 Jan;250:105256. doi: 10.1016/j.chemphyslip.2022.105256. Epub 2022 Nov 11.
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.
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，本研究旨在采用热熔乳化和探头超声法制备包封MET的纳米脂质载体（NLCs）。通过三因素三水平设计进行优化，其中脂质比例、表面活性剂浓度和超声时间为自变量，而粒径（PS，nm）、多分散指数（PDI）和包封率（EE，%）为因变量。优化后的MET-NLCs的PS、PDI、% EE和ζ电位（ZP）分别为114.9 ± 1.32 nm、0.268 ± 0.04%、60.10 ± 2.23%和ZP - 15.76 mV。形态特征、差示扫描量热法（DSC）、粉末X射线衍射（PXRD）和傅里叶变换红外光谱（FTIR）分析表明已确认形成了NLCs。此外，优化后的MET-NLCs在24小时内的MET释放率高达88%。此外，与MET溶液相比，MET-NLCs对KB口腔癌细胞显示出显著的细胞毒性，IC值降低表明了这一点。此外，MET-NLCs显示细胞内活性氧水平显著升高，表明MET-NLCs诱导KB细胞死亡。因此，可以探索通过不同给药途径递送MET的MET-NLCs用于口腔癌的有效治疗。
