Nanostructured lipid carrier-loaded metformin hydrochloride: Design, optimization, characterization, assessment of cytotoxicity and ROS evaluation

IF 3.4 3区生物学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY Chemistry and Physics of Lipids Pub Date : 2023-01-01 DOI:10.1016/j.chemphyslip.2022.105256

Meghanath B. Shete , Ashwini S. Deshpande , Pravin K. Shende

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Abstract

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.

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纳米结构脂质载体负载盐酸二甲双胍:设计、优化、表征、细胞毒性评估和ROS评估

盐酸二甲双胍(Metformin hydrochloride, MET)常用于糖尿病的治疗。最近，它因其对多种癌症的抗癌潜力而引起了人们的兴趣。由于其亲水性，MET的输送和临床作用受到限制。因此，本工作旨在利用热熔乳化和探针超声方法开发met包封的NLCs。以脂质比、表面活性剂浓度、超声时间为自变量，PS (nm)、PDI、EE(%)为因变量，采用33 BB设计进行优化。优化后的GMSMET-NLCs的PS、PDI、% EE和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、DSC、PXRD和FTIR分析证实了NLCs的形成。此外，优化后的GMSMET-NLCs在24 h内的MET释放率高达88%。此外，与MET溶液相比，GMSMET-NLCs对KB口腔癌细胞表现出显著的细胞毒性，其IC50值降低。此外，GMSMET-NLCs显示细胞内ROS水平显著增加，表明GMSMET-NLCs诱导KB细胞死亡。因此，可以探索GMSMET-NLCs通过不同的给药途径提供MET，以有效治疗口腔癌。

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来源期刊

Chemistry and Physics of Lipids 生物-生化与分子生物学

CiteScore

7.60

自引率

2.90%

发文量

审稿时长

40 days

期刊介绍： Chemistry and Physics of Lipids publishes research papers and review articles on chemical and physical aspects of lipids with primary emphasis on the relationship of these properties to biological functions and to biomedical applications. Accordingly, the journal covers: advances in synthetic and analytical lipid methodology; mass-spectrometry of lipids; chemical and physical characterisation of isolated structures; thermodynamics, phase behaviour, topology and dynamics of lipid assemblies; physicochemical studies into lipid-lipid and lipid-protein interactions in lipoproteins and in natural and model membranes; movement of lipids within, across and between membranes; intracellular lipid transfer; structure-function relationships and the nature of lipid-derived second messengers; chemical, physical and functional alterations of lipids induced by free radicals; enzymatic and non-enzymatic mechanisms of lipid peroxidation in cells, tissues, biofluids; oxidative lipidomics; and the role of lipids in the regulation of membrane-dependent biological processes.