Formulation of apigenin-loaded solid lipid nanoparticles: characterisation, molecular docking, and anticancer assay.

IF 1.3 4区 医学 Q4 PHARMACOLOGY & PHARMACY
Sadaf Jamal Gilani, Najla Altwaijry, Ahlam Mansour Sultan, Reem Basoudan, Reem Albesher, Kaneez Fatima
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Abstract

1. Apigenin (APN), a natural flavonoid, showed strong therapeutic potential against skin cancer, but its clinical use is restricted due to its complex physicochemical characteristics.

2. Hence, this study aimed to fabricate APN-loaded solid lipid nanoparticles (APN-SLNs) for improved topical treatment of skin cancer. The developed APN-SLNs were evaluated for particle characterization, compatibility and crystallinity by employing FT-IR, DSC, and XRD. The selected APN-SLNs-loaded hydrogels further evaluated for gel evaluation, permeation and cytotoxicity assessment. The findings also supported with molecular docking study.

3. The developed APN-SLNs demonstrated nanometric size, low polydispersity index, negative surface charge, high encapsulation efficiency and a biphasic release profile. The developed APN-SLNs-loaded hydrogels represented comparatively higher viscosity, firmness, consistency, and cohesiveness compared with the pure APN-loaded hydrogels. The APN-SLNs-loaded hydrogels represented >2 times higher in vitro permeation than pure APN-loaded hydrogels. Further, MTT assay using B16-F10 melanoma cells revealed the superior cytotoxic potential of the developed nanocarrier than the native counterpart. The docking study also supports the findings of the cell viability assay with a high docking score.

4. Therefore, this study suggests that topical delivery of APN encapsulated in SLNs is a promising approach for skin cancer management.

芹菜素负载固体脂质纳米颗粒的配方:表征,分子对接和抗癌测定。
芹菜素(Apigenin, APN)是一种天然类黄酮,具有很强的抗皮肤癌治疗潜力,但其复杂的理化特性限制了其临床应用。脂质纳米载体局部治疗皮肤癌具有多种优势。因此,本研究旨在制备负载apn的固体脂质纳米颗粒(apn - sln),以改善皮肤癌的局部治疗。将纯APN和APN- sln进一步装入水凝胶中,以更好地外用。制备的apn - sln平均尺寸为174.3±6.7 nm,多分散性指数为0.18±0.02,表面电荷为-29.5±2.9 mV,封装效率为85.7±3.5%。采用FT-IR、DSC和XRD对制备的apn - sln的相容性和结晶度进行了评价。所制备的apn - sln具有优异的胶体稳定性和双相释放特性。与纯apn负载的水凝胶相比,所开发的apn - sln负载的水凝胶具有更高的粘度、硬度、稠度和内聚性。负载apn - sln的水凝胶比纯负载apn的水凝胶的体外渗透率高2倍。此外,使用B16-F10黑色素瘤细胞的MTT试验显示,开发的纳米载体比天然载体具有更高的细胞毒性潜力。该对接研究也支持了高对接评分的细胞活力测定结果。因此,这项研究表明,局部递送包裹在sln中的APN是一种很有前途的皮肤癌治疗方法。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
Xenobiotica
Xenobiotica 医学-毒理学
CiteScore
3.80
自引率
5.60%
发文量
96
审稿时长
2 months
期刊介绍: Xenobiotica covers seven main areas, including:General Xenobiochemistry, including in vitro studies concerned with the metabolism, disposition and excretion of drugs, and other xenobiotics, as well as the structure, function and regulation of associated enzymesClinical Pharmacokinetics and Metabolism, covering the pharmacokinetics and absorption, distribution, metabolism and excretion of drugs and other xenobiotics in manAnimal Pharmacokinetics and Metabolism, covering the pharmacokinetics, and absorption, distribution, metabolism and excretion of drugs and other xenobiotics in animalsPharmacogenetics, defined as the identification and functional characterisation of polymorphic genes that encode xenobiotic metabolising enzymes and transporters that may result in altered enzymatic, cellular and clinical responses to xenobioticsMolecular Toxicology, concerning the mechanisms of toxicity and the study of toxicology of xenobiotics at the molecular levelXenobiotic Transporters, concerned with all aspects of the carrier proteins involved in the movement of xenobiotics into and out of cells, and their impact on pharmacokinetic behaviour in animals and manTopics in Xenobiochemistry, in the form of reviews and commentaries are primarily intended to be a critical analysis of the issue, wherein the author offers opinions on the relevance of data or of a particular experimental approach or methodology
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