{"title":"Formulation of apigenin-loaded solid lipid nanoparticles: characterisation, molecular docking, and anticancer assay.","authors":"Sadaf Jamal Gilani, Najla Altwaijry, Ahlam Mansour Sultan, Reem Basoudan, Reem Albesher, Kaneez Fatima","doi":"10.1080/00498254.2025.2517113","DOIUrl":null,"url":null,"abstract":"<p><p>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.</p><p><p>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.</p><p><p>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 <i>in vitro</i> 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.</p><p><p>4. Therefore, this study suggests that topical delivery of APN encapsulated in SLNs is a promising approach for skin cancer management.</p>","PeriodicalId":23812,"journal":{"name":"Xenobiotica","volume":" ","pages":"1-13"},"PeriodicalIF":1.3000,"publicationDate":"2025-06-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Xenobiotica","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1080/00498254.2025.2517113","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
引用次数: 0
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.
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