Liakopoulou Aggeliki, Letsiou Sophia, Avgoustakis Konstantinos, Patrinos George P, Lamari Fotini N, Hatziantoniou Sophia
Laboratory of Pharmaceutical Technology, Department of Pharmacy, School of Health Sciences, University of Patras, GR-265 04 Patras, Greece.
Laboratory of Pharmacogenomics and Individualized Therapy, Department of Pharmacy, School of Health Sciences, University of Patras, GR-265 04 Patras, Greece.
Pharmaceutics. 2025 Jan 21;17(2):144. doi: 10.3390/pharmaceutics17020144.
Oxidative stress significantly impacts skin health, contributing to conditions like aging, pigmentation, and inflammatory disorders. Curcumin, with its potent antioxidant properties, faces challenges of low solubility, stability, and bioavailability. This study aimed to encapsulate curcumin in three lipid nanocarriers-solid lipid nanoparticles (SLNs), nanostructured lipid carriers (NLCs), and nanoemulsions (NEs)-to enhance its stability, bioavailability, and antioxidant efficacy for potential therapeutic applications in oxidative-stress-related skin disorders. The lipid nanocarriers were characterized for size, polydispersity index, ζ-potential, and encapsulation efficiency. Stability tests under various conditions and antioxidant activity assays (DPPH and FRAP methods) were conducted. Cytotoxicity in human dermal fibroblasts was assessed using MTT assays, while the expression of key antioxidant genes was evaluated in human dermal fibroblasts under oxidative stress. Skin penetration studies were performed to analyze curcumin's distribution across the stratum corneum layers. All nanocarriers demonstrated high encapsulation efficiency and stability over 90 days. NLCs exhibited superior long-term stability and enhanced skin penetration, while NE formulations facilitated rapid antioxidant effects. Antioxidant assays confirmed that curcumin encapsulation preserved and enhanced its bioactivity, particularly in NLCs. Gene expression analysis revealed upregulation of key antioxidant markers (, , , , and ) with curcumin-loaded nanocarriers under oxidative and non-oxidative conditions. Cytotoxicity studies confirmed biocompatibility across all formulations. Lipid nanocarriers effectively enhance curcumin's stability, antioxidant activity, and skin penetration, presenting a targeted strategy for managing oxidative stress in skin applications. Their versatility offers opportunities for tailored therapeutic formulations addressing specific skin conditions, from chronic disorders like psoriasis to acute stress responses such as sunburn.
氧化应激对皮肤健康有显著影响，会导致衰老、色素沉着和炎症性疾病等状况。姜黄素具有强大的抗氧化特性，但面临着低溶解度、稳定性和生物利用度等挑战。本研究旨在将姜黄素封装在三种脂质纳米载体——固体脂质纳米粒（SLNs）、纳米结构脂质载体（NLCs）和纳米乳剂（NEs）中，以提高其稳定性、生物利用度和抗氧化功效，用于氧化应激相关皮肤疾病的潜在治疗应用。对脂质纳米载体的粒径、多分散指数、ζ电位和包封率进行了表征。进行了各种条件下的稳定性测试和抗氧化活性测定（DPPH和FRAP方法）。使用MTT法评估人皮肤成纤维细胞的细胞毒性，同时在氧化应激条件下评估人皮肤成纤维细胞中关键抗氧化基因的表达。进行皮肤渗透研究以分析姜黄素在角质层各层中的分布。所有纳米载体在90天内均表现出高包封率和稳定性。NLCs表现出卓越的长期稳定性和增强的皮肤渗透性，而NE制剂促进了快速的抗氧化作用。抗氧化测定证实，姜黄素的封装保留并增强了其生物活性，尤其是在NLCs中。基因表达分析显示，在氧化和非氧化条件下，负载姜黄素的纳米载体可上调关键抗氧化标志物（、、、和）。细胞毒性研究证实了所有制剂的生物相容性。脂质纳米载体有效地提高了姜黄素的稳定性、抗氧化活性和皮肤渗透性，为皮肤应用中管理氧化应激提供了一种靶向策略。它们的多功能性为针对特定皮肤状况定制治疗制剂提供了机会，从银屑病等慢性疾病到晒伤等急性应激反应。
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