Kim Taelin, Cho A Yeon, Lee Sang-Wha, Lee Hyun Jong
School of Chemical, Biological and Battery Engineering, Gachon University, Seongnam-si, Gyeonggi-do, Republic of Korea.
Int J Nanomedicine. 2024 Jun 8;19:5441-5458. doi: 10.2147/IJN.S463765. eCollection 2024.
Quercetin (QUER), a flavonoid abundant in fruits and vegetables, is emerging as a promising alternative therapeutic agent for obesity treatment due to its antioxidant and anti-adipogenic properties. However, the clinical application of QUER is limited by its poor solubility, low bioavailability, and potential toxicity at high doses. To address these challenges, this study aims to develop an advanced drug delivery system using fluorescent mesoporous silica nanoparticles (FMSNs) coated with polydopamine (PDA) for the efficient and sustained delivery of QUER to inhibit adipogenesis.
The research included the synthesis of PDA-coated FMSNs for encapsulation of QUER, characterization of their mesoporous structures, and systematic investigation of the release behavior of QUER. The DPPH assay was used to evaluate the sustained radical scavenging potential. Concentration-dependent effects on 3T3-L1 cell proliferation, cellular uptake and adipogenesis inhibition were investigated.
PDA-coated FMSNs exhibited well-aligned mesoporous structures. The DPPH assay confirmed the sustained radical scavenging potential, with FMSNs-QUER@PDA showing 53.92 ± 3.48% inhibition at 72 h, which was higher than FMSNs-QUER (44.66 ± 0.57%) and free QUER (43.37 ± 5.04%). Concentration-dependent effects on 3T3-L1 cells highlighted the enhanced efficacy of PDA-coated FMSNs for cellular uptake, with a 1.5-fold increase compared to uncoated FMSNs. Adipogenesis inhibition was also improved, with relative lipid accumulation of 44.6 ± 4.6%, 37.3 ± 4.6%, and 36.5 ± 7.3% at 2.5, 5, and 10 μM QUER concentrations, respectively.
The study successfully developed a tailored drug delivery system, emphasizing sustained QUER release and enhanced therapeutic effects. FMSNs, especially when coated with PDA, exhibit promising properties for efficient QUER delivery, providing a comprehensive approach that integrates advanced drug delivery technology and therapeutic efficacy.
槲皮素（QUER）是一种在水果和蔬菜中含量丰富的黄酮类化合物，由于其抗氧化和抗脂肪生成特性，正成为一种有前景的肥胖治疗替代药物。然而，QUER的临床应用受到其溶解度低、生物利用度低以及高剂量时潜在毒性的限制。为应对这些挑战，本研究旨在开发一种先进的药物递送系统，使用涂覆有聚多巴胺（PDA）的荧光介孔二氧化硅纳米颗粒（FMSNs）来高效持续递送QUER以抑制脂肪生成。
该研究包括合成用于包封QUER的PDA涂覆的FMSNs，表征其介孔结构，并系统研究QUER的释放行为。采用DPPH测定法评估持续的自由基清除潜力。研究了对3T3-L1细胞增殖、细胞摄取和脂肪生成抑制的浓度依赖性影响。
PDA涂覆的FMSNs呈现出排列良好的介孔结构。DPPH测定法证实了持续的自由基清除潜力，FMSNs-QUER@PDA在72小时时显示出53.92±3.48%的抑制率，高于FMSNs-QUER（44.66±0.57%）和游离QUER（43.37±5.04%）。对3T3-L1细胞的浓度依赖性影响突出了PDA涂覆的FMSNs在细胞摄取方面的增强功效，与未涂覆的FMSNs相比增加了1.5倍。脂肪生成抑制也得到改善，在2.5、5和10μM的QUER浓度下，相对脂质积累分别为44.6±4.6%、37.3±4.6%和36.5±7.3%。
该研究成功开发了一种定制的药物递送系统，强调了QUER的持续释放和增强的治疗效果。FMSNs，特别是涂覆有PDA时，在高效递送QUER方面表现出有前景的特性，提供了一种整合先进药物递送技术和治疗效果的综合方法。
