Ashfaq Rabia, Tóth Nóra, Kovács Anita, Berkó Szilvia, Katona Gábor, Ambrus Rita, Polgár Tamás Ferenc, Szécsényi Mária, Burián Katalin, Budai-Szűcs Mária
Institute of Pharmaceutical Technology and Regulatory Affairs, Faculty of Pharmacy, University of Szeged, H-6720 Szeged, Hungary.
Core Facility, HUN-REN Biological Research Centre, H-6726 Szeged, Hungary.
Pharmaceutics. 2025 May 7;17(5):620. doi: 10.3390/pharmaceutics17050620.
: This study aimed to develop and evaluate nanostructured lipid carriers (NLCs) loaded with meloxicam (Melox) and a therapeutic antibacterial and anti-inflammatory liquid lipid, clove oil (CO) for periodontitis treatment, a complex inflammatory condition necessitating advanced drug delivery systems. The NLC-Melox formulation was integrated into three hydrogels, hypromellose (HPMC), zinc hyaluronate (ZnHA), and sodium hyaluronate (NaHA), to conduct a comparative analysis focusing on enhanced localized drug delivery, improved mucoadhesion, prolonged retention, and significant therapeutic outcomes. NLC-Melox was prepared by homogenization and characterized by dynamic light scattering (DLS). Subsequently, NLC-Melox-loaded gels were subjected to transmission electron microscopy (TEM), differential scanning calorimetry (DSC), X-ray diffraction (XRD), Raman spectroscopy, and rheological analysis. In vitro drug release, anti-inflammatory activity (BSA denaturation assay), and antibacterial efficacy (MIC, MBC) were investigated to assess therapeutic potential. DLS revealed a particle size of 183 nm with a polydispersity index of 0.26, indicating homogeneity. TEM confirmed consistent morphology and uniform nanoparticle distribution. DSC and XRD demonstrated the amorphous nature of Melox, enhancing solubility and stability. Spectroscopy confirmed no chemical interactions between components. Rheological studies identified ZnHA as the most mucoadhesive and structurally stable gel. In vitro release studies showed sustained drug release over 24 h. Melox and CO-loaded formulations demonstrated significant anti-inflammatory activity and notable antibacterial efficacy due to the antibacterial oil. The study highlighted the potential of NLC-based mucoadhesive hydrogels as an effective strategy for periodontitis treatment. The formulation offered improved drug solubility, therapeutic efficacy, mucoadhesivity, and prolonged delivery, making it a promising candidate for localized therapy.
本研究旨在开发和评估负载美洛昔康(Melox)以及治疗性抗菌和抗炎液态脂质丁香酚(CO)的纳米结构脂质载体(NLCs)用于治疗牙周炎,牙周炎是一种复杂的炎症性疾病,需要先进的药物递送系统。将NLC-Melox制剂整合到三种水凝胶中,即羟丙甲纤维素(HPMC)、透明质酸锌(ZnHA)和透明质酸钠(NaHA),以进行比较分析,重点关注增强局部药物递送、改善粘膜粘附性、延长滞留时间和显著的治疗效果。通过均质法制备NLC-Melox,并通过动态光散射(DLS)进行表征。随后,对负载NLC-Melox的凝胶进行透射电子显微镜(TEM)、差示扫描量热法(DSC)、X射线衍射(XRD)、拉曼光谱和流变学分析。研究体外药物释放、抗炎活性(牛血清白蛋白变性试验)和抗菌功效(MIC、MBC)以评估治疗潜力。DLS显示粒径为183 nm,多分散指数为0.26,表明具有均一性。TEM证实形态一致且纳米颗粒分布均匀。DSC和XRD证明美洛昔康为无定形性质,提高了溶解度和稳定性。光谱学证实各组分之间无化学相互作用。流变学研究确定ZnHA是粘膜粘附性最强且结构最稳定的凝胶。体外释放研究表明药物在24小时内持续释放。负载美洛昔康和丁香酚的制剂由于含有抗菌油而表现出显著的抗炎活性和显著的抗菌功效。该研究强调了基于NLC的粘膜粘附水凝胶作为牙周炎治疗有效策略的潜力。该制剂提高了药物溶解度、治疗功效、粘膜粘附性并延长了递送时间,使其成为局部治疗的有前景的候选药物。