Department of Pharmaceutics, Faculty of Pharmacy, University of Tabuk, Tabuk 71491, Saudi Arabia.
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Tabuk, Tabuk 71491, Saudi Arabia.
Int J Pharm. 2024 Dec 5;666:124761. doi: 10.1016/j.ijpharm.2024.124761. Epub 2024 Sep 25.
Diabetic wounds pose a significant global health challenge. Although curcumin exhibits promising wound healing and antibacterial properties, its clinical potential is limited by low aqueous solubility, and poor tissue penetration. This study aimed to address these challenges and enhance the wound healing efficacy of curcumin by loading it onto gold nanoparticles (AuNPs). The properties of the AuNPs, including particle size, polydispersity index (PDI), zeta potential, percent drug entrapment efficiency (%EE) and UV-Vis spectra were significantly influenced by the curcumin/gold chloride molar ratio used in the synthesis of AuNPs. The optimal formulation (F2) exhibited the smallest particle size (41.77 ± 6.8 nm), reasonable PDI (0.59 ± 0.17), high %EE (94.43 ± 0.25 %), a moderate zeta potential (-8.44 ± 1.69 mV), and a well-defined surface Plasmon resonance peak at 526 nm. Formulation F2 was incorporated into Pluronic® F127 gel to facilitate its application to the skin. Both curcumin AuNPs solution and gel showed sustained drug release and higher skin permeation parameters compared with the free drug solution. AuNPs significantly enhanced curcumin's antibacterial efficacy by lowering the minimum inhibitory concentrations and enhancing antibacterial biofilm activity against various Gram-positive and Gram-negative bacterial strains. In a diabetic wound rat model, AuNPs-loaded curcumin exhibited superior wound healing attributes compared to the free drug. Specifically, it demonstrated improved wound healing percentage, reduced wound oxidative stress, increased wound collagen deposition, heightened anti-inflammatory effects, and enhanced angiogenesis. These findings underscore the potential of AuNPs as efficacious delivery systems of curcumin for improved wound healing applications.
糖尿病伤口是一个重大的全球健康挑战。尽管姜黄素具有有前景的伤口愈合和抗菌特性，但由于其低水溶解度和组织穿透性差，其临床潜力受到限制。本研究旨在通过将其负载到金纳米粒子（AuNPs）上来解决这些挑战并提高姜黄素的伤口愈合功效。AuNPs 的性质，包括粒径、多分散指数（PDI）、zeta 电位、药物包封效率（%EE）和紫外可见光谱，都受到用于合成 AuNPs 的姜黄素/氯化金摩尔比的显著影响。最佳配方（F2）表现出最小的粒径（41.77 ± 6.8 nm）、合理的 PDI（0.59 ± 0.17）、高的%EE（94.43 ± 0.25%）、适度的 zeta 电位（-8.44 ± 1.69 mV）和在 526 nm 处有明显的表面等离子体共振峰。将配方 F2 掺入泊洛沙姆 F127 凝胶中，以方便其应用于皮肤。姜黄素 AuNPs 溶液和凝胶均表现出与游离药物溶液相比，具有持续的药物释放和更高的皮肤渗透参数。AuNPs 通过降低最小抑菌浓度和增强对各种革兰氏阳性和革兰氏阴性细菌菌株的抗菌生物膜活性，显著提高了姜黄素的抗菌功效。在糖尿病伤口大鼠模型中，负载 AuNPs 的姜黄素与游离药物相比，表现出优越的伤口愈合特性。具体而言，它显示出改善的伤口愈合百分比、减少的伤口氧化应激、增加的伤口胶原沉积、增强的抗炎作用和增强的血管生成。这些发现强调了 AuNPs 作为姜黄素有效传递系统的潜力，可用于改善伤口愈合应用。
