Laboratoire des Substances Bioactives, Centre de Biotechnologie de Borj-Cedria, BP 901, Hammam-Lif 2050, Tunisia.
Valorization of Useful Material Laboratory (LVMU), National Research Center in Material Sciences (CNRSM) Technopôle Borj Cedria, BP 73, Soliman 8027, Tunisia.
Molecules. 2023 Jul 27;28(15):5681. doi: 10.3390/molecules28155681.
Nanoencapsulation is widely considered as a highly effective strategy to enhance essential oils' (EO) stability by protecting them from oxidative deterioration and evaporation. The present study aims to optimize and characterize an efficient technique for encapsulating essential oil into chitosan nanoparticles using response surface methodology (RSM). Moreover, the optimized EO nanoparticle was investigated for its antibacterial (against Gram-positive and Gram-negative bacteria), antifungal (against ), and antiparasitic activity (against parasites). Five parameters were investigated using a Plackett-Burman and Box-Behnken statistical design: the chitosan molecular weight, TPP concentration, EO/chitosan ratio, mixing method, and the duration of the reaction. Encapsulation efficiency and anti-candida activity were considered as responses. The antibacterial, anticandidal, and anti-leishmanial activities were also assessed using a standard micro-broth dilution assay and the cytotoxicity assay was assessed against the macrophage cell line RAW 264.7. The optimized nanoparticles were characterized using Fourier transform infrared spectroscopy, Zeta potential, and scanning electron microscopy. The study results indicated that under optimal conditions, the nanoencapsulation of EO into chitosan nanoparticles resulted in an encapsulation efficiency of 92.58%, with a regular distribution, a nanoparticle size of 480 ± 14.55 nm, and a favorable Zeta potential of 35.64 ± 1.37 mV. The optimized EO/chitosan nanoparticles showed strong antifungal activity against pathogens (CMI = 125 µg mL), notable antibacterial activity against both Gram-positive and Gram-negative bacteria (ranging from 125 to 250 µg mL), high leishmanicidal potential against the promastigotes form of and (IC50 = 10.47 and 15.09 µg mL, respectively), and a four-fold cytotoxicity reduction compared to non-encapsulated essential oil. These results suggest that EO-loaded chitosan nanoparticles could be a promising delivery system for the treatment of cutaneous infections.
纳米胶囊化被广泛认为是一种通过保护精油免受氧化劣化和蒸发来提高其稳定性的有效策略。本研究旨在使用响应面法（RSM）优化和表征将精油包封到壳聚糖纳米粒子中的有效技术。此外，还研究了优化的精油纳米粒子的抗菌（针对革兰氏阳性和革兰氏阴性细菌）、抗真菌（针对 ）和抗寄生虫活性（针对 寄生虫）。使用 Plackett-Burman 和 Box-Behnken 统计设计研究了五个参数：壳聚糖分子量、TPP 浓度、精油/壳聚糖比、混合方法和反应时间。包封效率和抗念珠菌活性被视为响应。还使用标准微量肉汤稀释法评估了抗菌、抗真菌和抗利什曼原虫活性，并使用巨噬细胞 RAW 264.7 细胞系评估了细胞毒性。使用傅里叶变换红外光谱、Zeta 电位和扫描电子显微镜对优化的纳米粒子进行了表征。研究结果表明，在最佳条件下，将精油纳米胶囊化到壳聚糖纳米粒子中可获得 92.58%的包封效率，具有规则的分布、纳米粒子尺寸为 480 ± 14.55nm 和有利的 Zeta 电位 35.64 ± 1.37mV。优化的精油/壳聚糖纳米粒子对病原体表现出强烈的抗真菌活性（CMI = 125µgmL），对革兰氏阳性和革兰氏阴性细菌均表现出显著的抗菌活性（范围为 125 至 250µgmL），对前鞭毛体形式的 和 具有高杀利什曼原虫潜力（IC50 分别为 10.47 和 15.09µgmL），与未包封的精油相比，细胞毒性降低了四倍。这些结果表明，负载精油的壳聚糖纳米粒子可能是治疗皮肤 感染的有前途的给药系统。
