Silva Pontes Cristiano, Garcia de Carvalho Gabriel, Rosa Perin Leite Andressa, Chorilli Marlus, Palomari Spolidorio Denise Madalena
Department of Physiology and Pathology, School of Dentistry at Araraquara, São Paulo State University (Unesp), Araraquara 14801-903, SP, Brazil.
Department of Dental Materials and Prosthodontics, School of Dentistry, São Paulo State University (Unesp), Rua Humaitá, 1680, Araraquara 14801-903, SP, Brazil.
Pharmaceutics. 2023 Oct 17;15(10):2475. doi: 10.3390/pharmaceutics15102475.
Geraniol (GE) is a monoterpene alcohol with excellent antifungal activity. However, its low solubility and high volatility impair its use. Nanoemulsions (NE) are excellent delivery systems for poorly soluble and volatile drugs, achieving controlled release of the active ingredient. The aim of this study was to improve the delivery of geraniol (GE) incorporated in NE against in order to evaluate the antibiofilm effect and cytotoxicity. Nanoemulsion containing 10% oil phase (cholesterol) (/), 10% surfactant (mixture of soy phosphatidylcholine and Brij 58; 1:2) (/), and 80% aqueous phase (phosphate buffer) (/) was synthesized. Incorporation of GE was carried out by sonication and the final compounds were characterized by hydrodynamic diameter, polydispersity index (PDI), and zeta potential (ZP), in addition to evaluation of physicochemical stability after 6 months and 1 year. The GE-NE effect was evaluated on biofilms and cytotoxic effect was evaluated on immortalized normal oral cell line NOK-Si. The diameter of GE-NE was 232.3 ± 2.7 nm and PDI 0.155 with exhibited homogeneity and stability in solution. GE-NE showed antibiofilm activity at a concentration of 75 μg/mL with reduction of >6.0 log, and no cytotoxicity against NOK-Si cells at concentrations below 150 μg/mL was observed. GE-NE proved to be a promising candidate for prevention and treatment of fungal diseases.
香叶醇（GE）是一种具有出色抗真菌活性的单萜醇。然而，其低溶解度和高挥发性限制了它的应用。纳米乳剂（NE）是难溶性和挥发性药物的优良递送系统，可实现活性成分的控释。本研究的目的是改善纳米乳剂中香叶醇（GE）的递送效果，以评估其抗生物膜作用和细胞毒性。合成了含有10%油相（胆固醇）（/）、10%表面活性剂（大豆磷脂酰胆碱和Brij 58的混合物；1:2）（/）和80%水相（磷酸盐缓冲液）（/）的纳米乳剂。通过超声处理将GE掺入其中，最终化合物通过流体动力学直径、多分散指数（PDI）和zeta电位（ZP）进行表征，此外还评估了6个月和1年后的物理化学稳定性。评估了GE-NE对生物膜的作用，并在永生化正常口腔细胞系NOK-Si上评估了细胞毒性作用。GE-NE的直径为232.3±2.7 nm，PDI为0.155，在溶液中表现出均匀性和稳定性。GE-NE在浓度为75μg/mL时显示出抗生物膜活性，对数减少>6.0，在浓度低于150μg/mL时未观察到对NOK-Si细胞的细胞毒性。GE-NE被证明是预防和治疗真菌疾病的有前景的候选物。
