Carbone Claudia, Teixeira Maria do Céu, Sousa Maria do Céu, Martins-Gomes Carlos, Silva Amelia M, Souto Eliana Maria Barbosa, Musumeci Teresa
Laboratory of Drug Delivery Technology, Department of Drug Sciences, University of Catania, viale A. Doria 6, 95125 Catania, Italy.
Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Coimbra (FFUC), 3030-548 Coimbra, Portugal.
Pharmaceutics. 2019 May 13;11(5):231. doi: 10.3390/pharmaceutics11050231.
The increasing development of resistance of species to traditional drugs represents a great challenge to the medical field for the treatment of skin infections. Essential oils were recently proposed to increase drug effectiveness. Herein, we developed and optimized (2 full factorial design) Mediterranean essential oil (, x "Sumian", subsp. ) lipid nanoparticles for clotrimazole delivery, exploring the potential synergistic effects against spp. Small sized nanoparticles (<100 nm) with a very broad size distribution (PDI < 0.15) and long-term stability were successfully prepared. Results of the in vitro biosafety on HaCaT (normal cell line) and A431 (tumoral cell line), allowed us to select and as anti-proliferative agents with the potential to be used as co-adjuvants in the treatment of non-tumoral proliferative dermal diseases. Results of calorimetric studies on biomembrane models, confirmed the potential antimicrobial activity of the selected oils due to their interaction with membrane permeabilization. Nanoparticles provided a prolonged in vitro release of clotrimazole. In vitro studies against , and , showed an increase of the antifungal activity of clotrimazole-loaded nanoparticles prepared with or , thus confirming nanostructured lipid carriers (NLC) containing Mediterranean essential oils represent a promising strategy to improve drug effectiveness against topical candidiasis.
物种对传统药物的耐药性不断增强，这给皮肤感染治疗的医学领域带来了巨大挑战。最近有人提出使用精油来提高药物疗效。在此，我们开发并优化了（2全因子设计）用于递送克霉唑的地中海精油（，x“Sumian”，亚种）脂质纳米颗粒，探索其对 spp. 的潜在协同作用。成功制备了尺寸小（<100 nm）、尺寸分布非常宽（PDI < 0.15）且具有长期稳定性的纳米颗粒。对HaCaT（正常细胞系）和A431（肿瘤细胞系）的体外生物安全性研究结果，使我们能够选择 和 作为抗增殖剂，它们有可能在非肿瘤性增殖性皮肤病的治疗中用作辅助剂。对生物膜模型的量热研究结果证实，所选精油由于与膜通透性相互作用而具有潜在的抗菌活性。纳米颗粒使克霉唑在体外实现了长效释放。针对 、 和 的体外研究表明，用 或 制备的载克霉唑纳米颗粒的抗真菌活性有所提高，从而证实含有地中海精油的纳米结构脂质载体（NLC）是提高针对局部念珠菌病药物疗效的一种有前景的策略。
