Rizg Waleed Y, Hosny Khaled M, Mahmoud Samar S, Kammoun Ahmed K, Alamoudi Abdulmohsin J, Tayeb Hossam H, Bukhary Haitham A, Badr Moutaz Y, Murshid Samar S A, Alfayez Eman, Ali Sarah A, Mushtaq Rayan Y, Abualsunun Walaa A
Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia.
Center of Excellence for Drug Research and Pharmaceutical Industries, King Abdulaziz University, Jeddah 21589, Saudi Arabia.
Gels. 2022 Mar 12;8(3):176. doi: 10.3390/gels8030176.
Tongue cancer is one of the most common carcinomas of the head and neck region. The antitumor activities of statins, including lovastatin (LV), and the essential oil of eucalyptus (Eu oil), have been adequately reported. The aim of this study was to develop a nanoemulgel containing LV combined with Eu oil that could then be made into a nanoemulsion and assessed to determine its cytotoxicity against the cell line human chondrosarcoma-3 (HSC3) of carcinoma of the tongue. An I-optimal coordinate-exchange quadratic mixture design was adopted to optimize the investigated nanoemulsions. The droplet size and stability index of the developed formulations were measured to show characteristics of the nanoemulsions. The optimized LV loaded self-nanoemulsifying drug delivery system (LV-Eu-SNEDDS) was loaded into the gelling agent Carbopol 934 to develop the nanoemulgel and evaluated for its rheological properties. The cytotoxic efficiency of the optimized LV-Eu-SNEDDS loaded nanoemulgel was tested for cell viability, and the caspase-3 enzyme test was used against the HSC3 cell line of squamous carcinoma of the tongue. The optimized nanoemulsion had a droplet size of 85 nm and a stability index of 93%. The manufactured nanoemulgel loaded with the optimum LV-Eu-SNEDDS exhibited pseudoplastic flow with thixotropic behavior. The developed optimum LV-Eu-SNEDDS-loaded nanoemulgel had the best half-maximal inhibitory concentration (IC) and caspase-3 enzyme values of the formulations developed for this study, and these features improved the ability of the nanoemulsion-loaded gel to deliver the drug to the investigated target cells. In addition, the in vitro cell viability studies revealed the synergistic effect between LV and Eu oil in the treatment of tongue cancer. These findings illustrated that the LV-Eu-SNEDDS-loaded gel formulation could be beneficial in the local treatment of tongue cancer.
舌癌是头颈部最常见的癌症之一。他汀类药物(包括洛伐他汀(LV))和桉叶精油(Eu油)的抗肿瘤活性已有充分报道。本研究的目的是开发一种含有LV与Eu油的纳米乳凝胶,然后将其制成纳米乳液,并评估其对舌癌人软骨肉瘤-3(HSC3)细胞系的细胞毒性。采用I-最优坐标变换二次混合设计优化所研究的纳米乳液。测量所开发制剂的液滴大小和稳定性指数以显示纳米乳液的特性。将优化的载有LV的自纳米乳化药物递送系统(LV-Eu-SNEDDS)负载到胶凝剂卡波姆934中以制备纳米乳凝胶,并评估其流变学性质。测试优化的载有LV-Eu-SNEDDS的纳米乳凝胶的细胞毒性效率以检测细胞活力,并使用半胱天冬酶-3酶试验针对舌鳞状细胞癌的HSC3细胞系进行检测。优化后的纳米乳液液滴大小为85 nm,稳定性指数为93%。制备的负载最佳LV-Eu-SNEDDS的纳米乳凝胶表现出具有触变性的假塑性流动。所开发的最佳负载LV-Eu-SNEDDS的纳米乳凝胶在本研究开发的制剂中具有最佳的半数最大抑制浓度(IC)和半胱天冬酶-3酶值,这些特性提高了负载纳米乳液的凝胶将药物递送至所研究靶细胞的能力。此外,体外细胞活力研究揭示了LV和Eu油在舌癌治疗中的协同作用。这些发现表明,负载LV-Eu-SNEDDS的凝胶制剂可能对舌癌的局部治疗有益。