目的:癌症是全球第二大死亡原因,常规疗法受限于明显的副作用。褪黑素(MEL),一种具有抗肿瘤特性的天然化合物,具有不稳定性和低溶解度。为了克服这些问题,将MEL包封到含有玫瑰果油的纳米结构脂质载体(MEL-NLC)中以增强稳定性并增强其抗肿瘤活性。方法:通过实验设计方法对MEL-NLC进行优化,并对其理化性质进行表征。评估了稳定性和生物制药行为,以及对各种癌细胞系的相互作用研究和体外抗肿瘤功效。结果:优化的MEL-NLC表现出理想的物理化学特性,包括小粒径和持续的MEL释放,长期稳定。体外研究表明,MEL-NLC在几种癌细胞系中选择性诱导细胞毒性,同时保留健康细胞。结论:MEL-NLC是一种有希望的癌症替代方案,结合增强的稳定性和靶向抗肿瘤活性,有可能克服常规治疗的局限性。
尽管目前取得了进展,癌症是全球第二大死因,但是常规疗法有副作用和有限的疗效。自然疗法正在成为合适的替代品,其中,褪黑素是一种众所周知的具有抗肿瘤特性的化合物。然而,它被光降解,降低其治疗活性。为了有效地将褪黑素传递到癌细胞中,它已经被封装在含有玫瑰果油的可生物降解的纳米粒子中,这可能会增强抗肿瘤特性。这些纳米粒子已经过优化,显示小尺寸和高褪黑素封装,药物持续释放,稳定性好。此外,体外研究证明了对几种癌细胞系的抗肿瘤活性,也显示出它们内部的高度内化。此外,使用鸡胚鸡蛋进行的研究,表明纳米粒子是无毒的,从而证实了其有希望的治疗应用。
Aim: Cancer constitutes the second leading cause of death worldwide, with conventional therapies limited by significant side effects. Melatonin (MEL), a natural compound with antitumoral properties, suffers from instability and low solubility. To overcome these issues, MEL was encapsulated into nanostructured lipid carriers (MEL-NLC) containing rosehip oil to enhance stability and boost its antitumoral activity. Methods: MEL-NLC were optimized by a design of experiments approach and characterized for their physicochemical properties. Stability and biopharmaceutical behavior were assessed, along with interaction studies and in vitro antitumoral efficacy against various cancer cell lines. Results: Optimized MEL-NLC exhibited desirable physicochemical characteristics, including small particle size and sustained MEL release, along with long-term stability. In vitro studies demonstrated that MEL-NLC selectively induced cytotoxicity in several cancer cell lines while sparing healthy cells. Conclusion: MEL-NLC represent a promising alternative for cancer, combining enhanced stability and targeted antitumoral activity, potentially overcoming the limitations of conventional treatments.
Despite current advances, cancer is the second cause of death worldwide, but conventional therapies have side effects and limited efficacy. Natural therapies are emerging as suitable alternatives and, among them, Melatonin is a well-known compound with antitumoral properties. However, it is degraded by light, decreasing its therapeutical activity. In order to effectively deliver Melatonin into cancer cells, it has been encapsulated into biodegradable nanoparticles containing rosehip oil, which may boost the antitumoral properties. These nanoparticles have been optimized, showing a small size and a high Melatonin encapsulation, sustained drug release and good stability. Furthermore, in vitro studies demonstrated antitumoral activity against several cancer cell lines, also showing a high internalization inside them. Moreover, studies conducted using chicken embryonated eggs, showed that nanoparticles were non-toxic, thus confirming its promising therapeutical applications.