Department of Pharmacy, Pharmaceutical Technology & Physical Chemistry, University of Barcelona, Barcelona, 08028, Spain.
Institute of Nanoscience & Nanotechnology (IN2UB), University of Barcelona, Barcelona, 08028, Spain.
Nanomedicine (Lond). 2024;19(23):1879-1894. doi: 10.1080/17435889.2024.2379757. Epub 2024 Aug 2.
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. 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 antitumoral efficacy against various cancer cell lines. Optimized MEL-NLC exhibited desirable physicochemical characteristics, including small particle size and sustained MEL release, along with long-term stability. studies demonstrated that MEL-NLC selectively induced cytotoxicity in several cancer cell lines while sparing healthy cells. MEL-NLC represent a promising alternative for cancer, combining enhanced stability and targeted antitumoral activity, potentially overcoming the limitations of conventional treatments.
癌症是全球第二大致死原因,传统疗法受到严重副作用的限制。具有抗肿瘤特性的天然化合物褪黑素(MEL),其稳定性和低溶解度较差。为了克服这些问题,MEL 被封装到含有玫瑰果油的纳米结构化脂质载体(MEL-NLC)中,以提高其稳定性并增强其抗肿瘤活性。通过实验设计方法对 MEL-NLC 进行了优化,并对其理化性质进行了表征。评估了稳定性和生物药剂学行为,以及相互作用研究和对各种癌细胞系的抗肿瘤功效。优化后的 MEL-NLC 表现出理想的理化特性,包括小粒径和持续的 MEL 释放,以及长期稳定性。研究表明,MEL-NLC 选择性诱导几种癌细胞系的细胞毒性,同时对健康细胞无毒性。MEL-NLC 为癌症提供了一种有前途的替代方法,结合了增强的稳定性和靶向抗肿瘤活性,可能克服传统治疗方法的局限性。