Antitumoral melatonin-loaded nanostructured lipid carriers.

Nanomedicine (London, England) Pub Date : 2024-01-01 Epub Date: 2024-08-02 DOI:10.1080/17435889.2024.2379757
Lorena Bonilla-Vidal, Marta Świtalska, Marta Espina, Joanna Wietrzyk, Maria Luisa García, Eliana B Souto, Anna Gliszczyńska, Elena Sánchez-López
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Abstract

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.

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抗肿瘤褪黑激素纳米脂质载体。
目的:癌症是全球第二大死因,传统疗法因副作用大而受到限制。褪黑素(MEL)是一种具有抗肿瘤特性的天然化合物,但存在不稳定和溶解度低的问题。为了克服这些问题,我们将褪黑素封装到含有玫瑰果油的纳米结构脂质载体(MEL-NLC)中,以提高其稳定性并增强其抗肿瘤活性。研究方法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。对其稳定性和生物制药行为进行了评估,同时还进行了相互作用研究和体外抗肿瘤效果研究。结果:优化后的 MEL-NLC 具有理想的理化特性,包括小粒径、持续释放 MEL 以及长期稳定性。体外研究表明,MEL-NLC 可选择性地诱导多种癌细胞株产生细胞毒性,同时保护健康细胞。结论:MEL-NLCMEL-NLC 是一种很有前景的癌症替代疗法,它结合了更强的稳定性和靶向抗肿瘤活性,有可能克服传统疗法的局限性。
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