研究动态
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用于皮肤癌治疗的负载多西他赛的纳米结构脂质载体的开发和评估。

Development and Evaluation of Docetaxel-Loaded Nanostructured Lipid Carriers for Skin Cancer Therapy.

发表日期:2024 Jul 19
作者: Florentina-Iuliana Cocoș, Valentina Anuța, Lăcrămioara Popa, Mihaela Violeta Ghica, Mihaela-Alexandra Nica, Mirela Mihăilă, Radu Claudiu Fierăscu, Bogdan Trică, Cristian Andi Nicolae, Cristina-Elena Dinu-Pîrvu
来源: Pharmaceutics

摘要:

本研究的重点是负载多西紫杉醇的纳米结构脂质载体(NLC)的设计、表征和优化,用于治疗皮肤癌。采用以实验设计 (DoE) 原则为指导的系统制剂开发流程,对粒径、多分散指数 (PDI)、zeta 电位和包封效率等关键参数进行优化,以确保 NLC 的稳定性和载药功效。结合 XRD 和冷冻 TEM 分析进行 NLC 纳米结构评估,确认形成了明确的纳米结构。体外动力学研究表明多西紫杉醇可在 48 小时内受控且持续释放,强调了延长治疗效果的潜力。对人脐静脉内皮细胞 (HUVEC) 和 SK-MEL-24 黑色素瘤细胞系的细胞毒性测定表明,对癌细胞的功效增强,具有显着的选择性细胞毒性,对正常细胞的影响最小。这种多维方法,包括配方优化和综合表征,使负载多西紫杉醇的 NLC 成为晚期皮肤癌治疗的有希望的候选者。研究结果强调了这些纳米载体的潜在转化影响,为未来皮肤癌治疗的临床前研究和临床应用铺平了道路。
This study focuses on the design, characterization, and optimization of nanostructured lipid carriers (NLCs) loaded with docetaxel for the treatment of skin cancer. Employing a systematic formulation development process guided by Design of Experiments (DoE) principles, key parameters such as particle size, polydispersity index (PDI), zeta potential, and entrapment efficiency were optimized to ensure the stability and drug-loading efficacy of the NLCs. Combined XRD and cryo-TEM analysis were employed for NLC nanostructure evaluation, confirming the formation of well-defined nanostructures. In vitro kinetics studies demonstrated controlled and sustained docetaxel release over 48 h, emphasizing the potential for prolonged therapeutic effects. Cytotoxicity assays on human umbilical vein endothelial cells (HUVEC) and SK-MEL-24 melanoma cell line revealed enhanced efficacy against cancer cells, with significant selective cytotoxicity and minimal impact on normal cells. This multidimensional approach, encompassing formulation optimization and comprehensive characterization, positions the docetaxel-loaded NLCs as promising candidates for advanced skin cancer therapy. The findings underscore the potential translational impact of these nanocarriers, paving the way for future preclinical investigations and clinical applications in skin cancer treatment.