Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, India.
Department of Biological Sciences, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, India.
Eur J Pharm Biopharm. 2022 Nov;180:119-136. doi: 10.1016/j.ejpb.2022.09.024. Epub 2022 Oct 2.
Melanoma is the most malignant form of skin cancer across the globe. Conventional therapies are currently ineffective which could be attributed to the rampant chemo-resistance, metastasis, inability to cross the skin barriers and accumulate within the tumor microenvironment. This advent brings in the principles of drug repurposing by repositioning Niclosamide (NIC), an anthelmintic drug for skin cancer. Incorporation into the liposomes facilitated enhanced melanoma cell uptake and apoptosis. Cytotoxicity studies revealed 1.756-fold enhancement in SK-MEL-28 cytotoxicity by NIC-loaded liposomes compared to free drug. Qualitative and quantitative cell internalization indicated greater drug uptake within the melanoma cells illustrating the efficacy of liposomes as efficient carrier systems. Nuclear staining showed blebbing and membrane shrinkage. Elevated ROS levels and apoptosis shown by DCFDA and acridine orange-ethidium bromide staining revealed greater melanoma cell death by liposomes compared to free drug. Incorporating NIC liposomes into the thermogel system restricted the liposomes as a depot onto the upper skin layers. Sustained zero order release up to 48 h with liposomes and 23.58-fold increase in viscosity led to the sol-to-gel transition at 33℃ was observed with liposomal thermogel. Ex vivo gel permeation studies revealed that C-6 loaded liposomes incorporated within the thermogel successfully formed a depot over the upper skin layer for 6 h to prevent transdermal delivery and systemic adverse effects. Thus, it could be concluded that NIC loaded liposomal thermogel system could be an efficacious therapeutic alternative for the management of melanoma.
黑色素瘤是全球最恶性的皮肤癌形式。目前的常规疗法无效,这可能归因于猖獗的化疗耐药性、转移、无法穿透皮肤屏障并在肿瘤微环境中积累。这一进展带来了药物再利用的原则,即将驱虫药尼氯苯(NIC)重新定位用于皮肤癌。将其纳入脂质体中促进了黑色素瘤细胞的摄取和凋亡。细胞毒性研究表明,与游离药物相比,载有 NIC 的脂质体使 SK-MEL-28 的细胞毒性增强了 1.756 倍。定性和定量的细胞内化表明,黑色素瘤细胞内的药物摄取更多,说明了脂质体作为有效载体系统的功效。核染色显示出起泡和膜收缩。DCFDA 和吖啶橙-溴化乙锭染色显示 ROS 水平升高和细胞凋亡,表明脂质体比游离药物更能引起黑色素瘤细胞死亡。将 NIC 脂质体纳入温敏凝胶系统将脂质体限制在上层皮肤的储存库中。脂质体可持续释放 48 小时,达到零级释放,粘度增加 23.58 倍,在 33℃时观察到脂质体温敏凝胶发生溶胶-凝胶转变。体外凝胶渗透研究表明,载有 C-6 的脂质体成功地在温敏凝胶中形成了一个在上层皮肤的储存库,以防止透皮递送和全身不良反应,持续 6 小时。因此,可以得出结论,载有 NIC 的脂质体温敏凝胶系统可能是治疗黑色素瘤的有效治疗替代方法。