Shaker Dalia S, Shaker Mohamed A, Hanafy Mahmoud S
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Helwan University, Cairo, Egypt; Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences and Pharmaceutical Industries, FUE, Cairo, Egypt.
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Helwan University, Cairo, Egypt.
Int J Pharm. 2015 Sep 30;493(1-2):285-94. doi: 10.1016/j.ijpharm.2015.07.041. Epub 2015 Jul 19.
One of the main challenges in Tamoxifen cancer therapy is achieving localized, efficient and sustained delivery without harming normal healthy organs. This study focused on evaluating Tamoxifen Citrate (TMC) niosomes for localized cancer therapy through in-vitro breast cancer cytotoxicity as well as in-vivo solid anti-tumor efficacy. Different niosomal formulae were prepared by film hydration technique and characterized for entrapment efficiency% (E. E), vesicle size, morphology, and in-vitro release. The cellular uptake and anti-cancer activity were also tested in-vitro using MCF-7 breast cancer cell line. Moreover, in-vivo anti-tumor efficacy was examined in Ehrlich carcinoma mice model through reporting solid tumor volume regression and tissue TMC distribution. The obtained niosomes prepared with Span 60: cholesterol (1: 1 molar ratio) showed a distinct nano-spherical shape with EE up to 92.3%± 2.3. Remarkably prolonged release of TMC following diffusion release behavior was detected. The optimized formula showed significantly enhanced cellular uptake (2.8 fold) and exhibited significantly greater cytotoxic activity with MCF-7 breast cancer cell line. In-vivo experiment showed enhanced tumor volume reduction of niosomal TMC when compared to free TMC. Based on these results, the prepared niosomes demonstrated to be promising as a nano-size delivery vehicle for localized and sustained TMC cancer therapy.
他莫昔芬癌症治疗的主要挑战之一是在不损害正常健康器官的情况下实现局部、高效和持续的给药。本研究聚焦于通过体外乳腺癌细胞毒性以及体内实体抗肿瘤疗效来评估柠檬酸他莫昔芬（TMC）脂质体用于局部癌症治疗的效果。采用薄膜水化技术制备了不同的脂质体配方，并对其包封率%（E.E）、囊泡大小、形态和体外释放进行了表征。还使用MCF-7乳腺癌细胞系在体外测试了细胞摄取和抗癌活性。此外，通过报告实体瘤体积消退和组织中TMC分布，在艾氏癌小鼠模型中检测了体内抗肿瘤疗效。用司盘60：胆固醇（摩尔比1：1）制备的脂质体呈现出明显的纳米球形，包封率高达92.3%±2.3。检测到TMC在扩散释放行为后有显著延长的释放。优化后的配方显示细胞摄取显著增强（2.8倍），并且对MCF-7乳腺癌细胞系表现出显著更高的细胞毒性活性。体内实验表明，与游离TMC相比，脂质体TMC的肿瘤体积缩小更为明显。基于这些结果，所制备的脂质体被证明有望作为一种纳米尺寸的给药载体用于局部和持续的TMC癌症治疗。
