Department of Global Health and Biomedical Sciences, School of Life Science and Bioengineering, Nelson Mandela African Institution of Science and Technology, P.O. Box 447, Arusha 23100, Tanzania.
Centre for Traditional Medicine and Drug Research, Kenya Medical Research Institute, P.O. Box 54840, Nairobi 00200, Kenya.
Molecules. 2022 Jul 11;27(14):4430. doi: 10.3390/molecules27144430.
Moringa oleifera leaf polyphenols (Mopp) were encapsulated with phytosomes to enhance their efficacy on 4T1 cancer cell lines. The Mopp were extracted via microwave-assisted extraction. Moringa oleifera polyphenol-loaded phytosomes (MoP) were prepared with the nanoprecipitation method and characterized using the dynamic light scattering and dialysis membrane techniques. The in vitro cytotoxic and antiproliferative activity were investigated with the (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazole) MTT assay. Acute toxicity was assessed using Swiss albino mice. An MoP particle size of 296 ± 0.29 nm, −40.1 ± 1.19 mV zeta potential, and polydispersity index of 0.106 ± 0.002 were obtained. The total phenolic content was 50.81 ± 0.02 mg GAE/g, while encapsulation efficiency was 90.32 ± 0.11%. The drug release profiles demonstrated biphasic and prolonged subsequent sustained release. In vitro assays indicated MoP had a low cytotoxicity effect of 98.84 ± 0.53 μg/mL, doxorubicin was 68.35 ± 3.508, and Mopp was 212.9 ± 1.30 μg/mL. Moreover, MoP exhibited the highest antiproliferative effect on 4T1 cancer cells with an inhibitory concentration of 7.73 ± 2.87 μg/mL and selectivity index > 3. The results indicated a significant difference (p ≤ 0.001) in MoP when compared to Mopp and doxorubicin. The in vivo investigation showed the safety of MoP at a dose below 2000 mg/kg. The present findings suggest that MoP may serve as an effective and promising formulation for breast cancer drug delivery and therapy.
辣木叶叶多酚（Mopp）被包封在植物固醇中，以提高其对 4T1 癌细胞系的疗效。Mopp 通过微波辅助提取法提取。辣木叶多酚负载的植物固醇（MoP）通过纳米沉淀法制备，并通过动态光散射和透析膜技术进行表征。体外细胞毒性和增殖抑制活性通过（3-[4,5-二甲基噻唑-2-基]-2,5-二苯基四唑）MTT 测定法进行研究。急性毒性使用瑞士白化小鼠进行评估。获得 MoP 粒径为 296 ± 0.29nm、-40.1 ± 1.19mV ζ 电位和 0.106 ± 0.002 的多分散指数。总酚含量为 50.81 ± 0.02mgGAE/g，包封效率为 90.32 ± 0.11%。药物释放曲线呈两相和随后持续延长的缓释。体外试验表明 MoP 的细胞毒性作用低，为 98.84 ± 0.53μg/mL，阿霉素为 68.35 ± 3.508μg/mL，Mopp 为 212.9 ± 1.30μg/mL。此外，MoP 对 4T1 癌细胞表现出最高的增殖抑制作用，抑制浓度为 7.73 ± 2.87μg/mL，选择性指数>3。结果表明，MoP 与 Mopp 和阿霉素相比，差异有统计学意义（p≤0.001）。体内研究表明，MoP 在低于 2000mg/kg 的剂量下是安全的。本研究结果表明，MoP 可能成为一种有效的、有前途的乳腺癌药物传递和治疗制剂。
