Diagnostic Research Centre, Department Pharmacological, Faculty of Pharmacy, Al-Ahliyya Amman University, Amman 19328, Jordan.
Cell Therapy Center, The University of Jordan, Amman 11942, Jordan.
Nutrients. 2021 Nov 10;13(11):3995. doi: 10.3390/nu13113995.
Medicinal plants have proven their value as a source of molecules with therapeutic potential, and recent studies have shown that capsaicin has profound anticancer effects in several types of human cancers. However, its clinical use is handicapped due to its poor pharmacokinetics. This study aims to enhance capsaicin's pharmacokinetic properties by loading the molecule into nanoliposomes model and testing its anticancer activity.
Nanoliposomes were prepared using the thin-film method, and characteristics were examined followed by qualitative and quantitative analyses of encapsulation efficiency and drug loading using HPLC at different lipid/capsaicin ratios. Cell viability assay (MTT) was used to determine IC.
Capsaicin-loaded nanoliposomes showed optimum characteristics of morphology, particle size, zeta potential, and stability. In vitro anticancer activity of capsaicin and capsaicin-loaded nanoliposomes were compared against MCF7, MDA-MB-231, K562, PANC1, and A375 cell lines. Capsaicin-loaded nanoliposomes showed significant improvement in anticancer activity against cancers cell lines studied ( < 0.001), with increased selectivity against cancer cells compared to capsaicin.
The encapsulated capsaicin nanoliposomes produced an improvement in pharmacokinetics properties, enhancing the anticancer activity and selectivity compared with capsaicin. This model seems to offer a potential for developing capsaicin formulations for the prevention and treatment of cancer.
药用植物已被证明是具有治疗潜力的分子的来源，最近的研究表明，辣椒素对多种人类癌症具有显著的抗癌作用。然而，由于其较差的药代动力学特性，其临床应用受到限制。本研究旨在通过将分子载入纳米脂质体模型来增强辣椒素的药代动力学特性，并测试其抗癌活性。
采用薄膜法制备纳米脂质体，对不同脂质/辣椒素比例下的包封效率和载药量进行定性和定量分析，考察其特性。采用 MTT 法测定细胞活力（IC）。
载辣椒素的纳米脂质体表现出最佳的形态、粒径、Zeta 电位和稳定性特征。体外抗癌活性比较了游离辣椒素和载辣椒素的纳米脂质体对 MCF7、MDA-MB-231、K562、PANC1 和 A375 细胞系的作用。载辣椒素的纳米脂质体对研究的癌细胞系表现出显著提高的抗癌活性（<0.001），与游离辣椒素相比，对癌细胞的选择性更高。
包封的辣椒素纳米脂质体改善了药代动力学特性，与游离辣椒素相比，提高了抗癌活性和选择性。该模型似乎为开发用于癌症预防和治疗的辣椒素制剂提供了潜力。
