Department of Pathology, Faculty of Medicine, Dalhousie University, Halifax, NS, Canada.
Department of Pathology, Faculty of Medicine, Dalhousie University, Halifax, NS, Canada
Anticancer Res. 2020 Feb;40(2):689-694. doi: 10.21873/anticanres.13998.
BACKGROUND/AIM: Piperine, a major alkaloid of the fruit of black pepper plants, selectively inhibits the growth of triple-negative breast cancer cells but its lipophilicity restricts possible clinical application. This study therefore determined the feasibility of encapsulating piperine in nanoparticles (NPs) to increase its solubility in an aqueous environment.
Piperine-loaded biodegradable methoxy poly(ethylene glycol)-poly(lactic-co-glycolic) acid copolymer-based NPs were produced by single emulsion solvent extraction and thin-film hydration. Growth and viability of triple-negative breast cancer (TNBC) cells were determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and Annexin-V-FLUOS/propidium iodide staining, respectively.
Thin-film hydration was superior to single emulsion solvent extraction, yielding piperine-loaded NPs with an average size of 50 nm. Piperine-loaded NPs inhibited TNBC cell growth and induced apoptosis while sparing normal fibroblasts.
It is feasible to deliver a cytotoxic concentration of piperine to TNBC cells via NPs with the potential for improved bioavailability and solubility in biological fluids.
背景/目的：胡椒碱是黑胡椒植物果实中的主要生物碱，它选择性地抑制三阴性乳腺癌细胞的生长，但由于其亲脂性，限制了其可能的临床应用。因此，本研究旨在确定将胡椒碱包封在纳米颗粒（NPs）中以增加其在水相环境中溶解度的可行性。
采用单乳液溶剂萃取法和薄膜水化法制备载胡椒碱的可生物降解甲氧基聚乙二醇-聚（乳酸-共-乙醇酸）共聚物纳米颗粒。三阴性乳腺癌（TNBC）细胞的生长和活力分别通过 3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐（MTT）法和 Annexin-V-FLUOS/碘化丙啶染色法来测定。
薄膜水化法优于单乳液溶剂萃取法，可得到平均粒径为 50nm 的载胡椒碱纳米颗粒。胡椒碱纳米颗粒抑制 TNBC 细胞生长并诱导细胞凋亡，同时对正常成纤维细胞无影响。
通过 NPs 传递细胞毒性浓度的胡椒碱是可行的，这可能提高生物利用度和在生物流体中的溶解度。
