α-amyrin-loaded nanocapsules produce selective cytotoxic activity in leukemic cells

• Main Authors: Serafim Florentino Neto, Ariadna Lafourcade Prada, Leonardo Domingo Rosales Achod, Heron Fernandes Vieira Torquato, Cauê Santos Lima, Edgar Julian Paredes-Gamero, Maria Oneide Silva de Moraes, Emerson Silva Lima, Edgar Hernandez Sosa, Tatiane Pereira de Souza, Jesus Rafael Rodriguez Amado
• Format: Article
• Language: English
• Published: Elsevier 2021-07-01
• Series: Biomedicine & Pharmacotherapy
• Subjects: Nanotechnology; Cytotoxicity; Caspase; Kollicoat® Mae
• Online Access: http://www.sciencedirect.com/science/article/pii/S0753332221004388

Introduction: Amyrins are triterpenes that have attractive pharmacological potential; however, their low water solubility and erratic stomach absorption hinders their use as a drug. The aim of this paper was to develop a novel α-amyrin-loaded nanocapsule for intestinal delivery and evaluate, preliminarily, its cytotoxic ability against leukemic cells. Material and methods: Five nanocapsule formulations were designed by the solvent displacement-evaporation method. Poly-ε-caprolactone, Eudragit® E100, and Kollicoat® Mae 100 P were used as film-former materials. Particle size, polydispersity index (PdI), zeta potential, and the pH of all formulations were measured. The cytotoxic potential of the nanocapsules was evaluated in vitro using different leukemic lineages Results: Nanocapsules coated with Kollicoat® Mae 100 P presented the smallest particle size (130 nm), the lowest zeta-potential (−38 mV), and the narrowest size distribution (PdI = 0.100). The entrapment efficiency was 65.47%, while the loading capacity was 2.40%. Nanocapsules release 100% of α-amyrin in 40 min (pH 7.4), by using a possible mechanism of swelling-diffusion. The formulation showed excellent on-shelf physicochemical stability during one year. Additionally, nanocapsules produced a selective cytotoxic effect on a human leukemia lineage Kasumi-1, an acute myeloid leukemia cell line, and produced cell death by apoptosis Conclusion: α-amyrin-loaded nanocapsules appear to be a promising nanoformulation that could be used against leukemia.