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

2021; Elsevier BV; Volume: 139; Linguagem: Inglês

10.1016/j.biopha.2021.111656

1950-6007

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, Émerson Silva Lima, Edgar Hernández Sosa, Tatiane Pereira de Souza, Jesús Rafael Rodríguez Amado,

Natural Compounds in Disease Treatment

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. 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 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 α-amyrin-loaded nanocapsules appear to be a promising nanoformulation that could be used against leukemia.