Open AccessLinseed Oil Nanoemulsion with Pluronic® F127 Loaded with Betulinic Acid: Preparation, Rheology, MTT Assay and in vitro Release Kinetics
Author(s) -
Louhana Rebouças,
A. Sousa,
Nilce Gramosa,
Tamara de Araújo,
Fátima de Cássia de Oliveira,
Cláudia Pessoa,
Rinaldo dos Santos Araújo,
Emília Santos,
Nágila M.P.S. Ricardo
Publication year - 2022
Publication title -
journal of the brazilian chemical society
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.337
H-Index - 70
eISSN - 1678-4790
pISSN - 0103-5053
DOI - 10.21577/0103-5053.20220063
Subject(s) - betulinic acid , chemistry , zeta potential , mtt assay , in vitro , poloxamer , cytotoxicity , ic50 , dispersity , kinetics , pulmonary surfactant , chromatography , nuclear chemistry , biochemistry , nanoparticle , materials science , organic chemistry , nanotechnology , polymer , genetics , physics , copolymer , quantum mechanics , biology
The main objective of this work was to develop a nanoemulsion based on linseed oil and betulinic acid, stabilized with Pluronic F127 and polyglycerol polyricinoleate, for anticancer applications. The nanoemulsions were synthesized by ultrasound and evaluated for in vitro cytotoxicity, particle size, polydispersity index, zeta potential, morphology, encapsulation efficiency, storage stability, rheology and in vitro release kinetics. In vitro cytotoxicity assays were performed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay (72 h) against HCT-116 (colorectal carcinoma), SNB-19 (glioblastoma), NCI-H460 (lung carcinoma) and L-929 (normal fibroblasts) cells. The determination of 50% inhibitory concentration (IC50) showed an increased selectivity for the emulsified betulinic acid when compared to its free form for the HCT-116 cells. The IC50 values for the synthesized nanoemulsions showed a range from 3.2 to 3.7 μM (HCT-116), 5.6 and 11.5 μM (NCI-H460), 5.8 and 7.3 μM (SNB-19) and > 16.5 μM for normal fibroblasts. In the 48 h in vitro release assays, it presented controlled release explained by the Korsmeyer-Peppas model, releasing 572.25 and 619.95 μg of betulinic acid in a controlled way, generating promising perspectives for the prolonged release of betulinic acid in anticancer applications.