Development and characterization of lipid based solid dispersion of quassinoid enriched fraction of Simarouba glauca for enhanced lipid membrane permeability in MCF7 breast cancer cells

Simarouba glauca leaves are rich in quassinoids, known for anticancer properties. This study aimed to develop a lipid-based solid dispersion of the quassinoid-enriched fraction (LBSD-QEF) to enhance permeability in MCF7 breast cancer cells. LBSD-QEF of SG was prepared by hot homogenization using soy lecithin and Pluronic F68 (1:2) with varying concentrations of SGQEF. Out of the six developed formulations, the F5 (LBSD-QEF of SG) was chosen as the best one based on the zeta potential (-33.2 mV), polydispersity index (0.413), and an average mean particle size (275 nm). It comprises 50 mg of SG quassinoid enriched fraction in addition to 1:2 ratio of lipid (12.5 mg) and surfactant (25 mg). F5 remained stable for 3 months at 4 ± 2.0°C/50 % ± 5 % RH. In vitro drug release F5 (LBSD-QEF of SG) showed 76 % quassinoid release in the first hour and 80 % in the second through dialysis membrane. Cellular uptake of F5 in Caco-2 cells demonstrated strong FITC signal expression. Cytotoxicity studies showed F5 had an IC₅₀ of 12.45 µg/ml against MCF7 cells, outperforming SGQEF (IC₅₀ = 35.05 µg/ml) and crude methanol extract (IC₅₀ = 49.19 µg/ml). The developed F5 (LBSD-QEF of Simarouba glauca ) enhances membrane permeability and exhibits greater cytotoxicity in ER+ breast cancer cells.