Phyto-emulsomes as a novel nano-carrier for morine hydrate to combat leukemia: In vitro and pharmacokinetic study

Abstract

This study tackles the development of morin hydrate-loaded Phyto-Emulsomes (MH-EMs) using β-sitosterol as a ‘heart-friendly’ alternative to cholesterol for curing leukemia. β-sitosterol was isolated from the aerial parts of C. pallescens Delile (Compositae). Phyto-Emulsomes were prepared using different ratios of glyceryl monostearate (GMS), phospholipon 80H (P80H) and ß-sitosterol (SS), then, their size, entrapment efficiency, and drug release were evaluated. Among the prepared formulae, MH-EM5 composed of GMS: P80H: SS (2:0.5:0.5) had the highest drug release efficiency (RE = 82.28 ± 1.96%) and the smallest particle size (271.7 ± 4.86 nm) with a uniform distribution. MH-EM5 was subjected to characterization including the micro-morphological examination using TEM, thermal analysis, in addition to biological evaluation. The biostability of MH-EM5 in serum and bile salts was proved. The potential cytotoxicity of the free drug, MH-EM5 and its corresponding unmedicated formulation against normal oral epithelial cell and acute monocytic leukemia was studied. The results showed a negligible cytotoxicity in normal cells for all tested samples, while, cancer cells had a significant decrease in the cell viability in case of the selected formula (MH-EM5) compared to the corresponding unmedicated one as well as the free drug, at different concentrations up to 300 μg/ml. Also, the oral bioavailability study proved the significant increase of all measured pharmacokinetic parameters, after a single oral administration of MH-EM5 compared to the free drug suspension. Regarding these findings, phyto-emulsomes can be considered as a safe and promising nanometric delivery system for the oral administration of morin hydrate due to the enhancement of its solubility, oral bioavailability and antitumor efficacy.