Phytochemical Studies on Linum Usitatissimum Seeds and the Nanoformulation of the Bioactive Butanol Extract

Abstract

The phytochemical investigation of Linum usitatissimum, family Linaceae, resulted in the separation and identification of a lignane, 8–5' neolignan 1 (dehydrodiconiferyl alcohol-4-β-D-glucoside), in addition to identification of many compounds by the GC/MS technique. The antimicrobial activities of hexane, methylene chloride and butanol fractions were comparable to ampicillin. The activities against E. coli were 29.2%, 37.5%, and 66.7%, respectively; against S. aureus were 45.4%, 36.4% and 63.6%, respectively, and against C. albicans were 26.9%, 46.1% and 73.1%, respectively. Antioxidant activity was assessed by ABTS method. It decreased in the following order: ascorbic acid > butanol fraction > methylene chloride fraction > hexane fraction. The cytotoxicity against HePG2 was found to be “moderate” for butanol and methylene chloride fractions, and “weak” for the hexane fraction. The cytotoxicity against MCF-7 was found to be “strong” for butanol fraction, and “weak” for both hexane and methylene chloride fractions. The lignane-rich subfraction, Lu 3d was incorporated into pluronic nano-micelles using nanoprecipitation technique through a modified procedure. The physicochemical characteristics of the developed Lu 3d-loaded nano-micelles such as particle size, potential and morphology were determined using DLS and HR-TEM. The average diameters of the prepared plain and Lu 3d-loaded pluronic nano-micelles were found to be 207 ± 12 and 225 ± 18 nm, respectively. The encapsulation of Lu 3d into nano-sized particles has enhanced their aqueous dissolution and consequently improved their bioavailability. Nanoformulation of Lu 3d led also to a stable colloidal dispersion with a strong green color, indicating its homogenous distribution in the aqueous medium at a significantly higher concentration than that obtained using other solvents.