Abstract
BackgroundO. stamineus is a medicinal herb with remarkable pharmacological properties. However, poor solubility of the active principles limits its medicinal value. This study sought to prepare nano liposomes of OS ethanolic extract in unpurified soybean phospholipids in order to improve its solubility and permeability. OS liposomes were prepared by the conventional film method, and were characterized for solubility, entrapment efficiency, Fourier transform infrared spectroscopy (FTIR), transmission electron microscopy (TEM), particle size and zeta potential, release, absorption in everted rat intestinal sacs, and DPPH scavenging effect.ResultsOS liposomes showed substantial enhancement of extract’s solubility from 956 ± 34 to 3979 ± 139 μg/ml, with entrapment efficiency of 66.2 ± 0.9%. FTIR study indicates interaction between soybean phospholipids and OS extract. TEM and dynamic light scattering showed presence of round anionic nano liposomes with particle size and zeta potential of 152.5 ± 1.1 nm and −49.8 ± 1.0 mV, respectively. A study using the fluorescent probe pyrene showed the critical micellar concentration is 9.2 ± 2.9 μg/ml. Release studies showed 94 ± 0.1% release in non-formulated extract and 62.4 ± 0.1% in OS liposomes. Released extract from OS liposomes showed improvement in DPPH scavenging effect, IC50 = 23.5 ± 1.1 μg/ml compared to 32.4 ± 0.5 μg/ml in non-formulated extract. OS liposomes were stable at pH 5.5 and 7.4, but showed reversible agglomeration at pH 1.6. Absorption in everted rat intestinal sacs showed substantial improvement in permeability of 3′-hydroxy-5, 6, 7, 4″-tetramethoxyflavone, sinensetin, eupatorin, and 3 other unknown compounds.ConclusionsEnhanced solubility, absorption and antioxidant effect may improve the overall pharmacological effects and medicinal value of OS ethanolic extract.
Highlights
O. stamineus is a medicinal herb with remarkable pharmacological properties
The percentage of PC in crude soybean phospholipids, soybean phospholipid extract prepared in ethanol (PH-Et), soybean phospholipid extract prepared in acetone (PH-Ac), and phospholipid fraction prepared by column chromatography (PH-Fr) was 13.4%, 21.6%, 10.6% and 42%, respectively
The formulations were prepared by mixing ethanolic solution of the extract with chloroform solution of phospholipids followed by evaporation of solvents and hydration of the resulting film
Summary
O. stamineus is a medicinal herb with remarkable pharmacological properties. OS liposomes were prepared by the conventional film method, and were characterized for solubility, entrapment efficiency, Fourier transform infrared spectroscopy (FTIR), transmission electron microscopy (TEM), particle size and zeta potential, release, absorption in everted rat intestinal sacs, and DPPH scavenging effect. Research on OS has increased recently due to its various pharmacological properties such as diuretic and hypouricemic [2], hepatoprotective [3], phospholipids obtained from food grade soybean lecithin, in order to improve the extract’s solubility and permeability as major factors for improving oral bioavailability. The liposomes were prepared by the film method and were evaluated for solubility, entrapment efficiency, stability under various pH conditions, critical micellar concentration, particle size and zeta potential, FTIR spectroscopy, TEM, drug release, absorption through everted rat’s small intestinal sacs, and free radical scavenging effect. Improving solubility of the lipophilic flavones may improve the bioavailability and the overall pharmacological activity of OS extracts
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