Antioxidant activity of Sophora exigua and liposome development of its powerful extract.

Sophora exigua (SE) was sequentially extracted using hexane, ethyl acetate, and ethanol. The obtained extracts were tested for antioxidant activity. Among them, the fractionated ethyl acetate extract (SE-EA) showed the highest potential in free radical scavenging and ferric-reducing properties. The chemical analysis identified sophoraflavanone G as one of the active ingredients in SE-EA. According to SE-EA solubility, SE-EA liposomes were developed using a sonication-assisted thin film method. Cholesterol and phospholipids were used as the main compositions of the liposomes. The obtained liposomes were spherical with different nano-size ranges, size distribution, and zeta potential depending on SE-EA and total lipid concentrations. SE-EA liposomes were slightly bigger than their empty liposomes. All liposomes exhibited a phospholipid crystalline structure. Cholesterol and SE-EA existed in the liposomes as an amorphous state. SE-EA liposomes with high total lipid content exhibited high entrapment efficiency and sustained release behavior. Whereas liposomes with low total lipid content showed low entrapment efficiency and fast-release behavior. All SE-EA liposomes showed stronger antioxidant activity than the non-entrapped SE-EA. In conclusion, SE-EA is a natural source of potent antioxidants. The developed SE-EA liposomes are a promising pharmaceutical formulation to efficiently deliver the active ingredients of SE-EA and are suitable for further study in vivo.

Development of Tea Seed Oil Nanostructured Lipid Carriers and In Vitro Studies on Their Applications in Inducing Human Hair Growth.

Synthetic drugs used to treat hair loss cause many side-effects. Natural tea seed oil possesses many activities that can suppress hair loss. However, it is oily and sticky in direct application. In this study, tea seed oil loaded nanostructured lipid carriers (NLC) using Tween 80 (NLC-T), Varisoft 442 (NLC-V), and a combination of both surfactants (NLC-C) was developed. The obtained nanoformulations showed spherical particles in the size range 130-430 nm. Particle size and size distribution of NLC-C and NLC-T after storage at 4, 25, and 40 °C for 90 days were unchanged, indicating their excellent stability. The pH of NLC-T, NLC-V, and NLC-C throughout 90 days remained at 3, 4, and 3.7, respectively. NLC-C showed significantly greater nontoxicity and growth-stimulating effect on human follicle dermal papilla (HFDP) cells than the intact oil. NLC-T and NLC-V could not stimulate cell growth and showed high cytotoxicity. NLC-C showed melting point at 52 ± 0.02 °C and its entrapment efficiency was 96.26 ± 2.26%. The prepared hair serum containing NLC-C showed better spreading throughout the formulation than that containing the intact oil. Using 5% NLC-C showed a 78.8% reduction in firmness of the hair serum while enhancing diffusion efficiency by reducing shear forces up to 81.4%. In conclusion, the developed NLC-C of tea seed oil is an effective alternative in stimulating hair growth. Hair serum containing NLC-C obviously reduces sticky, oily, and greasy feeling after use.

Physicochemical characterization of lycopene-loaded nanostructured lipid carrier formulations for topical administration.

Nanostructured lipid carriers (NLC) are interesting delivery systems for enhancing the penetration of an active substance through the skin after topical administration. In the present study, lycopene was loaded into NLC, composed of Eumulgin(®) SG, orange wax and rice bran oil, using high pressure homogenization (HPH). Photon correlation spectroscopy analysis showed that the lycopene-loaded NLC had a size of 150-160nm with a relatively small size distribution (PdI<0.15). The entrapment efficiency of lycopene was found to be 100±0% for all formulations. An in vitro release study of lycopene showed a biphasic release profile: a relatively fast release during the first 6h followed by a sustained release during the next 18h. An in vitro occlusion test showed that the occlusive properties of NLC increased with increasing lycopene loading. A free radical scavenging activity test of the NLC loaded with 50mg% lycopene showed a Trolox equivalent antioxidant capacity value of 36.6±0.4µM Trolox/mg NLC which is higher than that of the NLC base (26.6±0.1µM Trolox/mg NLC). The concentration of 50% antioxidant activity (IC50) of the lycopene-loaded NLC was 14.1±0.6mg/mL, and lower than that of the formulation without lycopene (17.7±0.4mg/mL). The particle size, size distribution, and zeta potential of lycopene-loaded NLC stored at different temperatures of 4, 30, 40°C for 120 days did not change in time, demonstrating an excellent colloidal stability of the systems. Chemical stability data indicated that the utilization of NLC increased the stability of lycopene and it was found that the degradation of lycopene was retarded when stored at low temperatures. In conclusion, NLC are attractive systems for the cutaneous delivery of lycopene.

Potential technique for tiny crystalline detection in lycopene-loaded SLN and NLC development.

CONTEXT: The advantage of solid nanocarriers like solid lipid nanoparticles (SLN) or nanostructured lipid carriers (NLC) is related to some degree of crystalline characteristics of the lipid. However, the detection of tiny content of crystalline structure in such nanoparticles is difficult. OBJECTIVE: The aim of this study was to explore a potential method for detection of low degree of crystalline characteristics of lycopene-loaded SLN and NLC. METHODS: Crystalline characteristics investigation was done by polarized light microscope (PLM), differential scanning calorimeter (DSC), X-ray diffractometer (XRD) and transmission electron microscope (TEM). RESULTS AND DISCUSSION: It was found that high crystalline characteristics as anisotropic molecular organization crystal of pure orange wax and lycopene could be investigated by PLM, DSC and WAXS. Low crystallinity of lycopene-loaded SLN and NLC could not be detected by those techniques. Electron diffraction mode of TEM showed potential detection of tiny crystalline characteristics of such systems. The diffraction pattern of lycopene-loaded SLN and NLC exhibited obvious zero order laue zone indicating an isotropic fine grained polycrystalline of the nanoparticles. CONCLUSION: It could be concluded that TEM is a promising method for detection of low-level crystallinity of solid nanocarriers.

Effect of surfactant on lycopene-loaded nanostructured lipid carriers.

Nanostructured lipid carriers (NLC) have gained high interest as enhancing drug delivery systems via topical application during the last few years. NLC can enhance stability of many active substances against environmental stress. The extremely small size of NLC plays an important role in skin penetration. The unchanged size of NLC upon storage indicates its physical stability. The aim of this work was to investigate the effect of surfactant type on physical properties and stability of lycopene-loaded NLC. The preparation of the NLC was achieved by means of high pressure homogenization. The results indicate that different types of surfactant yield NLC with different properties. We also explored the effect of contact angle on the size of the NLC. It was found that the small contact angle gave NLC with small size. Among two small contact angle surfactants, Plantacare 1200 gave lycopene-loaded NLC with smaller size, higher zeta potential and narrower size distribution. The particle size, size distribution, and zeta potential of lycopene-loaded NLC prepared with Plantacare 1200 was unchanged during 30 days of storage. It was concluded that Plantacare 1200 is the most suitable surfactant for lycopene-loaded NLC. The chemical stability of lycopene entrapped in the NLC was significantly enhanced.