Isoflavone content and antioxidant activity of Thai fermented soybean and its capsule formulation

Soybeans (Glycine max) are usually eaten as processed foods. Fermented soybeans are among the most popular of these processed foods. The aim of this study was to determine the effect of fermentation duration on isoflavone content and antioxidant activity of fermented soybeans. Capsule formulation of fermented soybeans was also studied. The Thai soybean variety, Rajamangala60, was fermented with Aspergillus oryzae. Isoflavone content and antioxidant activity were studied at 0, 12, 18,36, 48, 96, 120, 168, 240, 360 and 480 h of fermentation duration. The results showed that isoflavone glycones (daidzin and genistin) decreased during fermentation, but aglycones (daidzein and genistein) increased. The highest amount of isoflavone aglycones was 384.30 ± 4.60 and 116.50 ± 1.56 mg/100 g fermented soybeans for daidzein and genistein, respectively. Antioxidant activity of fermented soybeans was evaluated by ABTS cation radical scavenging and ferric reducing antioxidant power(FRAP) methods. Antioxidant activity of fermented soybeans is increased during fermentation. Increases in isoflavone aglycones content and antioxidant activity were related to fermentation duration. The highest antioxidant activity of fermented soybean was found at the 240 h of fermentation with trolox equivalent antioxidant capacity (TEAC) 1.98 ± 0.09 ìg trolox/g fermented soybean and FRAP value of 0.623 ± 0.002 g FeSO4/g fermented soybean. Soybeans fermented for 240 h were thenformulated as capsules by a wet granulation method. They were then assessed for appearance, weight variation, disintegration time and antioxidative properties. The results showed that fermented soybeancapsules conformed to USP32/NF27 criteria on weight variation and disintegration. Their antioxidant activity was lower than 240 h fermented soybeans, but still higher than the non-fermented ones (p <0.05)

Improvement of Biophysical Skin Parameters of Topically Applied Fermented Soybean Extract-Loaded Niosomes with No Systemic Toxicity in Ovariectomized Rats

Despite the known beneficial impacts of estrogen used as hormone replacement therapy to ameliorate signs of skin aging in postmenopausal women, its compliance rates are low. A significant amount of estrogen may be absorbed into the blood circulation and can lead to systemic actions. Soy isoflavone exhibits biological activities similar to synthetic estrogen because it is a heterocyclic phenolic compound. The disadvantage of most topical ingredients based on isoflavone is that they contain biologically inactive glycoside forms, which must be converted to a readily absorbed aglycone for the topical application. The purposes of this study were to develop niosomes-loaded Aspergillus oryzae-fermented soybean extract (FSE) to enhance skin absorption with proven systemic side effect compared to estrogen application. Skin hydration and viscoelasticity of 75 days post-ovariectomized (OVX) Wistar rats following 84-day topical treatment with various tested gel formulations containing fermented soybean extract (FSE) were evaluated. The tested formulations were gel + FSE nanoniosomes, gel + FSE microniosomes, gel + FSE (200 µg FSE/9 cm2/rat), gel + blank nanoniosomes (a negative control), and gel + 17β-estradiol (E2) nanoniosomes (a positive control, 20 µg E2/9 cm2/rat). Changes in vaginal cornifications and weights of uteri, livers, and kidneys in the OVX rats and signs of primary skin irritation in the rabbits were evaluated for their toxicities. Results showed that FSE-loaded nanoniosomes improved the skin hydration and viscoelasticity better than gel + FSE microniosomes and gel + FSE, respectively, but lower than those of gel + E2 nanoniosomes (p < 0.05). Unlike all gel + E2 nanoniosomes, the FSE formulations showed no changes in vaginal cells and weights of uteri, livers, and kidneys and no signs of skin irritation. In conclusion, The FSE niosome-based gels should be promising candidates for delivering phytoestrogens against signs of skin aging with no systemic toxicities

Optimization and Transfollicular Delivery of Finasteride-Loaded Proniosomes for Hair Growth Stimulation in C57BL/6Mlac Mice

The study aimed to develop the finasteride-loaded proniosome (FLP) to enhance the transfollicular delivery of finasteride (FN). The response surface methodology (RSM) combined with central composite design (CCD) with three independent variables (FN concentrations, total lipid content, and cholesterol content) was used to optimize the FLP preparation. The particles size, zeta potential, entrapment efficiency, and drug loading capacity of the FLP were analyzed. The transfollicular delivery of the optimum formulation was investigated in vitro. In vivo hair growth stimulation study was performed on C57BL/6Mlac mice dorsal areas. The Draize primary skin irritation test for erythema and edema was performed in the New Zealand white rabbit skin. The optimum FLP consists of 5.0 mM of FN, 10.1 mM of total lipid content, and 50.0% of the cholesterol in the total lipid. The prepared proniosome delivered the FN significantly (p < 0.05), compared to the naked finasteride solution in a dose- and time-dependent manner. The FLP treatment significantly increases the number and size of hair follicles in a dose-dependent manner. The efficiency of 1% FLP was comparable to the 2% minoxidil solution. The FLP exhibited no skin irritation after 72 h. Therefore, the results demonstrated that the FLP could stimulate hair growth via a transfollicular delivery system

Enhanced Transdermal Delivery of Concentrated Capsaicin from Chili Extract-Loaded Lipid Nanoparticles with Reduced Skin Irritation

The aim of this study was to develop lipid-based nanoparticles that entrapped a high concentration of capsaicin (0.25%) from a capsicum oleoresin extract. The solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) were strategically fabricated to entrap capsaicin without a hazardous solvent. Optimized nanosize lipid particles with high capsaicin entrapment and loading capacity were achieved from pair-wise comparison of the solid lipid mixtures consisting of fatty esters and fatty alcohols, representing small and large crystal-structure molecules combined with a compatible liquid lipid and surfactants (crystallinity index = 3%). This report was focused on selectively captured capsaicin from oleoresin in amorphous chili extract-loaded NLCs with 85.27% ± 0.12% entrapment efficiency (EE) and 8.53% ± 0.01% loading capacity (LC). The particle size, polydispersity index, and zeta potential of chili extract-loaded NLCs were 148.50 ± 2.94 nm, 0.12 ± 0.03, and −29.58 ± 1.37 mV, respectively. The favorable zero-order kinetics that prolonged capsaicin release and the significantly faster transdermal penetration of the NLC attributed to the reduction in skin irritation of the concentrated capsaicin NLCs, as illustrated by the in vitro EpiDermTM three-dimensional human skin irritation test and hen’s egg test chorioallantoic membrane assay (HET-CAM)

Antioxidant and 5α-Reductase Inhibitory Activity of <i>Momordica charantia</i> Extract, and Development and Characterization of Microemulsion

Momordica charantia (M. charantia) is rich in flavonoids, which possess a strong antioxidant capacity and may help prevent hair loss. This study aims to develop the microemulsion of M. charantia with antioxidant activity and 5α-reductase (5aR) inhibitory activity. The total phenolic content (TPC), antioxidant activity, and 5aR inhibitory activity of ethanolic and aqueous extracts of the fruit were investigated. The preparation of M. charantia extract-loaded microemulsion (MELM) was optimized and characterized the MELM. The aqueous extract of M. charantia fruit flesh displayed a TPC of 780.75 ± 24.82 mg Gallic acid equivalence/g of extract. ABTS (2,2′-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid), DPPH (2,2-diphenyl-1-picrylhydrazyl), and nitric oxide (NO) radical scavenging activities were observed in all the extracts. About 0.461 ± 0.003 mg finasteride equivalence/g of extract of 5aR inhibitory activity was detected in the aqueous extract of the inner tissue of M. charantia fruit. Based on NO radical scavenging and 5aR inhibitory activity, an aqueous extract of the inner tissue (pericarp with seed) of M. charantia fruit was used to prepare the MELM. The MELM was prepared using a different ratio of tween 80 and ethanol as Smix. The results showed that the 1:1 ratio of tween 80: ethanol produced microemulsion of an optimum size, zeta potential, and polydispersity index. The MELM samples were stored at 5, 30, and 40 °C for 12 weeks, and the stability was assessed. The results revealed that the size, zeta potential, and polydispersity index of the formulated MELM remained unchanged during the investigated time. This study primarily reports the 5aR inhibitory activity of M. charantia extract and the development of microemulsion. The prepared MELM could be further developed into cosmetic or pharmacological preparations to manage hair loss

Effects of Litsea cubeba (Lour.) Persoon Essential Oil Aromatherapy on Mood States and Salivary Cortisol Levels in Healthy Volunteers

Aromatherapy is one of the complementary therapies to improve health. The aromatic essential oils have been used in the treatment procedure through inhalation of essential oil vapor, massage, and herbal bathing. Litsea species are generally used in traditional medicine, and Litsea cubeba (Lour.) Persoon is a potent fumigant plant, used in cosmetics and foods as essence. The chemical composition of the essential oil of different parts of L. cubeba has been found to be varied. L. cubeba essential oil (LEO) is known for the treatment of cognition-associated discomforts. The current study assessed the impact of inhalation of LEO on mood states and salivary cortisol levels of healthy people. Fifteen healthy volunteers were involved in the study. The Profile of Mood States (POMS) Questionnaire and ELISA methods were employed to determine the mood states and salivary cortisol level, respectively. (-)-β-pinene, β-citral, cis- and trans-citral, citronellal, limonene, linalool, and 6-methyl-5-hepten-2-one were detected in LEO by GC-MS analysis. The heart rate and blood pressure were not affected significantly during LEO exposure. The inhalation of LEO significantly improved the total mood disturbance and reduced the confusion among the healthy human subjects. LEO inhalation reduced the salivary cortisol level at a notable level. The results of the current study warrant further studies on the beneficial effect of LEO aromatherapy in healthy and diseased subjects to uncover the therapeutic nature of the L. cubeba plant

Development and Evaluation of Elaeagnus rhamnoides (L.) A. Nelson Oil-Loaded Nanostructured Lipid Carrier for Improved Skin Hydration

Sea buckthorn (SB) (Elaeagnus rhamnoides (L.) A. Nelson) is rich in flavonoids, phenolic compounds, anthocyanins, carotenoids, and phytosterol. Its phytochemicals exhibit various biological activities, such as antioxidant, immunomodulatory and anti-carcinogenic activities. SB also helps prevent the development of wrinkles and protects the skin&rsquo;s surface from UV rays. The purpose of the present study was to develop and characterize an SB oil (SBO)-loaded nanostructured lipid carrier (NLC) for improved skin hydration. The response surface methodology (RSM) and central composite design (CCD) were employed to optimize the influencing factors (wax percentage, surfactant percentage, and PEG400 percentage in the surfactant) to achieve the desirable qualities in SBO-NLCs. The optimum (minimum) size of SBO-NLCs (105.26 nm) was obtained with a combination of 2.5% wax, 7.5% surfactant, and 30% PEG400 in the surfactant. A narrow polydispersity index (PDI; 0.16), relatively low zeta potential (ZP; &minus;15.63 mV), and high entrapment efficiency (EE; 90.88%) were observed in this study. Reduced quadratic and reduced 2FI models were adapted to predict conditions to attain the optimum size and PDI of SBO-NLCs, respectively. ZP and EE were predicted with the help of a reduced cubic model. All of the predicted models were statistically significant. Differential scanning calorimetry results suggested that the SBO-NLCs had less crystallinity and therefore reduced the rate of drug expulsion from the inner core of the NLCs. A noticeable level of occlusion effect was observed in the SBO-NLCs. The SBO-NLCs showed a faster vitamin E (biomarker for the drug) release rate into the skin within 24 h, and the released vitamin E level after 48 h was significantly higher than that for the free SBO. Additionally, SBO-NLCs delivered vitamin E into the inner skin significantly (22.73 &plusmn; 1.67 &micro;g/cm2 of skin). In conclusion, the SBO-NLC is a potential delivery system that can be used to prevent skin water loss and improve skin hydration. Further investigations, such as drug stability and safety evaluations, are required prior to commercialization for human use