Microemulsions and Nanoemulsions for Topical Delivery of Tripeptide-3: From Design of Experiment to Anti-Sebum Efficacy on Facial Skin.

The targeted delivery of a hydrophilic Tripeptide-3 to the skin using microemulsions or nanoemulsions for facial oil reduction was the focus of this study. The impact factors affecting oil/water transparent dispersion formation, such as the surfactant system, HLB value, and co-solvent, were identified through the water titration method and pseudoternary phase diagram plots. The interfacial tension between caprylic/capric triglyceride (CCT oil) and water was significantly reduced by the surfactant/co-surfactant combination (Smix) of Cremophore® RH40 and a double-tails co-surfactant, polyglycerol-3-diisostearate, at an HLB of 13 together with a water-to-co-solvent (PG) ratio of 1:1. A two-level full factorial design of experiment (FFD-DoE) emphasized the independent variables of the HLB value, co-solvent, and CCT oil contents affecting the optimal compositions for micro- or nanoemulsion formation. The low-energy spontaneous emulsification of the optimized combination at a low Smix content (10%) yielded the translucent oil-in-water Tripeptide-3 nanoemulsions with an internal droplet size of 25.7 ± 1.20 nm, a narrow polydispersity index of 0.237 ± 0.129, and 70.6 ± 0.58% transmittance. The in vitro skin permeation study revealed a significantly higher skin penetration and retention of the Tripeptide-3 nanoemulsions compared to the high surfactant microemulsions and coarse emulsions. Skin irritation and oil control efficacy were evaluated in healthy volunteers before and after product application for 28 days. The obtained nanoemulsions not only decreased sebum production but also enhanced skin moisture levels. In conclusion, the meticulously designed nanoemulsions, incorporating suitable excipients, show a promising delivery system for hydrophilic peptides to control sebum overproduction in oily facial skin.

Natural Stabilizers and Nanostructured Lipid Carrier Entrapment for Photosensitive Compounds, Curcumin and Capsaicin.

Capsaicin and curcumin, the active components of chili and turmeric, are prone to instability when exposed to light. Therefore, this research aimed to enhance the photostability of both extracts via the use of antioxidants, natural sunscreen, and nanostructured lipid carriers (NLCs). NLCs were chosen for this this study due to their advantages in terms of stability, drug loading capacity, occlusive effect, skin penetration, and controlled release. The photostability of each extract and extracts mixed with antioxidants, including grape seed extract, tea extract, and chlorogenic acid, were determined. Chlorogenic acid can enhance the photostability of capsaicin from 6.79 h to 16.50 h, while the photostability of curcumin increased from 9.63 h to 19.25 h. In addition, the use of natural sunscreen (sunflower oil) also increased the photostability of capsaicin and curcumin. The mixed extracts were then loaded into NLCs. The particle size of the formulation was 153.73 nm with a PDI value of 0.25. It exhibited high entrapment efficiency (more than 95%). In addition, it effectively reduced the decomposition of capsaicin and curcumin. Importantly, the natural stabilizers chosen for NLC fabrication significantly improved the photostability of curcumin and capsaicin by 600% and 567% compared to the unstabilized counterparts. This improvement contributes to the sustainability and bioavailability of these compounds in both cosmeceutical and pharmaceutical products.

Influence of Benincasa hispida Peel Extracts on Antioxidant and Anti-Aging Activities, including Molecular Docking Simulation.

Benincasa hispida peel, a type of postconsumer waste, is considered a source of beneficial phytochemicals. Therefore, it was subjected to investigation for biological activities in this study. B. hispida peel was extracted using 95% v/v, 50% v/v ethanol and water. The obtained extracts were B95, B50 and BW. B95 had a high flavonoid content (212.88 ± 4.73 mg QE/g extract) and phenolic content (131.52 ± 0.38 mg GAE/g extract) and possessed high antioxidant activities as confirmed by DPPH, ABTS and lipid peroxidation inhibition assays. Moreover, B95 showed inhibitory effects against collagenase and hyaluronidase with values of 41.68 ± 0.92% and 29.17 ± 0.66%, which related to anti-aging activities. Via the HPLC analysis, one of the potential compounds found in B95 was rutin. Molecular docking has provided an understanding of the molecular mechanisms underlying the interaction of extracts with collagenase and hyaluronidase. All extracts were not toxic to fibroblast cells and did not irritate the hen's egg chorioallantoic membrane, which indicated its safe use. In conclusion, B. hispida peel extracts are promising potential candidates for further use as antioxidant and anti-aging agents in the food and cosmetic industries.

The in vitro effects of black soldier fly larvae (Hermitia illucens) oil as a high-functional active ingredient for inhibiting hyaluronidase, anti-oxidation benefits, whitening, and UVB protection.

Objective: Larvae of Hermitia illucens, or black soldier fly larvae (BSFL), have been recognized for their high lipid yield with a remarkable fatty acid profile. BSFL oil (SFO) offers the added value of a low environmental footprint and a sustainable product. In this study, the characteristics and cosmetic-related activities of SFO were investigated and compared with rice bran oil, olive oil and krill oil which are commonly used in cosmetics and supplements. Methods: The physicochemical characteristics were determined including acid value, saponification value, unsaponifiable matter and water content of SFO. The fatty acid composition was determined using GC-MS equipped with TR-FAME. The in vitro antioxidant properties were determined using DPPH, FRAP and lipid peroxidation inhibition assays. Antihyaluronidase (anti-HAase) activity was measured by detecting enzyme activity and molecular docking of candidate compounds toward the HAase enzyme. The safety assessment towards normal human cells was determined using the MTT assay and the UVB protection upon UVB-irradiated fibroblasts was determined using the DCF-DA assay. The whitening effect of SFO was determined using melanin content inhibition. Results: SFO contains more than 60% polyunsaturated fatty acids followed by saturated fatty acids (up to 37%). The most abundant component found in SFO was linoleic acid (C18:2 n-6 cis). Multiple anti-oxidant mechanisms of SFO were discovered. In addition, SFO and krill oil prevented hyaluronic acid (HA) degradation via strong HAase inhibition comparable with the positive control, oleanolic acid. The molecular docking confirmed the binding interactions and molecular recognition of major free fatty acids toward HAase. Furthermore, SFO exhibited no cytotoxicity on primary human skin fibroblasts, HaCaT keratinocytes and PBMCs (IC50 values > 200 µg/mL). SFO possessed significant in-situ anti-oxidant activity in UVB-irradiated fibroblasts and the melanin inhibition activity as effective as well-known anti-pigmenting compounds (kojic acid and arbutin, p < 0.05). Conclusion: This study provides scientific support for various aspects of SFO. SFO can be considered an alternative oil ingredient in cosmetic products with potential implications for anti-skin aging, whitening and UVB protection properties, making it a potential candidate oil in the cosmetic industry.

Antioxidant, Anti-Inflammatory and Attenuating Intracellular Reactive Oxygen Species Activities of Nicotiana tabacum var. Virginia Leaf Extract Phytosomes and Shape Memory Gel Formulation.

Oxidative stress is one of the major causes of skin aging. In this study, the shape memory gels containing phytosomes were developed as a delivery system for Nicotiana tabacum var. Virginia fresh (VFL) and dry (VDL) leaf extracts. The extracts were loaded in the phytosomes by a solvent displacement method. The physical and chemical characteristics and stability of phytosomes were evaluated by dynamic light scattering and phytochemistry, respectively. The in vitro antioxidant activity and intracellular reactive oxygen species reduction of phytosomes and/or extracts were investigated by the DPPH and ABTS radical scavenging assays, FRAP assay, and DCFH-DA fluorescent probe. The cytotoxicity and anti-inflammatory activity of VDL and VFL phytosomes were studied by an MTT and a nitric oxide assay, respectively. Here, we first reported the total phenolic content in the dry leaf extract of N. tabacum var. Virginia was significantly greater than that of the fresh leaf extract. The HPLC analysis results revealed that VDL and VFL extracts contained 4.94 ± 0.04 and 3.13 ± 0.01 µg/mL of chlorogenic acid and 0.89 ± 0.00 and 0.24 ± 0.00 µg/mL of rutin, respectively. The phytosomes of the VDL and VFL extracts displayed stable size, polydispersity index, zeta potential values, and good chemical stability. VDL and VDL phytosomes showed higher phenolic and flavonoid contents which showed stronger DPPH and ABTS radical scavenging effects and reduced the intracellular ROS. The results suggested that the phenolic compounds are the main factor in their antioxidant activity. Both VDL and VFL phytosomes inhibited nitric oxide production induced by LPS, suggesting the anti-inflammatory activity of the phytosomes. The shape memory gel containing VDL and VFL phytosomes had good physical stability in terms of pH and viscosity. The VDL and VFL phytosomes dispersed in the shape memory gels can be considered as a promising therapeutic delivery system for protecting the skin from oxidation and reactive oxygen species.

Comparison of Biological Activities and Protective Effects on PAH-Induced Oxidative Damage of Different Coffee Cherry Pulp Extracts.

Polycyclic aromatic hydrocarbons (PAHs) are the main toxic components of ambient air particulate matter (PM), causing oxidative damage to the skin and ultimately resulting in skin aging. This study was conducted to determine the anti-oxidant, anti-aging properties and protective effects of the extracts of coffee cherry pulp (Coffea arabica L.), which is a by-product of the coffee industry, against the oxidative damage induced by PAH exposure in human epidermal keratinocytes (HaCaT). Three different techniques were used to extract the coffee cherry pulp: maceration, Soxhlet and ultrasonication to obtain CCM, CCS and CCU extract, respectively, which were then compared to investigate the total phenolic content (TPC) and total flavonoid content (TFC). The chemical compositions were identified and quantified using high-performance liquid chromatography (HPLC). The results demonstrated that Soxhlet could extract the highest content of chlorogenic acid, caffeine and theophylline. CCS showed the significantly highest TPC (324.6 ± 1.2 mg GAE/g extract), TFC (296.8 ± 1.2 mg QE/g extract), anti-radical activity against DPPH free radicals (98.2 ± 0.8 µM Trolox/g extract) and lipid peroxidation inhibition (136.6 ± 6.2 µM Trolox/g extract). CCS also showed the strongest anti-aging effects based on collagenase, elastase, hyaluronidase and tyrosinase inhibitory enzymes. In addition, CCS can protect human keratinocyte cells from PAH toxicity by increasing the cellular anti-oxidant capacity. This study suggests that CCS has the potential to be used as a cosmetic material that helps alleviate skin damage caused by air pollution.

Stability enhancement of lycopene in Citrullus lanatus extract via nanostructured lipid carriers.

Lycopene is one of naturally occurring carotenoids in plants including watermelon (Citrullus lanatus). Heat, light, and oxygen effect on lycopene isomerization and degradation. Nanostructured lipid carriers (NLCs) are drug delivery system which can enhance the stability of active compound. Therefore, this study aimed to develop watermelon extract loaded in NLCs for lycopene stability improvement. The NLCs were prepared using a hot homogenization technique. Cocoa butter was used as solid lipid. Grape seed oil was used as liquid lipid. Span® 80 and Plantasens® HE20 were used as an emulsifier. The selected unloaded NLCs contained solid lipid to liquid lipid at the ratio of 3:1 and 10% (w/w) of total lipid. The particle size of watermelon extract-loaded NLCs (WH-loaded NLCs) was 130.17 ± 0.72 nm with low PDI and high zeta potential. It also presented high entrapment efficiency. For stability study, the WH-NLC3 could enhance stability and maintain lycopene content after stability test. It exhibited the highest values of lycopene content (83.26 ± 2.30%) when stored at 4°C. It also possessed a prolonged release pattern over 48 hr. Therefore, the NLCs could improve stability and release profile of lycopene from watermelon extract.

Chemical Constituents, Antioxidant, Anti-MMPs, and Anti-Hyaluronidase Activities of Thunbergia laurifolia Lindl. Leaf Extracts for Skin Aging and Skin Damage Prevention.

This study aimed to investigate the potential usage of Thunbergia laurifolia Lindl. leaf extracts in the cosmetic industry. Matrix metalloproteinases (MMPs) and hyaluronidase inhibition of T. laurifolia leaf extracts, prepared using reflux extraction with deionized water (RE) and 80% v/v ethanol using Soxhlet's apparatus (SE), were determined. Rosmarinic acid, phenolics, and flavonoids contents were determined using high-performance liquid chromatography, Folin-Ciocalteu, and aluminum chloride colorimetric assays, respectively. Antioxidant activities were determined by 1,1-diphenyl-2-picrylhydrazyl (DPPH) and linoleic acid-thiocyanate assays. MMP-1 inhibition was investigated using enzymatic and fluorescent reactions, whereas MMP-2, MMP-9, and hyaluronidase inhibition were investigated using gel electrophoresis. Cytotoxicity on human fibroblast cell line was also investigated. The results demonstrated that SE contained significantly higher content of rosmarinic acid (5.62% ± 0.01%) and flavonoids (417 ± 25 mg of quercetin/g of extract) but RE contained a significantly higher phenolics content (181 ± 1 mg of gallic acid/g of extract; p < 0.001). SE possessed higher lipid peroxidation inhibition but less DPPH• scavenging activity than RE. Both extracts possessed comparable hyaluronidase inhibition. SE was as potent an MMP-1 inhibitor as gallic acid (half maximal inhibitory concentration values were 12.0 ± 0.3 and 8.9 ± 0.4 mg/cm3, respectively). SE showed significantly higher MMP-2 and MMP-9 inhibition than RE (p < 0.05). Therefore, SE is a promising natural anti-ageing ingredient rich in rosmarinic acid and flavonoids with antioxidant, anti-hyaluronidase, and potent MMPs inhibitory effects that could be applied in the cosmetic industry.

Phonophoresis of Phyllanthus amarus nanoparticle gel improves functional capacity in individuals with knee osteoarthritis: A randomized controlled trial.

OBJECTIVE: This study examined the effects of treatment with Phyllanthus amarus nanoparticle gel applied by phonophoresis (PP) and ultrasound therapy (UT) in patients with symptomatic knee osteoarthritis (OA) using a randomized, double-blind, controlled trial. METHODS: Patients with knee OA (n = 40; mean age ±â€¯SD, 64.30 ±â€¯9.71 years), who had visual analogue scale (VAS) scores for knee pain intensity of 68.00 ±â€¯9.58 (UT group) and 71.00 ±â€¯8.74 (PP group, respectively) before treatment, were randomly allocated into two groups. Both groups were treated with an ultrasound program in continuous mode, 1.0 W/cm2, 10 min per session, for 10 sessions. Nanoparticles of P. amarus were used in the PP group, whereas a nondrug coupling gel was used in the UT group. The 6-min walk test (6-MWT) was performed to evaluate functional capacity. The VAS and the 6-MWT were evaluated before and after 10 treatment sessions in both groups using a double-blind procedure. RESULTS: VAS and 6-MWT showed significant improvement after treatment in both groups (p < 0.05). The PP group showed more significant effects than the UT group, in terms of both reducing the VAS pain score (p < 0.05) and improving 6-MWT (p < 0.05). CONCLUSIONS: PP is suggested as an effective method for the treatment of symptomatic knee OA for reducing pain and improving functional capacity.

Phonopheresis Associated with Nanoparticle Gel from Phyllanthus amarus Relieves Pain by Reducing Oxidative Stress and Proinflammatory Markers in Adults with Knee Osteoarthritis / 中国结合医学杂志

OBJECTIVE@#To determine the changes in serum levels of inflammatory biomarkers and antioxidant levels among the knee osteoarthritis (OA) patients after treatment with Phyllanthus amarus (PP) by nanoparticle gel phonophoresis.@*METHODS@#This study was a randomized, double-blind, placebo-control, parallel-group, clinical trial involving 30 subjects with mild-to-moderate degree of knee OA. The patients were allocated to two groups using a computer-generated random numbers, and received conventional ultrasound therapy (control group, 15 cases) and PP (treatment group, 15 cases) once daily for 10 sessions. The pain was evaluated by visual analogue scale (VAS). Serum levels of tumor necrosis factor-α (TNF-α) were determined by enzyme-linked immunosorbnent assay (ELISA). Nitric oxide (NO) was determined by modified Griess reagent. The antioxidant effects, including superoxide dismutase (SOD) and total antioxidant capacity (TAC), were also measured by ELISA assay.@*RESULTS@#The VAS score was significantly decreased in the treatment group compared with the control group after treatment (P<0.01). The serum concentrations of TNF-α and NO were significantly reduced in the treatment group compared with the control group (P<0.01) after treatment. However, the serum concentrations of SOD and TAC in the treatment group were significantly higher after treatment compared with the control group (P<0.01).@*CONCLUSION@#PP could alleviate knee pain and significantly reduce systemic anti-inflammatory effects in knee OA patients.

Appraisal of biological activities and identification of phenolic compound of African marigold (Tagetes erecta) flower extract.

The flowers of African marigold (Tagetes erecta L), a medicinal plant widely cultivated in Thailand, were subjected to evaluation for total phenolics, DPPH scavenging and thiobarbituric acid-reactive substance (TBARs) assays as well as tyrosinase inhibitory activity. In preliminary studies, the ethyl acetate (EA) extract obtained by continuous extraction showed the highest activities with highest phenolic content among all extracts. Bioassay-guided fractionation of EA extract led to isolation of a flavonoid identified as quercetagetin. Interestingly, it was found that quercetagetin exhibited potent DPPH scavenging activity with IC50 of 3.70 µg/ml which is about 2-3 times higher activity than standard quercetin (IC50 5.07 µg/ml) and trolox (IC50 9.93 µg/ml). Moreover, it exhibited tyrosinase inhibitory activity on L-tyrosine (IC50 89.31 µg/ml), higher than α- and ß-arbutins (IC50 157.77 and 222.35 µg/ml) and slightly higher (IC50 128.41 µg/ml) than ellagic acid (IC50 151.1 µg/ml) when using L-DOPA as substrate. Testing with skin fibroblasts, all the extracts and quercetagetin demonstrated no toxic effect. These finding strongly indicate that African marigold flower is a promising source of natural antioxidative and tyrosinase inhibitory substances with safe to skin.