RESUMEN
This study aimed to characterize and investigate the potential of the oils from Gryllus bimaculatus, Teleogryllus mitratus, and Acheta domesticus to be used in nanoemulsions. The oils were extracted by a cold press method and characterized for their fatty acid profiles. Their irritation effects on the chorioallantoic membrane (CAM) were evaluated, along with investigations of solubility and the required hydrophilic-lipophilic balance (RHLB). Various parameters impacting nanoemulsion generation using high-pressure homogenization were investigated. The findings revealed that G. bimaculatus yielded the highest oil content (24.58% w/w), followed by T. mitratus (20.96% w/w) and A. domesticus (15.46% w/w). Their major fatty acids were palmitic, oleic, and linoleic acids. All oils showed no irritation, suggesting safety for topical use. The RHLB values of each oil were around six-seven. However, they could be successfully developed into nanoemulsions using various surfactants. All cricket oils could be used for the nanoemulsion preparation, but T. mitratus yielded the smallest internal droplet size with acceptable PDI and zeta potential. Nanoemulsion was found to significantly enhance the antioxidant and anti-skin wrinkle of the T. mitratus oil. These findings pointed to the possible use of cricket oils in nanoemulsions, which could be used in various applications, including topical and cosmetic formulations.
RESUMEN
Capsaicin is an active compound in chili peppers (Capsicum chinense) that has been approved for chronic pain treatment. The topical application of high-strength capsaicin has been proven to reduce pain; however, skin irritation is a major drawback. The aim of this study was to investigate an appropriate and scalable technique for preparing nanostructured lipid carriers (NLCs) containing 0.25% capsaicin from capsicum oleoresin (NLC_C) and to evaluate the irritation of human skin by chili-extract-loaded NLCs incorporated in a gel formulation (Gel NLC_C). High-shear homogenization with high intensity (10,000 rpm) was selected to create uniform nanoparticles with a size range from 106 to 156 nm. Both the NLC_C and Gel NLC_C formulations expressed greater physical and chemical stabilities than the free chili formulation. Release and porcine biopsy studies revealed the sustained drug release and significant permeation of the NLCs through the outer skin layer, distributing in the dermis better than the free compounds. Finally, the alleviation of irritation and the decrease in uncomfortable feelings following the application of the Gel NLC_C formulation were compared to the effects from a chili gel and a commercial product in thirty healthy volunteers. The chili-extract-loaded NLCs were shown to be applicable for the transdermal delivery of capsaicin whilst minimizing skin irritation, the major noncompliance cause of patients.
Asunto(s)
Capsaicina/administración & dosificación , Capsicum/química , Sistemas de Liberación de Medicamentos , Nanoestructuras/administración & dosificación , Pruebas de Irritación de la Piel/métodos , Piel/efectos de los fármacos , Administración Cutánea , Adulto , Preparaciones de Acción Retardada , Femenino , Humanos , Masculino , Persona de Mediana Edad , Nanoestructuras/química , Adulto JovenRESUMEN
In the present study, the fractionated extracts of Sesbania grandiflora bark were prepared and evaluated for their biological activities. The ethyl acetate fractionate (EAF) showed high antioxidant activity along with free radical scavenging and reducing mechanisms. The free radical scavenging antioxidant activity of EAF was 69.3 ± 3.6% where its Trolox equivalent antioxidant capacity was 13.6 ± 0.7 mM/mg. EAF exhibited the reducing power equivalent to ferrous sulfate at 152 ± 2 mM/mg and equivalent to gallic acid at 1.05 ± 0.01 mM/mg. In addition, EAF presented high potential on inhibition of bacterial growth with the minimum bactericidal concentration less than 1 mg/mL. Further isolation of EAF using normal-phase open column of silica gel 60, showed that the fractions eluted with the mixture of chloroform and methanol at the ratios of 4:1, 3:2, and 2:3 possessed antibacterial activity. The recovery activity of total different active fractions was 5% EAF, 20 times less than that of EAF. The chromatogram of EAF from a high-performance liquid chromatography was compared with caffeic acid, catechin, coumaric acid, ellagic acid, gallic acid, quercetin, syringin, naringic acid, trans-cinnamic acid, and vanilic acid. The result demonstrated that one major compound of EAF was gallic acid. These results suggest that the fractionated extracts of S. grandiflora bark contained antioxidant and antibacterial activities.
Asunto(s)
Antibacterianos/farmacología , Antioxidantes/farmacología , Corteza de la Planta , Extractos Vegetales/farmacología , Sesbania , Staphylococcus aureus/efectos de los fármacos , Ácidos Cafeicos/química , Catequina/química , Cromatografía Liquida , Cinamatos/química , Ácidos Cumáricos/química , Ácido Elágico/química , Depuradores de Radicales Libres/farmacología , Ácido Gálico/química , Glucósidos/química , Pruebas de Sensibilidad Microbiana , Fenilpropionatos/química , Extractos Vegetales/química , Quercetina/química , Staphylococcus aureus/crecimiento & desarrollo , Ácido Vanílico/químicaRESUMEN
CONTEXT: Antibiotic resistance is a serious problem worldwide. Searching for new potential agents is, therefore, essential. The bark of Sesbania grandiflora (L.) Pers. (Fabaceae) has been used in folk medicine against various diseases. OBJECTIVE: To investigate the antibacterial activity of S. grandiflora bark and explore the therapeutic effect of the highest potent fraction. MATERIALS AND METHODS: Bacteria and healthy silkworms were exposed to three fractionated extracts (3.1-400 mg/mL) of S. grandiflora bark from hexane (HXF), chloroform (CFF), and ethyl acetate (EAF). The sets of bacteria were incubated at 37 °C while silkworms were kept at 27 °C for 24 h. To evaluate the therapeutic effect, silkworms infected with bacteria were exposed to the extracts (0.5-60 mg/mL) and incubated at 27 °C for 52 h. Qualitative analysis of the most potent extract was done using HPLC. RESULTS: EAF showed the highest activity with MIC against methicillin resistant Staphylococcus aureus (MRSA) and vancomycin resistant enterococci (VRE) of 1.6 and 0.4 mg/mL, respectively, and against Gram-negative Escherichia coli and Pseudomonas aeruginosa of 6.2 and 3.1 mg/mL, respectively. It is nontoxic to silkworms with LC50 >400 mg/mL and has high therapeutic effect on infected silkworms with EC50 of 1.9 mg/mL. EAF consists of at least five major compounds, one of them is gallic acid. The activity of EAF is higher than the sum of individual activities of separated compounds. DISCUSSION AND CONCLUSION: These results suggest that EAF is a promising antibacterial extract, suitable for further investigation in rodents infected with drug resistant bacteria.
Asunto(s)
Antibacterianos/farmacología , Bombyx/efectos de los fármacos , Bombyx/microbiología , Extractos Vegetales/farmacología , Sesbania , Animales , Antibacterianos/aislamiento & purificación , Relación Dosis-Respuesta a Droga , Escherichia coli/efectos de los fármacos , Escherichia coli/fisiología , Staphylococcus aureus Resistente a Meticilina/efectos de los fármacos , Staphylococcus aureus Resistente a Meticilina/fisiología , Pruebas de Sensibilidad Microbiana/métodos , Corteza de la Planta , Extractos Vegetales/aislamiento & purificación , Pseudomonas aeruginosa/efectos de los fármacos , Pseudomonas aeruginosa/fisiologíaRESUMEN
Clinical applications of Sesbania grandiflora bark extract (SGE) are limited because of its poor water solubility and stability. SGE was loaded in micelles of Pluronics. In vitro and in vivo antibacterial and toxicity tests were investigated using broth dilution and silkworm model. Aqueous solubility of SGE was improved by these micelles. Activity and toxicity of SGE loaded micelles were dependent on type and concentration of Pluronics. The micelles composed of 1:3 SGE to Pluronic F68 (SGE-PF68-13) showed small size (24.95 ± 0.34 nm), narrow PdI (<0.2), high entrapment efficiency (99.63 ± 0.19%) and negative zeta potential (-41.53 ± 0.15 mV). Stability of SGE in SGE-PF68-13 was 10 times higher than the unentrapped SGE. SGE-PF68-13 showed a dose dependent activity and significantly higher therapeutic effect than the unentrapped SGE. It is concluded that encapsulation of SGE in Pluronic micelles can enhance SGE solubility, stability, and antibacterial activity. SGE-PF68-13 is suitable for further study in mammalian animals.