Medicinal plants are candidates for the discovery of potential new anti-inflammatory agents. Curcumin is the active compound found in turmeric root, which has high anti-inflammatory activity. One of ...the limitations of curcumin as a therapeutic agent is its low solubility in water and extensive first-pass effect metabolism. The aim of this study was to formulate curcumin nanoemulsion for parenteral injection. We prepared curcumin nanoemulsions with a homogenizer using three surfactant concentrations (1.8%; 2.4%; and 3%) and two curcumin concentrations (1% and 3%). Formulas were evaluated for droplet diameter, polydispersity index, zeta potential, viscosity, pH, entrapment efficiency (EE), osmolality, sterility, and morphology. The nanoemulsion containing 1% curcumin and 3% surfactant (F3) demonstrated good stability. Curcumin nanoemulsions at 20 and 40 mg/kg doses showed anti-inflammatory activity on carrageenan-induced paw edema in male Sprague-Dawley rats. These two doses inhibited paw edema by 33% and 56% respectively at 5 h after carrageenan induction. Inhibition of edema volume by curcumin nanoemulsion at a dose of 40 mg/kg did not show a significant difference (P > 0.05) compared to the activity of the standard drug ketorolac at a dose of 2.7 mg/kg. We conclude that curcumin nanoemulsion has anti-inflammatory activity and can be a promising anti-inflammatory agent.
Intranasal drug transport through the olfactory route to the brain is an effective drug route for increased absorption and bioavailability of the drug. The objective of this study was to increase the ...penetration of valproic acid as an anticonvulsant into a delivery system comprising liposomes. Valproic acid liposomes were prepared by a thin-layer hydration technique using soybean phosphatidylcholine and cholesterol as the main ingredients. The formulations were evaluated for diameter size, entrapment efficiency (EE), zeta potential, polydispersity index, and morphology. ex vivo permeation using sheep nasal mucosa and in vivo efficacy were assessed by performing a pharmacokinetic study in Wistar albino rats following intranasal administration of the formulations in comparison with pure drug. The mean size particle of optimized liposomes ranged from 90 to 210 nm with a low polydispersity index (<0.5). The EE of optimized liposomes was between 60% and 85%, increasing the concentration of phosphatidylcholine added to the formula. Transmission electron microscopy observations (40,000×) showed that valproic acid liposomes have a spherical molecular shape and a particle size of below 250 nm. The ex vivo and in vivo results showed that liposomal formulations provided enhanced brain exposure. Among the formulations studied, Formula 4 (F4) showed greater uptake of valproic acid into the brain than plasma. The high brain targeting efficiency index for F4 indicated the preferential transport of the drug to the brain. The study demonstrated the successful formulation of surface-modified valproic acid liposomes for nasal delivery with brain targeting potential.
Intranasal; Liposome; Valproic acid; Penetration; Epilepsy; Brain.
N-Methyl-3, 4-methylenedioxyamphetamine (MDMA), or ecstasy is a recreational drug of abuse. It is a synthetic substance that affects the body’s systems, which its mechanism of action and treatment ...should be more investigated. MDMA provides an immediate enjoyable feeling by stimulating the release of neurotransmitters, such as dopamine and serotonin in the brain. Unfortunately, abnormal regulation of the brain neurotransmitters, as well as the increased oxidative stress causes damage to the brain neurons after the MDMA exposure. Only a few studies have been done regarding its treatment. Thus, the treatment of MDMA complications should be further explored mainly by targeting its mechanism of action in the neurotransmitter systems. Hence, this study presents a short review regarding the recent findings on the role of neurotransmitters to cause MDMA neurotoxicity. The results will be useful for future research in elucidating the potential treatment based on the targeted mechanisms to treat the neurotoxic effects of MDMA.
Tobacco leaf contains antibacterial secondary metabolite compounds, such as phenol, alkaloids, and essential oils. This study compares the potential antibacterial effects of Indonesian tobacco leaf ...extracted using the heat reflux method (producing an extract) and pyrolysis method (providing a bio-oil). The tobacco leaf extract was challenged against Staphylococcus aureus ATCC 25923, Enterococcus faecalis ATCC 29212, Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853. The bio-oil from the pyrolysis method showed inhibitory Kirby Bauer zones higher than those of the extract from heat reflux method, with the maximum results in the pyrolysis method indicating zones of 6.35 mm (S. aureus), 5.90 mm (E. faecalis), 3.97 mm (E. coli), and 5.025 mm (P. aeruginosa). Further study analyzed the effectiveness of the disc and well diffusion antibacterial test methods for measuring the antibacterial effect of bio-oils against Escherichia coli ATCC 25922 and Pseudomonas aeruginosa ATCC 27853. The bio-oil used in the well diffusion test method showed the most significant antibacterial effectiveness. It showed the biggest inhibition zone, with a maximum of 11.65 mm and 8.90 mm for E. coli and P. aeruginosa. Our results showed Nicotiana tabacum var. Virginia Bio Oil from Ponorogo (Indonesia) is a strong potential antimicrobial, especially using well diffusion test.
Pharmaceutical dosage forms containing gelatin are recently of high attention in regard to its porcine content. In Muslim countries, halal products assurance is strictly regulated, not only for food ...but also for pharmaceutical products. This study aimed to develop gelatin identification and verification method in capsule shells by performing simple simultaneous protein- and nucleic acid based-identification methods. Identification and verification performing polyacrylamide gel electrophoresis (PAGE)—coupled with principle component analysis, and polymerase-chain-reaction (PCR)-restriction fragment length polymorphism (RFLP) were carried out. Gelatin was obtained by extracting the capsules using cold acetone; the precipitate was used directly for PAGE, and was used as well for DNA extraction. The results showed that the porcine gelatin reference showed 12 major bands of peptide profile, with predominant bands at ±200 and ±100–135 kDa on 8 % Tris-glycine gel, while bovine gelatin only showed four major bands. Further, PCR-RFLP result showed two specific bands of the porcine gelatin DNA at 228 and 131 bp, whereas the bovine gelatin DNA bands occurred at 316 and 44 bp. The results demonstrated that the capsule shell samples used in this study contained the following: sample 1 was verified contain porcine gelatin, whereas the three other samples identified contain bovine gelatin. Although the simultaneous approaches seemed need to be improved, it is crucial to maintain their low cost and simple protocol.
Objective: Centella asiatica (Pegagan) contains asiaticoside for treatment of striae patients by increasing the synthesis of collagen. Asiaticoside has a large hydrophilic molecule (959.12 g/mol), ...causing difficulty in penetration through the skin. Nanoemulsion has small droplet size so that the active substance can be delivered into the skin layer. This study aims to formulate and test the stability of nanoemulsion lotion containing pegagan extract. Methods: Nanoemulsion containing pegagan extract formulated in the form of lotion using High Pressure Homogenizer. Nanoemulsion lotion were then evaluated and tested for penetration in vitro. Result: The mean particle size of nanoemulsion was 19.88 ± 2.3 nm and nanoemulsion in lotion was 198.4 ± 11.52 nm; polydispersity index value 0.329 ± 0.065, and zeta potensial was -30.9 mV. Nanoemulsion lotion was stable against storage for 8 weeks at cold, room, and high temperature (4 ± 2°C, 28 ± 2°C, 40 ± 2°C). There were no change in physical properties and pH value of the nanoemultion lotion. The cumulative amount of the penetrated asiaticoside was 1558.65 ± 66.93 μg/cm2 for nanoemulsion lotion and 1260.364 ± 71.42 μg/cm2 for lotion only. Flux of nanoemulsion lotions and lotion were 2.1255 ± 0.31 μg/cm2/hr and 1.4506 ± 0.49 μg/cm2/hr, respectively. Conclusion: It can be concluded that nanoemulsion lotion stable in physical properties during storage and can penetrate more than the non nanoemulsion lotion.
Objective: An emulsion of black cumin seed oil was developed using an orally safe surfactant, sucrose palmitate, to make it more comfortable to consume.
Methods: The emulsion was made using a 3% ...concentration of sucrose palmitate to emulsify 5% (F1) and 7.5% (F2) black cumin seed oil to the developed stable emulsion. The hedonic test was applied to 30 panelists, showing the accepted formulation.
Results: The pH value of each formulation degraded during 12 w of storage. The formula of 5% oil (F1) has better physical stability, and its bioactive component, Thymoquinone, showed a slight degradation on the first day. But it showed a rapid degradation after 60 d of storage due to its instability in a solution. The F1 formula (mean = 3.1667) is more preferred than the F2 formula (mean = 3) of the 1-5 hedonic scale, with the significance score (p) valued less than 0.05 and considered to be significantly different from its original form.
Conclusion: The emulsion of black cumin oil can be developed and more comfortable to consume.
Objective: The study aimed to evaluate the physicochemical properties and nutrition of Moringa leaf extract. In addition, the preliminary study for the preparation of Moringa leaf extract-loaded ...phytosomes for a supplement.
Methods: Extraction of Moringa leaf made using microwave-assisted extraction, followed by evaluation of proximate analysis (water, total ash, acid-insoluble of ash contents, and residual n-hexane), phytochemical screening, and nutrition such as crude protein, amino acids, and minerals (iron, zinc, and calcium). The phytosomes were prepared by the anti-solvent precipitation method and assessed for the morphology, particle size, zeta potential, polydispersity index (PDI), entrapment efficiency (EE), and Fourier-transform infrared spectra.
Results: The nutrition contents of crude protein, iron, zinc, and calcium were 19.61±0.07%, 3.47±0.00 mg/100g, 5.46±0.05 mg/100g, and 747.40±4.89 mg/100g, respectively. The amino acids with the highest concentrations were glutamic acid, phenylalanine, aspartic acid, alanine, and arginine in the extract. The best preparation using sonication 10 min by morphology was a spherical included particle size, PDI, zeta potential, and EE of arginine was 87.16±1.73 nm, 0.22±0.04, −23.07±0.76 mV, and 108.94±0.52%, respectively.
Conclusion: These preliminary results provide evidence of the nutritional benefit of Moringa leaf extract-loaded phytosomes as a promising supplement to prevent stunting in children.
Objective: The purpose of this study was to formulate a phytosome lotion from Mangkokan leaf using green solvent extraction.
Methods: Ionic liquid, 1-butyl-3-methylimidazolium tetrafluoroborate, ...combined with microwave-assisted extraction, was used to obtain flavonoid compounds. Mangkokan leaf extract was formulated into a phytosome with three different ratios of phospholipon (1:0.5), (1:1), and (1:2). Three phytosome formulas were analyzed to identify the best formula. The analysis included morphology, particle size, and zeta potential, entrapment efficiency, and spectrum analysis using an FTIR spectrophotometer. The formula which chosen was formulated into three lotion formulas with different concentration (20%; 25%; 30%) then, evaluated for physical stability, and hair growth activity test included hair length, weight, and diameter. Minoxidil and non-phytosome lotion were used as comparison. Data were analyzed using two-way ANOVA.
Results: The FTIR of phytosome was confirmed a complex formation of extract and phospholipon. The phytosome morphology was displayed irregular spherical vesicles. Phytosome with the ratio of phospholipon (1:0.5) was formulated into lotion because has a smaller particle size (289 nm), and higher entrapment efficiency (99.76%±0.24) than others. Phytosome lotions displayed higher activity than 2% minoxidil (p = 0.0001). Phytosome lotion (30%) thus showed the highest efficacy for hair length, weight and diameter.
Conclusion: Mangkokan leaf that extracted using 1-butyl-3-methylimidazolium tetrafluoroborate solvent combined with microwave-assisted extraction then formulated into phytosome lotion has higher activity than 2% minoxidil. Lotion that contains 30% mangkokan leaf phytosome was showed the highest efficacy.
Objective: The main objective of this research is to make and evaluate the formulation of a griseofulvin microemulsion gel for topical use to increasethe solubility and safety of the drug.Methods: ...The optimized microemulsion formula contains 5% oleic acid as the oil phase, 25% Tween 80 as the surfactant, and 20% ethanol (96%)as the cosurfactant.Results: Organoleptic observations of the microemulsion showed that it had a clear and transparent yellowish color, while the microemulsion gel hada hazy yellowish color. Both the microemulsion and the microemulsion gel had the smell of alcohol. The size of the globules in the microemulsion andthe microemulsion gel was 158.0 nm and 226.0, respectively.Conclusions: The griseofulvin microemulsion gel was stable at 4°C±2°C, 25°C±2°C, and 40°C±2°C.
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