FORMULATION AND PHYSICAL STABILITY TEST OF GRISEOFULVIN MICROEMULSION GEL

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

FORMULATION OF NIOSOMAL GEL CONTAINING GREEN TEA EXTRACT (CAMELLIA SINENSIS L. KUNTZE) USING THIN-LAYER HYDRATION

Objective: Green tea is known as a source of antioxidants. The most abundant of these is epigallocatechin gallate, which has been shown to modulatebiochemical pathways in the skin. Niosomes are an alternative to liposomal drug-vehicle systems, which have disadvantages such as cost and stability.To overcome the problem of low permeation of active substances through skin layers and to increase their stability, a topical antioxidant preparationbased on niosomes was prepared.Materials and Methods: To enhance drug stability, niosomal formulations were prepared in four different molar ratios of surfactant-to-cholesterol,that is, 3:1 (F1), 2:1 (F2), 1:1 (F3), and 0.5:1 (F4). These were prepared using the thin-layer method. The niosomal suspensions were evaluated forparticle size and distribution, lamellarity, encapsulation efficiency, and zeta potential, and were then incorporated into gels using hydroxypropylmethylcellulose as the gelling agent. The niosomal gels were evaluated for organoleptic properties, pH, viscosity, stability, and antioxidant activityusing 1,1-diphenyl-2-picrylhydrazyl.Results: Results for the suspensions showed that F1 had the best encapsulation efficiency but experienced separation after 7 days.Conclusions: Results for the niosomal gels (using F3) showed stable formulation without changes

PHYSICAL STABILITY AND ANTIOXIDANT ACTIVITY ASSAY OF A NANOEMULSION GEL FORMULATION CONTAINING TOCOTRIENOL

Objective: Tocotrienols have an antioxidant potential higher than that of tocopherols. Nanoemulsion gel can deliver tocotrienols into the skin toprevent skin damage caused by free radicals and improve the stability of the dosage form. The present study aimed to determine the physical stabilityand antioxidant activity of a nanoemulsion gel formulation containing tocotrienol.Methods: The tocotrienol nanoemulsion was made using tocotrienols, oleic acid, Tween 80, 96% ethanol, and propylene glycol. The gel base was madeusing a carbomer and triethanolamine. A physical stability test was conducted at three different temperatures, namely, low temperature (4±2°C),room temperature (27±2°C), and high temperature (40±2°C). The antioxidant activity was measured using the 2,2-diphenyl-1-picrylhydrazyl methodfor determining inhibitory concentration (IC50) values.Results: Formula 1 demonstrated the best physical stability, with a pH of 6.2. The droplet size of the tocotrienol nanoemulsion gel was 596 nm, witha zeta potential value of −27.1 nm. The IC50 of the tocotrienol nanoemulsion gel was 6252.14 ppm.Conclusion: The nanoemulsion gel formulation retained antioxidant activity and was physically stable for 8 weeks

ARAH DAN PERKEMBANGAN LIPOSOME DRUGS DELIVERY SYSTEMS

Since the dicovery of liposome or lipid vesicles derived from self limiting enclosed lipid bilayer upon hydration, liposome drug delivery systems have played a significant role in formulation of potent drugs to improve therapeutics. Currently most of these liposome formulation are designed to reduced toxicity and to some extent increase accumulation at the target site(s) in a the number of clinical application. The current pharmaceutical preparations of liposome based therapeutics stem from our understanding of lipid drug interactions and the liposome disposition mechanism including the inhibition of rapid clearance of liposome by controlling size, charge and surface hydration. Key word : liposome, drug delivery systems, active target

FORMULATION AND STABILITY STUDY OF BLACK CUMIN (NIGELLA SATIVA L.) SEED OIL EMULSION USING SUCROSE PALMITATE AS EMULSIFIER

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

STUDIES ON THE FORMULATION, PHYSICAL STABILITY, AND IN VITRO ANTIBACTERIAL ACTIVITY OF TEA TREE OIL (MELALEUCA ALTERNIFOLIA) NANOEMULSION GEL

Objective: This study aimed to formulate tea tree oil into a nanoemulsion gel dosage form and evaluate its physical stability and antibacterial activity.Methods: Nanoemulsion gels were formulated with various concentrations of tea tree oil, namely, 5%, 7%, and 9%, using Tween-80 as a surfactantand propylene glycol as a cosurfactant. The tea tree oil nanoemulsion gels showed a stable physical appearance over 8 weeks of storage at lowtemperature (4±2°C) and room temperature (25±2°C), cycling test, and centrifugation test.Results: The best formula was nanoemulsion gel formulation 1 (F1), which contained 5% tea tree oil, due to its good stability, smaller globule size,and greater viscosity. The results for antibacterial activity, determined by in vitro study, showed that the tea tree oil nanoemulsion gels exhibitedantibacterial activity against Propionibacterium acnes through the formation of an inhibition zone.Conclusion: Higher concentrations of tea tree oil in nanoemulsion gels (5%, 7%, and 9%) showed greater mean inhibition zones (28.33±0.88 mm,30.33±0.33 mm, and 31.67±0.33 mm, respectively)

POTENCY OF Γ-ORYZANOL-RICH BLACK RICE BRAN (ORYZA SATIVA L. INDICA) EXTRACT FOR TYROSINASE INHIBITION

Objective: The objectives of this study were to quantify γ-oryzanol in an ethanolic extract of Oryza sativa L. Indica (black rice) bran and to evaluate its activity as a tyrosinase inhibitor. Methods: Black rice bran was extracted via maceration in 96% ethanol, and the γ-oryzanol concentration in the extract was measured through high-performance liquid chromatography. The applicability of the extract as a skin lightening agent was determined by evaluating its tyrosinase inhibition activity. Results: The dry rice bran contained 118.572 mg/g of γ-oryzanol, and the extract inhibited tyrosinase activity at an IC50 of 74.8%. Conclusion: The black rice bran extract was sufficiently potent for use in skin lightening formulations

HAIR GROWTH ACTIVITY AND SAFETY TEST OF ETHOSOMAL GEL ETHYL ACETATE FRACTION OF NOTHOPANAX LEAVES (NOTHOPANAX SCUTELLARIUM MERR.)

Objective: The aims of this study were to know the hair growth activity from the ethosomal gel of ethyl acetate fraction compared to the nonethosomal gel of ethyl acetate fraction, as well as its ability to penetrate into the skin and its safety from ethosomal gel testing.Methods: The hair growth activity was measured by three parameters: Hair length, hair thickness, and hair weight.Results: The results obtained are shown that the ethosomal gel with concentration 1% has better hair growth activity rather than the ethosomal gel with concentration 0.5% and the nonethosomal gel but it has similarity to the positive control (minoxidil gel with concentration 2%). In vitro penetration test using Franz diffusion cells shown that the ethosomal gel with concentration 1% has cumulative penetration of quercetin higher than nonethosomal gel, which value was 3.3175±0.02 μgcm−2 for the ethosomal gel with concentration 1%; and 2.7663±0.19 μgcm-2 for the nonethosomal gel with flux values for the ethosomal gel with concentration 1% and the nonethosomal gel, respectively, are 0.4147±0.01 μgcm−2h−1 and 0.3458±0.02 μgcm−2h−1.Conclusion: As for the safety test using hen's egg test-chorioallantoic membrane (HET- CAM) safety test) have shown that both concentrations 0.5% and 1% of the ethosomal gel can generate mild irritation for topical application

FORMULATION AND IN VITRO SKIN PENETRATION OF A SOLID LIPID NANOPARTICLE GEL CONTAINING COFFEA ARABICA EXTRACT

Objective: The extract of Coffea contains caffeine that could be used for its anticellulite activity. This study aimed to formulate a Coffea arabicagrounds residue extract into a solid lipid nanoparticles (SLNs) gel dosage form and examine the physical stability and in vitro skin penetration of theformulation.Methods: Coffee grounds residue (CGR) extracts were made into three SLN formulations with different glycerin monostearate (GMS) concentrationsof 1%, 2%, and 3%. The SLN F2 formulation was a gel created by high-pressure homogenization (HPH). The in vitro penetration assessed using Franzdiffusion cells and the physical stability of the SLN extract gels was compared with those of the nonsense extract gel.Results: Formulation F2 with 2% GMS had a mean particle size (PS) of 60.3 nm, a polydispersity index (PDI) of 0.278, and zeta potential of −32±1.40.The PS for the SLN gel after HPH was 159 nm and the PDI was 0.211. Cycling and mechanical tests showed that the SLN gel was physically stable. Thecumulative amount of caffeine penetrated in vitro was 5.55±0.08 for the CGR-SLN gel and 4.18±0.08 for the CGR gel.Conclusions: The amount of caffeine penetrated into rat skin was greater for the CGR-SLN gel than for the CGR gel

FORMULATION AND EVALUATION OF PHYTOSOME LOTION FROM NOTHOPANAX SCUTELLARIUM LEAF EXTRACT FOR HAIR GROWTH

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