RESUMO
Objective: To obtain formulations of Celastrol (Cst) nanoemulgel via transdermal route. Celastrol is classified in BCS 4 class as an anti-inflammatory drug. These routes are considered to reduce the risk of Celastrol side effects and have the same characteristics as skin morphology. Methods: Celastrol nanoemulgel was prepared by a high-pressure homogenizer (HPH) technique. To find the optimum nanoemulsion area by using the Chemix 7.00 ternary phase program. Celastrol nanoemulgel was evaluated by measuring the particle size, PDI, morphology, zeta potential, stability tests and in vitro using Franz diffusion cell Results: Results showed the ideal formula based on the ternary phase diagram using chemix 7.00 is oil: smix: water (5:45:50), with particle size 89.9±5 nm, PDI 0.1, and zeta-21 mV. The morphological shape is quite spherical ≤ 100±5 nm. The pH value of this formula is 4.5, which compatible with the pH of the skin. The highest recovery rate of Celastrol and encapsulation efficiency (EE) were formulas 3 μg/ml and 5 μg/ml, with EE 91.70% and 94.54%, respectively. In vitro test results showed that the formula 3 μg/ml and 5 μg/ml give better penetration results than the formula 2.5 μg/ml. Thus, Celastrol nanoemulgel formula has good potential to be developed as a transdermal anti-inflammatory drug. Conclusion: Transdermal nanoemulgel containing Celastrol has been successfully developed with particle size ≤ 200±2 nm.
RESUMO
The aim of the present study was to characterize and evaluate nanoemulgel of snakehead fish powder (SFP) for the poorly water-soluble drug. SFP was formulated into nanoemulsion utilizing the best comparison of surfactant, co-surfactant, and oil. Diverse nanoemulsion components (oil, surfactant, and co-surfactant) were chosen based on solvency and emulsification capacity. SFP 0.1% loaded nanoemulsion which tested by stress-stability testing which carried out for all formulations and those that passed these tests were characterized for droplet size, polydispersity index (PDI), zeta potential, pH, viscosity, and transmittance. After that, nanoemulsion was added with 1.5%, 2.0%, and 2.5% of HPMC in different concentrations and mixed until nanoemulgel form and evaluated for pH, viscosity, spreadability, and extrudability measurement. The results of this research showed that SF nanoemulsion produced clear, stable, and transparent formula having the transmittance value 99.87%. Mean droplet size and zeta potential of the optimized nanoemulsion (NE4) were found to be 98.6±0.93 nm (PDI 0.1±0.20) and -57.5±0.3 MV respectively. Meanwhile, the evaluation results of nanoemulgel (NEG) showed NEG1.5 gave pH 6.0, viscosity 210 cP, spreadability 5.8 g cm/s and extrudability 1.4 g/cm2. Otherwise, NEG2.0 and NEG2.5 had high viscosity and pH generating low spreading on the skin i.e. 3.9 g cm/s and 2.8 g cm/s respectively. The results of the evaluation and preparation stability test showed a good level of stability of NEG1.5 with the viscosity and pH by one way ANOVA which did not change significantly.