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.
Objective: Celastrol, which is classified as BCS 4, needs to be developed into a nanoemulsion formula for a stable and good formulation. The aim of the study was to determine the in vitro penetration ability and adsorption efficiency (EE) between two different base oils, namely Isopropyl myristate (IPM) and virgin coconut. oil (VCO). Methods: Two celastrol nanoemulsion formulas were prepared by high energy method using High share homogenizer (HSH) at 15,000 rpm for 15 min, using different oil-based components, F1 IPM and F2 VCO. Particle size, polydispersity index (PDI), D90, zeta potential, and morphology of nanoemulsions was evaluated. In vitro studies by Franz diffusion cell test method determined the difference. Results: The results showed that celastrol can be formulated well with a ternary ratio of 5:45:50 for IPM and 20:30:50 for VCO. The absorption efficiency test for celestrol levels was 96.49%±2.72 for IPM and 76.53%±1.19 for VCO. The mean particle size, PDI, and zeta potential were 70.81±0.20 nm, 0.1±0.03, and 50.2±0.60 mV, for VCO and 186.23±3, respectively. 12 nm, 0.2±0.07, and 45.5±1.10 mV for HDI. Spherical morphology<200 nm. Franz diffusion in vitro at 20 and 24 h, celastrol is well penetrated at levels of 2.4 g/ml gram and 2.5 g/ml for HDI and at 2.0 g/ml gram and 2.4 g/ml, respectively. ml/gram for VCO. Conclusion: Celastrol was successfully developed into nanoemulsions using IPM or VCO, particle size<200 nm, and stable spherical shape.
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