DoE Based Formulation Development and Characterization of Topical Nanoemulgel of Diacerein: In-Vitro Release and Permeation Studies

Diacerein (DCN) is the class II rhein derivative with low oral bioavailability, although it has good anti-osteoarthritic action. Because of the potential to induce adverse effects when taken orally, the current study focused on producing a topical nanoemulgel formulation based on the 3² Box-Behnken design. Seventeen nanoemulsion (NE) formulations were created according to the design, with varying concentrations of oleic acid (8–12%), tween 80 (10–15%), and propylene glycol (15–25%).

The formulations were examined for the selected dependent variables: particle size and percent drug loading efficiency (% LE). The particle size of the optimized DCN-NE formulation, F8, was 104.3 ± 0.118 nm, and the % LE was 18.5 ± 0.5 %. The F8 was dispersed in 1% carbopol 934P hydrogel and the pH and spreadability were determined to be 6.1 ± 0.3 and 6.2 ± 0.39 g cm/s. The drug content at the top, middle, and bottom was found to be 92.79 ± 1.17, 94.3± 1.2, and 96.54 ± 0.64. Furthermore, at 24 h, the in vitro drug release of DCN from DCN-nanoemulgel (NEG) was 93.61 ± 0.57 %.

The drug release kinetics followed the Higuchi model and non-Fickian pattern, according to mathematical model. DCN-NEG had a cumulative amount per cm² of 12.73 ± 0.23 at 24 h, with a flux of 0.574 ± 0.016. The results of the characterization parameters revealed that the DCN-NEG had a high percentage of drug release and permeability. As a result, it can be used to improve permeation through topical route.

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Nishal, S., Jhawat, V., Phaugat, P. et al. DoE Based Formulation Development and Characterization of Topical Nanoemulgel of Diacerein: In-Vitro Release and Permeation Studies. BioNanoSci. (2022). https://doi.org/10.1007/s12668-022-00980-4