Enhanced Topical Delivery Of Azelaic Acid Through Nanoemulsion Formulation: Optimization, Characterization, And Potential Therapeutic Application For Skin Disorders

Abstract

Rapid connectivity homogenization and ultra-probe sonication were used to manufacture the Azelic acid nanoemulsion. Everything is dissolved in clean water: Azelic acid, polyvinyl alcohol, xanthan gum, castor oil, vitamin E, Transcutol P, and Tween 80. To optimize it, we used Response Surface Methodology and measured a bunch of parameters, like droplet size (nm), surface morphology (FE-SEM, TEM), zeta potential (ZP), differential scanning calorimetry (DSC), polydispersity index (PDI), stability, pH, and viscosity. Both the penetration and retention of the Azelic acid -loaded nanoemulsion into the skin and its release profile were studied in vitro and ex vivo, respectively. The model's quadratic polynomial fitness was confirmed by the optimization analysis of variance (ANOVA), which yielded a significant F-value and a p-value below 0.0500. It was also determined that the lack-of-fit was not statistically significant. Globule size was 200 nm, PDI was 0.2, and entrapment efficacy was 84.99% following optimization of the Azelic acid nanoemulsion. A value of -35.90 mV was recorded for the Zeta Potential (ZP). The absence of chemical interactions was verified by the findings of FTIR, DSC, and XRD investigations, which demonstrated the effective trapping of Azelic acid. Results from scanning electron microscopy and transmission electron microscopy revealed the presence of small spherical particles in the enhanced formulation. Centrifugation, freeze-thaw cycles, and storage at 5°C and 25°C were all successfully completed by the sample in the stability tests. Storage at 40°C for 7 weeks resulted in subtle color shifts, most noticeably during the last week of the study. The results of the rheological tests showed that the revised recipe is elastic and May shear-thin and pseudo-plastic. Over the course of 12 hours, the Azelic acid nanoemulsion released 87.66 % and 97.99 of its active ingredient. A high degree of linearity was demonstrated by the sustained release pattern, which matched a zero-order kinetic model (R2 = 0. 0.9952). After 8 hours, the Azelic acid nanoemulsion had an ex vivo penetration rate of 82.24 %, indicating better skin distribution. Based on the results, Azelic acid nanoemulsion might be useful as a skin condition topical therapy. Nevertheless, further research, including studies conducted in living organisms, is necessary to prove that azelic acid nanoemulsion is both efficient and safe.