The Formulation and Evaluation of Deep Eutectic Vehicles for the Topical Delivery of Azelaic Acid for Acne Treatment

Abstract

The current work was aimed at the development of a topical drug delivery system for azelaic acid (AzA) for acne treatment. The systems tested for this purpose were deep eutectic systems (DESs) prepared from choline chloride (CC), malonic acid (MA), and PEG 400. Three CC to MA and eight different MA: CC: PEG400 ratios were tested. The physical appearance of the tested formulations ranged from solid and liquid to semisolid. Only those that showed liquid formulations of suitable viscosity were considered for further investigations. A eutectic mixture made from MA: CC: PEG400 1:1:6 (MCP 116) showed the best characteristics in terms of viscosity, contact angle, spreadability, partition coefficient, and in vitro diffusion. Moreover, the MCP116 showed close rheological properties to the commercially available market lead acne treatment product (Skinorin®). In addition, the formula showed synergistic antibacterial activity between the MA moiety of the DES and the AzA. In vitro diffusion studies using polyamide membranes demonstrated superior diffusion of MCP116 over the pure drug and the commercial product. No signs of skin irritation and edema were observed when MCP116 was applied to rabbit skin. Additionally, the MCP116 was found to be, physically and chemically, highly stable at 4, 25, and 40 °C for a one-month stability study.

Structural insights into novel therapeutic deep eutectic systems with capric acid using 1D, 2D NMR and DSC techniques with superior gut permeability

“…[7][8][9][10] Owing to their versatility, biocompatibility, and sustainability, DESs are increasingly involved in a multitude of pharmaceutical applications. 11,12 Ranging from being solvents for active pharmaceutical ingredients (APIs) to being utilised in drug delivery systems, DESs offered widespread advantages in the pharmaceutical realm. To this end, many recent reports displayed the utility of DESs in enhancing drug solubility of poorly soluble drugs, 10,[13][14][15] permeability, 9 stability, 16 drug delivery, as well as being involved in the synthesis and extraction of active pharmaceutical ingredients.…”