Novel ibuprofen hydrogels self-assembled with biocompatible amino acids: mechanistic understanding and performance...

Ibuprofen (IBU), a non-steroidal anti-inflammatory agent, faces restricted application mainly due to its intrinsically poor aqueous solubility and resultant low membrane permeability. With the continuous advancement of gel research, small-molecule hydrogels have garnered increasing attention in the field of pharmaceutical formulations. This study explores the potential of the proposed strategy as a new formulation approach for ameliorating the performance of IBU through self-assembly with biocompatible amino acids, and elucidates the underlying gelation mechanism. The formation of IBU hydrogels was governed by the compatibility of the IBU-amino acid systems, the dynamic equilibrium between dissolution and aggregation, and ionic interactions between components in aqueous surroundings, which were markedly modulated by component molar ratios, volumes of water addition, preparation temperatures, and pH values of aqueous media. Compared to pure IBU, the IBU solubility of the formed IBU-amino acid hydrogels was significantly improved by over 30-fold. Moreover, such IBU hydrogels exhibited excellent drug release performance and superior supersaturation maintenance capacity. Additionally, compared with commercially available IBU hydrogels, the prepared IBU-amino acid hydrogels significantly accelerated IBU membrane permeation, highlighting their great potential for the transdermal delivery system. In summary, this study presents a practical formulation strategy by designing drug-amino acid hydrogels to enhance their release and permeability for performance optimization.