Computational and Experimental Insights in Design and Development of Aceclofenac Co-Crystals

The present study is aimed at the design and development of aceclofenac co-crystals. Co-crystallization is one of the important techniques which helps to enhance the aqueous solubility of drugs by modifying the crystal structure using incorporation of the co-former into the formulation.. In the present study, supramolecular synthon approach and computational grid scan methods were used for the co-former selection. The different co-formers such as oxalic acid (OA), succinic acid (SA), maleic acid (MA), and benzoic acid (BA) were used. Aceclofenac (ACF) co-crystals were prepared by solvent evaporation and dry grinding method. Based on the computational results and experimental saturation solubility studies, maleic acid was considered as the suitable co-former for the preparation. The solid-state characterization showed partial conversion of ACF crystallinity to the amorphization as evident from the decrease in peak intensity and the number of peaks. The co-crystals showed increased aqueous solubility of ACF and higher drug release in basic pH. All the characterization parameters proved the co-crystal formation and the in vitro release studies showed that the solubility enhancement of the ACF by preparing ACF-MA co-crystals. Thus, it can be concluded that co-crystallization is one of the novel method for improving the bioavailability of aceclofenac.