Formulation, Evaluation and Comparison of Beta Cyclodextrins Based Nanosponges of Docosahexaenoic Acid and Aceclofenac for Improved Solubility

ABSTRACTThe poor aqueous solubility of many therapeutic drugs, including aceclofenac anddocosahexaenoic acid (DHA), poses a significant barrier to their clinical application. Thesepharmacologically significant compounds have established therapeutic roles in cardiovascular,neurological, and inflammatory disorders, but their poor solubility and variable oral bioavailabilityrestrict their clinical effectiveness. To address this challenge, β-cyclodextrin (β-CD)-basednanosponges were prepared, characterized, and evaluated for their potential to enhance thesolubility of these poorly soluble drugs. The nanosponges were synthesized using diphenylcarbonate as a crosslinker and loaded with aceclofenac and DHA. Characterization using UV-Visspectrophotometry, Fourier-transform infrared spectroscopy (FTIR), proton nuclear magneticresonance (1H NMR), scanning electron microscopy (SEM), X-ray diffraction (XRD), anddifferential scanning calorimetry (DSC) demonstrated a 5-10 fold solubility increase, high drugentrapment (>75%), and significant amorphization of drugs in nanosponges. The optimizednanosponge formulations exhibited significantly enhanced dissolution rates and improvedsolubility profiles compared to pure drugs and their physical mixtures, without any chemicalincompatibility. These findings indicate that β-CD nanosponges are a promising nanocarriersystem for improving the solubility and dissolution of aceclofenac and DHA, thereby enhancingtheir potential therapeutic efficacy and making them suitable candidates for future pharmaceuticaldevelopment.