Cryogel Carriers Comprising β‐Cyclodextrin Moieties for Improved Solubilization and Delivery of Aripiprazole

Aripiprazole is a second‐generation atypical antipsychotic used for the treatment of schizophrenia, bipolar disorder, tic disorders, major depressive disorder, etc. However, aripiprazole is poorly soluble in water and many efforts are focused on developing delivery systems which can improve the solubility and the therapeutic activity of aripiprazole. In this contribution, the fabrication of novel cryogel carriers comprising β‐cyclodextrin (β‐CD) moieties for improved solubilization of aripiprazole is reported. Cryogels are synthesized by photochemical crosslinking of N,N‐dimethylacrylamide (DMA) and β‐CD triacrylate (β‐CD‐Ac3) in frozen aqueous system using H2O2 as initiator. The effect of DMA/β‐CD‐Ac3 mass ratio on the reaction efficiency, physico‐mechanical properties of cryogel, and drug loading efficiency is evaluated. The cryogel carriers are loaded with aripiprazole via procedure favoring inclusion of drug molecules into the hydrophobic cavity of β‐CD. The release of aripiprazole from PDMA/β‐CD carriers at pH 1.2 and 6.8 is studied and compared to the pure PDMA carriers. Sponge‐like cryogels are fabricated by photochemical crosslinking of N,N‐dimethylacrylamide and β‐cyclodextrin triacrylate in frozen aqueous solution using H2O2 as initiator. Aripiprazole is loaded in the cryogels via “host‐guest” complexation between the hydrophobic cavity of β‐CD rings and drug molecules. Such cryogels enhance notably the solubility of aripiprazole in neutral physiological medium and ensure sustained release of the drug.