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

Abstract

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.

Polysaccharide Cryogels Containing β-Cyclodextrin for the Delivery of Cannabidiol

“…The study focused on fabricating cryogels comprising relatively high β-CD fraction because this is a prerequisite for complexation with more CBD molecules per unit mass of the carrier. A previous study revealed that intact cryogel from pure β-CDAc3 cannot be formed [26]. This is attributed to the specific feature of the β-CDAc3 molecule, which is bulky and inflexible.…”

“…These reactive species recombined to form a three-dimensional HEC/β-CD polymer network. Based on our previous experience, 5 min irradiation with UV light was consid-ered an optimal time to complete the crosslinking process [25,26]. Despite their different GF yield, cryogels were intact and preserved the initial shape and size when placed in water.…”

“…The crosslinking agent was synthesized by following a procedure described elsewhere [25,26]. Briefly, β-CD (2.00 g, 1.76 mmol) was dissolved in dimethylformamide (15 mL) in a round-bottomed flask.…”

“…The lower the HEC fraction, the higher the swelling degree of gels (Figure 3B). Firstly, the oligosaccharide β-CD was transformed into a crosslinking agent bearing acrylate groups via reaction with acryloyl chloride in the presence of triethylamine as described elsewhere [25,26]. To obtain a multifunctional crosslinking agent, i.e., several acrylate groups per one β-CD molecule, a given excess of acryloyl chloride was used.…”

Cryogels: recent applications in 3D-bioprinting, injectable cryogels, drug delivery, and wound healing

“…The drug aripiprazole used to treat schizophrenia was recently investigated for delivery using cryogels comprising β-cyclodextrin (β-CD) functionality [ 97 ]. The cryogels were synthesised by photochemical crosslinking of N , N -dimethylacrylamide (DMA) and β-CD triacrylate ( Figure 7 ) and aripiprazole was incorporated through inclusion inside the hydrophobic β - CD domains.…”