Ibrutinib (ITB) is a specific and novel irreversible inhibitor of Bruton’s tyrosine kinase enzyme, for which reason it exhibits potential chemotherapeutic effects against a few types of B-cell cancers. The… Click to show full abstract
Ibrutinib (ITB) is a specific and novel irreversible inhibitor of Bruton’s tyrosine kinase enzyme, for which reason it exhibits potential chemotherapeutic effects against a few types of B-cell cancers. The objective of this study was to design and characterize the targeted anti-cancer moiety of ITB encapsulated in polymeric nanosponges (IBNS 1-5). The IBNSs were fabricated using the ultrasonication-assisted solvent evaporation technique. They were optimized for robust nanocarriers by varying the ratio of ethylcellulose (50–200 mg), using a constant amount 50 mg of polyvinyl alcohol ((PVA) stabilizer), and drug ITB. Optimized INBS4 containing 50 mg of ITB, PVA, and 162.5 mg of EC was prepared and was studied for anti-cancer potential. Particle analysis and EE and DL calculation of optimized IBNS4 were 640.9 nm, 0.35, −30.2 mV in size, PDI, and ζp, respectively. Physicochemical characterization (FTIR and DSC) studies of IBNS4 showed that the drug was compatible with excipients, and was encapsulated properly within the core of nanosponges. In vitro drug release studies revealed that IBNS4 followed the Higuchi matrix model with anomalous non-Fickian release kinetics. The in vitro diffusion study of I-NS4 exhibited sustained release for 24 h. Enhanced cytotoxicity effects against the MCF-7 observed with the developed NSs (IBNS4) showed 1.96 times more cytotoxic potential compared to the pure drug (ITB).
               
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