In-vitro characterization and cytotoxicity study of flutamide loaded cyclodextrin nanosponges

Abstract

Cyclodextrin based nanosponge (CDNS) as a novel delivery system with solubility improvement ability was chosen for flutamide (FLT) encapsulating. This antiandrogen drug is commonly used for prostate cancer, and has low bioavailability through oral usage. The scope of this study was to characterize the best formulation of CDNSs for FLT loading and investigate their cell cytotoxicity. Two types of CDNSs were synthesized, and in-vitro tests such as particle size, zeta potential, loading percent, DSC, FTIR, and release tests were analyzed. Cellular study of the plain and loaded form of carrier was also tested in the PC3 cell line. DLS and TEM confirmed the nano-sized and sponge like structure of CDNSs. FTIR and DSC analysis showed the encapsulation of FLT into CDNSs. CDNS 1:4 showed not only high encapsulation but also a fast dissolution rate of FLT in comparison with CDNS 1:2. CDNS 1:4 with efficient cellular uptake (93.41% after 3 h) had almost no toxicity against the PC3 cell line. Free FLT displayed about two folds more toxic than FLT-CDNSs after 24 and 48 h at 0.1 mg/mL concentrations. Finally, CDNS 1:4 can be introduced as a non-toxic delivery system for FLT with dissolution rate improvement characteristic.