Preparation and evaluation of naringenin-loaded sulfobutylether-β-cyclodextrin/chitosan nanoparticles for ocular drug delivery.

The aim of this study was to prepare and characterize the naringenin-loaded sulfobutylether-β-cyclodextrin/chitosan nanoparticles (Nag-CD/CS-NPs) and evaluate their potential for the topical ophthalmic delivery. Naringenin was first complexed with sulfobutylether-β-cyclodextrin (SBE-β-CD), which can significantly enhance the solubility of poorly soluble drugs. Then, nanoparticles were prepared by ionic gelation of chitosan with SBE-β-CD, and their in vitro and vivo properties were investigated, respectively. The resulting nanoparticles showed an average size of 446.4±112.8nm and zeta potential of +22.5±4.91mV with predominant spherical in shape. The FT-IR and DSC confirmed the formation of Nag-CD/CS-NPs. The in vitro release study indicated that Nag-CD/CS-NPs achieved moderate sustained-release effect, and the in vivo study revealed that the prepared nanoparticles was nonirritating to rabbit's eye and had better ability to prolong the residence time than the naringenin suspension, which can significantly increase naringenin bioavailability in the aqueous humor. In conclusion, the developed CD/CS nanoparticles offer a potential alternative for the ocular administration of poorly soluble drugs.