Synthesis of tacrolimus nanocrystals and artificial tears surface modification

Abstract

Objective To synthesize a dual-function nanodrug with immunosuppression of tacrolimus (FK506) and lubrication of artificial tear carboxymethylcellulose sodium (CMC), and provide a basis for the clinical treatment of dry eye syndrome. Methods The FK506 nanocrystals were prepared by ultrasonic method, and polyallylamine hydrochloride (PAH) and CMC were deposited alternatively on the surface of FK506 nanocrystals using layer-by-layer (LbL) self-assembly technology to prepare the bifunctional nanodrug. The morphology, particle size, surface charge, and composition of the nanodrug were analyzed. Results The particle size of FK506 nanocrystals was uniform, and the FK506-(PAH/CMC)3 was approximately spherical with uneven surface. Zeta potential detection results showed that the charge changed alternatively with the increasing of layer number. The results of laser scanning confocal imaging and infrared spectroscopy showed that PAH and CMC were successfully modified on the surface of FK506 nanocrystals. Conclusion The prepared FK506-(PAH/CMC)3 nanodrug is expected to provide a scientific basis for the combined treatment of dry eye. Key words: Tacrolimus; Nanocrystals; Artificial tear; Dry eyes