Preparation,formulation optimization and preliminary pharmacodynamic experi-ment of insulin-loaded N-trimethyl chitosan nanoparticles / 药学实践杂志

ABSTRACT

Objective To prepare and optimize insulin-loaded N-trimethyl chitosan nanoparticles via orthogonal design , and preliminarily study the effects on blood glucose level .Methods The insulin-loaded N-trimethyl chitosan nanoparticles (INS-NPs) were prepared by ionic gelation ,and the optimal proportion was obtained with orthogonal design .The nanoparticles were characterized by transmission electron microscopy and zeta/sizer nano analyzer .The entrapment efficiency of insulin-load-ed nanoparticles and the in vitro releasing characteristics were studied by HPLC .A preliminary pharmacodynamic study of the insulin-loaded nanoparticles was also carried out .Results The INS-NPs exhibited narrow distribution .The mean diameter of INS-NPs was (63 .26 ± 1 .88)nm ,while the entrapment efficiency was (37 .92 ± 2 .11)% .After 8 hours of subcutaneous injec-tion of the INS-NPs ,the blood glucose level in diabetic rats decreased to normal level and kept stable .Conclusion The opti-mized insulin-loaded nanoparticles had homogeneous spherical shape ,small size ,and could be a new approach of administration for insulin .