Preparation and Drug Release in vitro of N-Trimethyl Chitosan-coated Sparfloxacin Nanoliposomes in Situ Gels / 中国药师

ABSTRACT

Objective:To prepare N-trimethyl chitosan (TMC)-coated sparfloxacin (SL) nanoliposomes in situ gels(ISG)and in-vestigate the drug release in vitro.Methods:SL liposomes were prepared by a pH gradient method , and then homogenized to nanolipo-somes by high pressure .TMC was used as the coating material to prepare TMC-coated SL nanoliposomes .Poloxamer 407 was used as the gel base, and the optimal amount was selected according to the gelation temperature .TMC-coated SL nanoliposomes ISG was pre-pared using a cold method , and the morphology , size, zeta potential and entrapment efficiency of TMC-coated SL nanoliposomes were studied.A membraneless model was used to study the drug release in vitro, and the result was compared with that of TMC-coated SL nanoliposomes.Results:The optimal amount of poloxamer 407 in the formula was 25%, and the gelation temperature was 23.6℃in the artificial tears and 33 .5℃in the diluted artificial tears .The morphology of TMC-coated SL nanaoliposomes in the ISG was spherical with the mean diameter of (96.8 ±1.5) nm, zeta potential of (46.2 ±1.4) mV and entrapment efficiency of (76.6 ±2.4) %, and the indices had no significant difference when compared with those of TMC-coated SL nanoliposomes .Both the drug release in vitro and gel dissolution profile of TMC-coated SL nanoliposomes ISG exhibited the characteristics of zero-order kinetics, and compared with that of TMC-coated SL nanoliposomes , the sustained release property of the ISG was more significant .Conclusion:TMC-coated SL nanoli-posomes ISG has promising gelation temperature and notable sustained release property .