Preparation And Evaluation Of Melittin Perfluorocarbon Nanocapsules

Objective Prepare melittin perfluorocarbon(PFC) nanocapsules(NPs) and investigate the particle size, Zeta potential, morphology of electron microscopy, entrapment efficiency and stability. SGC-7901 cells were treated with different concentrations of mellitin and melittin perfluorocarbon nanocapsules for various periods, Comparative tumor cell growth inhibition rate by MTT assay.Methods Melittin loaded within PFC NPs were constructed by high pressure homogeneous processing method. The morphology and size of NPs were examined by transmission electron microscopy (TEM) and laser particle size analyzer. Drug entrapment efficiency was assessed by two-colorimetric Coomassie brilliant blue. The stability of melittin perfluorocarbon nanocapsules was investigated by evaluating the change of its average particle size and entrapment efficiency during storage at 4℃for 30 days. SGC-7901 cells were treated with different concentrations (1,2,4,8,16 and 32μg/ml)of mellitin and melittin perfluorocarbon nanocapsules for various periods(24,48 and 72h), the cell proliferation was examined by MTT assay.Results The average particle size of melittin perfluorocarbon nanocapsules is 84.41nm, Polydispersity is 0.115, Zeta potential is -52.1mv. The linear range of melittin was 0.5~25μg/ml(r=0.999 3). Entrapment efficiency of three batches of melittin perfluorocarbon nanocapsules was (86.31±0.76)%with RSD of less than l%. The average particle size and entrapment efficiency of melittin perfluorocarbon nanocapsules is almost no changed during storage at 4℃for 30 days, P>0.05. Melltin inhibited the growth of gastric adenocarcinoma SGC-7901 cells in time- and concentration-dependent manners with IC50 value of 2.424μg/ml (treatment with mellitin after 48h) while melittin perfluorocarbon nanocapsules inhibited the growth of gastric adenocarcinoma SGC-7901 cells with IC50 value of 1.688μg/ml. The difference of inhibition rate between test group and control group was obvious (P<0.05).Conclusions Melittin loaded within PFC NPs were constructed by high pressure homogeneous processing method is feasible. The investigation results of the particle size, morphology of electron microscopy and entrapment efficiency are good. Melittin perfluorocarbon nanocapsules can inhibit proliferation of gastric adenocarcinoma SGC-7901 cells and display effect in a dose-dependent manner. Compared with melittin, the effect of melittin perfluorocarbon nanocapsules have some improvement.