Study on preparation of geniposide chitosan-coated poly lactic acid-glycolic acid nanoparticles and intranasal cavity delivery for brain targeting

AIM To prepare chitosan-coated poly lacticoglycolic acid nanoparticles of geniposide(CS-PLGA-NPs of geniposide) and primarily evaluate the characteristics of nasal delivery for intracerebral targeting.METHODS CS-PLGA-NPs of geniposide was prepared by a double-emulsion evaporation technique and characterized in terms of size,zeta potential,stability and nasal ciliotoxicity.Taking another kind of nanoparticles of poly lactic acid-glycolic acid(PLGA-NPS) as the control,both of the mentioned preparations the nanoparticles were administered intranasally to rats,and then the concentrations in plasma and brain tissues were monitored and compared respectively.RESULTS CS-PLGA-NPs of geniposide was generally spherical in shape with a mean diameter of(204.3 ± s 2.4) nm,a positive surface charge(5.1 ± 0.7) mV and no ciliotoxicity.The intranasal administration of CS-PLGA-NPs of geniposide resulted in a 1.19-1.49 fold increase of AUC0-360 min in brain tissues,then that of PLGA-NPs of geniposide outcoming with the ratios of AUC in brain tissues and that in plasma of CS-PLGA-NPs of geniposide were significant higher than those of PLGA-NPs(P 0.01).CONCLUSION CS-PLGA-NPs possess the potential for promoting the efficiency of direct trans nasal cavity cerebral administration of drug and thus be the indeal vehicle for cerebral targeting treatment.