Chitosan coated chlorogenic acid and rutincomposite phospholipid liposomes: Preparation, characterizations, permeability and pharmacokinetic

ABSTRACT

In order to research and enhance bioavailability of chlorogenic acid and rutin[CA-R] via the oral route, chitosan coated composite phospholipid liposomes [C-CPLs] were applied to study on preparation, permeability and pharmacokinetic of C-CA-R-CPLs. TheC-CA-R-CPLs were prepared by the method of ethanol injection. The entrapment efficiency [EE], average particle sizes, polymer disperse index [PDI], zeta potential, shape and in vitro drug release were investigated to characterize physicochemical parameters of C-CA-R-CPLs. The penetration properties from C-CA-R-CPLs were studied through Caco-2 cells model and the pharmacokinetics in Sprague-Dawley [SD] rats were evaluated by rat jugular vein intubation tube. The EE of C-CA-R-CPLs of CA and R was 91.3+/-2.13% and 92.6+/-2.44%, particle size of C-CA-R-CPLs was 176.7+/-2.3 nm, PDI was 0.207+/-0.014 and zeta potential of 12.61+/-1.33 mV. CA-RCPLs and C-CA-R-CPLs were spherical or elliptical sphere and the bilayer of the CPL was observed obviously under transmission electron. The C [max], t1/2 and AUC[0-12] h values of CA and R for groups of C-CA-R-CPLs were significantly increased.In conclusion, TheC-CA-R-CPLs as a novel nano-formulation have potential to be used to enhance the oral bioavailability of poorlywater-soluble drugs after oral administration