Pharmacokinetics and tissue distribution profile of icariin propylene glycol-liposome intraperitoneal injection in mice

Objectives The pharmacokinetics and tissue distribution of icariin propylene glycol‐liposome suspension (ICA‐PG‐liposomes) have been investigated. Methods ICA‐PG‐liposomes or ICA‐PG‐solution were prepared and intraperitoneally injected to mice. Morphology and size distribution of ICA‐PG‐liposomes were observed by transmission electron microscopy (TEM) and laser particle sizer. Plasma and tissues were collected at different times after intraperitoneal injection and icariin concentrations were determined by HPLC. Key findings From TEM, ICA‐PG‐liposomes showed spherical vesicles with a mean particle size of 182.4 nm. The encapsulation efficiency of ICA‐PG‐liposomes reached 92.6%. Pharmacokinetics of ICA‐PG‐liposomes displayed the three open compartments model. ICA‐PG‐liposomes enhanced icariin absorption from the abdominal cavity, prolonged mean retention time (MRT_(0‐t)), increased area under curve (AUC_(0‐t)) and maximum concentration in plasma. Compared with ICA‐PG‐solution, ICA‐PG‐liposomes resulted in larger amounts of icariin being distributed into spleen (60.38% total icariin), liver (16.68%), lung (6.21%), kidney (4.64%), heart (1.43%) and brain (1.83%). AUC_(0‐t) values in most tissues (except lung) of mice administered ICA‐PG‐liposomes were higher than those administered ICA‐PG‐solution, while Clearance in most tissues (except brain and lung) decreased. The MRT_(0‐t) values of ICA‐PG‐liposomes in all tissues and half lives of most tissues (except brain) were prolonged. From Targeted efficiency and relative uptake data, the spleen was the target tissue of the ICA‐PG‐liposomes. Conclusions ICA‐PG‐liposomes changed the pharmacokinetic behaviour and enhanced icariin distribution in tissues. With nanometer size, high encapsulation efficiency and improved pharmacokinetics, ICA‐PG‐liposomes might be developed as promising carriers for icariin injection.