Characterization and bioactivity of self-assembled anti-angiogenic chondroitin sulfate-ES2-AF nanoparticle conjugate

Xing, Liang; Sun, Feng; Wang, Zhendong; Li, Yan; Yang, Zhifang; Wang, Fengshan; Zhai, Guangxi; Tan, Haining

Blood samples were collected at the predetermined time points from BALB/c mice and processed, the fluorescence intensity was measured, and the concentration of drug in the plasma was calculated. The pharmacokinetic time curves of the mice treated with CS-ES2-AF and ES2-AF are presented in Figure 7 . The plasma concentration of ES2-AF, which had not been modified by glycosylation, was lower than the lowest limit of quantitation after 12 hours of administration, and ES2-AF was not detected in plasma after 24 hours. While the plasma concentration of the glycosylated product CS-ES2-AF was lower than the ES2-AF group at 0.5 hour, the plasma concentrations were higher at the other time points. Table 1 . Compared with the unmodified ES2-AF, the half-life and average residence time of the glycosylationmodified product CS-ES2-AF was significantly prolonged, and the clearance rate was decreased in vivo. It was also found that the peak concentrations of the two drugs were similar. Thus, the plasma concentration of CS-ES2-AF in mice increased; maintenance of a high plasma concentration for a long time is expected to reduce the dosage and frequency of administration in clinical applications.