Abstract
To compare the differences in antitumor activity between cisplatin (CDDP)-loaded liposomes and nanoparticles in vitro. CDDP-gelatin nanoparticles (GPs-Pt) and CDDP-liposomes with similar size, zeta potential, drug loading efficiency and in vitro release property were prepared. The uptake in A549 cells and elimination kinetics were evaluated and antitumor activity was determined by MTT test. The internalization pathways of nanocarriers were studied with inhibitors. Internalization of two nanocarriers was clathrin and actin dependent. Pt accumulation delivered by GPs-Pt was significantly higher than that of liposomes. However, the results of kinetic analysis showed that liposomes had longer cellular retention, and the MRT and AUC were 3 times and twice of GPs-Pt, respectively. The IC(50) of liposomes was significantly lower than GPs-Pt. The values were 2.94±0.21 and 20.70±1.05 μg/ml, respectively. Nanocarriers with similar pharmaceutical parameters can induce differences in cellular internalization and elimination, which influence the antitumor activity eventually. Compared with gelatin nanoparticle, liposome is preferable for cisplatin delivery.
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