Aim: The aim of this study was to prepare biotinylated PAMAM dendrimers loaded with cisplatin and to evaluate the cytotoxicity in ovarian cancer cell lines.
Materials and methods: Biotinylated and unconjugated dendrimer-cisplatin complexes were investigated for encapsulation efficiency, in vitro cytotoxic activity and cellular accumulation of cisplatin in OVCAR-3, SKOV-3, A2780 (wild-type) and CP70 (A2780/CP70, cisplatin-resistant) cells.
Results: Encapsulation efficiency of cisplatin ranged from 5.33% to 21.10%. In vitro cytotoxic activity revealed that IC(50) values of dendrimer-cisplatin complexes were significantly lower than that of free cisplatin in OVCAR-3, SKOV-3 and CP70 cell lines. Cellular uptake data showed highest accumulation of platinum by PAMAMG(4) NH(2) dendrimer complexes of cisplatin in A2780 (19.41±0.85 μg/ml) and CP70 (25.25±1.25 μg/ml) cell lines in comparison with cisplatin uptake of only 1.77±0.351 μg/ml in A2780 and 2.31±0.421 μg/ml in CP70 cells.
Conclusion: In conclusion, biotinylated PAMAM dendrimers may be utilized as potential targeting agents for cisplatin delivery to ovarian cancer.