Asymmetrical Naproxen-Conjugated Dendrimer for Targeted- Drug Delivery to Human Prostatic Adenocarcinoma Cancer Cells

Abstract

Naproxen was directly conjugated to NH 2 -terminated dendrimers by an amide bond and OH-terminated dendrimers by an ester bond. The drug-conjugated polyamidoamine dendrimers showed better cellular uptake than free naproxen. Free naproxen and conjugates in vitro cytotoxicity studies were performed in U251, PC3, K-562, HCT-15, MCF-7 and SKLU-1 cancer cells using different cytotoxicity assays. Naproxen-conjugates of first and second generation showed significant cytotoxic effects in human prostatic adenocarcinoma PC-3 and human mammary adenocarcinoma MCF-7. Moreover, the naproxen-conjugates improved cytotoxicity compared to free naproxen. The increased therapeutic efficacy was observed in specific naproxen conjugates of first generation using low doses, demonstrating that the conjugate was as potent as the antiproliferative agent cisplatin.