Aptamer Functionalized Cisplatin-Albumin Nanoparticles for Targeted Delivery to Epidermal Growth Factor Receptor Positive Cervical Cancer.

Targeted nanocarriers may offer a new approach to improve the efficacy and tolerability of cisplatin， which are commonly used to treat cancers as a first line chemotherapy for most types of cancer. In the present study， we have developed EGFR-targeted albumin-cisplatin nanoparticles for tumor targeted delivery of cisplatin. The cisplatin NPs were conjugated with EGFR aptamer， which binded to Hela cells specifically， then taken up by tumor cells through receptor mediated endocytosis. The aptamers accumulate in the tumor and interact with the receptor on the surface of Hela cells， successfully blocked EGF-induced EGFR phosphorylation， exerting its targeting and therapy function. Here we demonstrate that the EGFR aptamer functioned NPs enhanced in vitro antitumor effects and markedly improved its tolerability and in vivo efficacy when compared with free cisplatin and other single treatment. Furthermore， the Apt-Pt NPs treatment resulted in reduced systemic and nephrotoxicity， validated by decreased biodistribution of platinum in the major organs as quantified by ICP-MS. The Apt-Pt NPs provides a remarkable improvement in the drug therapeutic efficacy and tolerability in vivo， and will be generalized as a principle for development of novel nanocarriers for targeted tumor therapy.