Abstract: Objective To preliminary study on the physical properties of HN- 1 modified adriamycin (DOX) nanoparticle system HPD and to prove its transplanted oral squamous cell carcinoma (OSCC)- targeting capability. Methods Firstly, the targeting capability of HN-1 for OSCC cells was verified. PEGylated DOX (PD) nanoparticles were synthesized by self-assembly in aqueous media. HN-1 was then chemically grafted onto the surface of PD nanoparticles to form HPD nanoparticles. The HPD nanoparticles were stored in H2O, PBS and PBS containing 10% serum for different time periods. The sizes and distribution diagrams of nanoparticles were evaluated at 1, 3, 5 and 7 days. The serum levels of DOX mediated by HPD nanoparticles were measured. The stability of HPD nanoparticles in vivo was studied. The tumor bearing mice were prepared by inoculating 2.0×106 SCC-25 cells into BALB/C nude mice. Then, mice were randomly divided into four groups (n=2 for each group), normal saline group (control), free DOX group, PD group and HPD nanoparticle group. A dose of 8.0 mg/kg body weight on a DOX basis was injected intravenously though tail vain. The mice were sacrificed at 8 h and 24 h after injection, and the major organs (heart, liver, spleen, lung and kidney) and tumor were excised. The ex vivo DOX fluorescence imaging was obtained using the IVIS. Results HN-1 showed strong capability of targeting OSCC cells. HPD nanoparticles showed an uniform spherical shape and a small size of 150 nm, which also showed strong stability. In the nude mice bearing OSCC tumor, HPD nanoparticles displayed remarkably enhanced tumor- targeting and penetrating efficiency compared with those of PD nanoparticles. Conclusion This study demonstrates that HPD nanoparticles mediated by HN-1 can efficiently target transplanted OSCC, and have potential application for the OSCC-targeting treatment.

Key words: mouth neoplasms, carcinoma, squamous cell, nanoparticles, HN-1, DOX, oral squamous cell carcinoma