In order to improve the lymphatic targeting efficiency of anti-cancer agent vincristine sulfate (VCR), the poly (butylcyanoacrylate) nanoparticles (VCR-PBCA-NPs) were prepared by emulsion polymerization and modified superficially with Pluronic F127. These prepared nanoparticles with (F127-VCR-PBCA-NPs) and without surface modification (VCR-PBCA-NPs) were characterized and their lymphatic targeting efficiencies were evaluated in vitro and in vivo. The results showed that VCR was released more sustained from both kinds of VCR-loaded nanoparticles, compared with the VCR solution. The up-taking efficiency of VCR into raji cells was enhanced by F127-VCR-PBCA-NPs, compared with the VCR-PBCA-NPs or VCR solution. Lower clearance (CL) of VCR from the systemic circulation and higher lymphatic targeting efficiency of VCR were observed for F127-VCR-PBCA-NPs than the VCR-PBCA-NPs or VCR solution, and F127-VCR-PBCA-NPs showed greater antitumor efficacy than the VCR-PBCA-NPs or VCR solution in the human Burkitt's lymphoma (raji)-bearing nude mice. These findings suggest that superficially modified nanoscale carriers might be promising vehicles for chemotherapeutic agents in the treatments of metastatic tumors and malignant lymphoma.
Keywords: Lymphatic targeting; Pluronic F127; pharmacokinetics; polybutylcyanoacrylate nanoparticles; tissue distribution; vincristine sulfate.