Journal Article

Design considerations for tumour-targeted nanoparticles

Nasr, Khaled, Choi, Hak Soo, Liu, Fangbing, Misra, Preeti, Liu, Wenhao, Bawendi, Moungi G., Frangioni, John V.

2010

Overview

Inorganic/organic hybrid nanoparticles are potentially useful in biomedicine, but to avoid non-specific background fluorescence and long-term toxicity, they need to be cleared from the body within a reasonable timescale 1 . Previously, we have shown that rigid spherical nanoparticles such as quantum dots can be cleared by the kidneys if they have a hydrodynamic diameter of approximately 5.5 nm and a zwitterionic surface charge 2 . Here, we show that quantum dots functionalized with high-affinity small-molecule ligands that target tumours can also be cleared by the kidneys if their hydrodynamic diameter is less than this value, which sets an upper limit of 5–10 ligands per quantum dot for renal clearance. Animal models of prostate cancer and melanoma show receptor-specific imaging and renal clearance within 4 h post-injection. This study suggests a set of design rules for the clinical translation of targeted nanoparticles that can be eliminated through the kidneys. Nanoparticles functionalized with ligands that target tumours can be cleared from the body through the kidneys if they have a hydrodynamic diameter of less than 5.5 nm.

• Publisher: Nature Publishing Group UK,Nature Publishing Group
• Subject: Animal models / Animals / Antigens, Surface - analysis / Cadmium Compounds - chemistry / Cell Line, Tumor / Chemistry and Materials Science / Design / Diagnostic Imaging - methods / Fluorescence / Glutamate Carboxypeptidase II - analysis / Humans / Injection / Integrin alphaV - analysis / Integrin beta3 - analysis / Kidneys / letter / Male / Materials Science / Melanoma / Melanoma - diagnosis / Mice / Nanoparticles / Nanotechnology / Nanotechnology and Microengineering / Prostate cancer / Prostatic Neoplasms - diagnosis / Quantum Dots / Selenium Compounds - chemistry / Tissue Distribution