Renal Clearable Theranostic Nanoplatforms for Gastrointestinal Stromal Tumors

Abstract Advances in molecular imaging modalities have accelerated the diagnosis and treatment of human diseases. However, tumors less than 1 cm in size still remain difficult to localize by conventional means because of the difficulty in specific targeting/delivery to the tumor site. Furthermore, high nonspecific uptake in the major organs and persistent background retention results in low tumor‐to‐background ratio. The targeting and therapy of gastrointestinal stromal tumors (GIST) using nonsticky and renal clearable theranostic nanoparticles (a.k.a. H‐Dots) are demonstrated. H‐Dots not only target GIST for image‐guided surgery, but also tailor the fate of anticancer drugs such as imatinib (IM) to the tumor site resulting in efficient treatment of unresectable GIST. In addition, H‐Dots can monitor targetability, pharmacokinetics, and drug delivery, while also showing therapeutic efficacy in GIST‐bearing xenograft mice following surgical resection. More importantly, IM loaded H‐Dots exhibit lower uptake into the immune system, improved tumor selectivity, and increased tumor suppression compared to free IM, which accumulates in the spleen/liver. Precisely designed H‐Dots can be used as a promising theranostic nanoplatform that can potentially reduce the side effects of conventional chemotherapies.