Transcatheter intra‐arterial therapy (TIT) has become valuable in the battle against primary and secondary hepatic malignancies. However, the lack of a mechanism to visualize real‐time drug release and avoid fast metabolic clearance of chemotherap...
Transcatheter intra‐arterial therapy (TIT) has become valuable in the battle against primary and secondary hepatic malignancies. However, the lack of a mechanism to visualize real‐time drug release and avoid fast metabolic clearance of chemotherapeutic agents is the primary barrier to TIT for hepatocellular carcinoma. Here, a specific near‐infrared (NIR) fluorescent prodrug platform, that is, DSPE‐mPEG/DCM‐S‐Pt micelles (DCM‐S‐Pt@PEG), to assist TIT in direct administration to large mammals like rabbits, is presented. DCM‐S‐Pt@PEG consists of a NIR fluorophore for tracing drug release, a nonspecific antitumor drug cisplatin for hepatocellular carcinoma treatment, a glutathione‐activatable disulfide linker, and a DSPE‐mPEG nano‐micelle carrier for controllable drug release. DCM‐S‐Pt@PEG can make the drug accumulation in tumor tissues enhance the therapeutic effect by: i) specific delivery of prodrug to hepatic tumor tissues through the femoral artery by TIT, ii) sustained drug‐release from the biodegradable lipid DSPE‐mPEG micelle to minimize metabolic clearance, and iii) cancer biomarker–activated drug release. It provides a promising strategy to assist TIT in treating unresectable devastating hepatocellular carcinoma administration in the rabbit model, rather than common mouse model.
A specific near‐infrared fluorescent prodrug platform, DSPE‐mPEG/DCM‐S‐Pt, is presented to realize real‐time drug release visualization and avoid fast metabolic clearance of chemotherapeutic agents during transcatheter intraarterial therapy by specific prodrug delivery, sustained drug‐release, and cancer biomarker activated drug‐release.