A Near-Infrared Fluorescent Macromolecular Dye for Precise Identification of Glioblastoma Boundaries.

Glioblastoma (GBM) is a highly invasive tumor with poorly defined boundaries, often leaving residual tissue after surgery, which contributes to the recurrence and poor prognosis. A critical challenge in GBM treatment is the precise identification of tumor boundaries during surgery to achieve a safe and complete resection. In this study, we present a novel near-infrared fluorescent agent, IR-PEG-cRGD, that is designed to accurately delineate GBM boundaries for surgical navigation of tumor resection.

Multifunctional Zwitterionic N-Oxide Polymers to Overcome Cascade Physiological Barriers for Efficient Anticancer Drug Delivery.

For efficient anticancer drug delivery, cascade physiological barriers must be overcome, which requires the drug delivery vehicles to possess different or even opposite properties at different stages. Poly(tertiary amine-oxide) (PTAO) polymers with the zwitterionic feature have distinct antifouling properties in blood circulation, which can be reduced and protonated in hypoxic tumors to promote cellular internalization. Nevertheless, the effects of various PTAO structures have not been studied systemically and optimized.

X-ray-Triggered Activation of Polyprodrugs for Synergistic Radiochemotherapy.

X-ray-induced photodynamic therapy (XPDT) can penetrate deeply into the tumor tissues to overcome the disadvantage of conventional PDT. However, the therapeutic efficacy of XPDT in cancer therapy is still restricted due to the insufficient reactive oxygen species (ROS) generation at a relatively low irradiation dosage. Herein, we present the tumor pH and ROS-responsive polyprodrug micelles to load the X-ray photosensitizer verteporfin (VP) as an ROS production enhancer.

Photoexcited Hantzsch Ester Anions Enabled C-F Bond Activation and Hydro-Difluoroalkylation of Arylethylenes Through Dual-SET Process.

In this study, we reported a new approach to activate the C-F bond of trifluoromethylarenes to achieve the hydro-difluoroalkylation of arylethylenes using photoexcited Hantzsch esters (HEs) anions. A wide range of α,α-difluoroalkanes was synthesized. Late-stage functionalization of drug molecules and synthesis of bioactive molecule bioisostere were also presented.

Potent Covalent Organic Framework Nanophotosensitizers with Staggered Type I/II Motifs for Photodynamic Immunotherapy of Hypoxic Tumors.

Photodynamic therapy (PDT) using oxygen-dependent type II photosensitizers is frequently limited by the hypoxic microenvironment of solid tumors. Type I photosensitizers show oxygen-independent reactive oxygen species (ROS) generation upon light irradiation but still face the challenges of aggregation-caused quenching (ACQ) and low efficiency to produce ROS. Herein, we first prepare an efficient type I photosensitizer from a perylene derivative via intramolecular donor-acceptor binding and sulfur substitution, which significantly enhance intersystem crossing between singlet and triplet states and electron transfer capability.

Polymersome Membrane Engineering with Active Targeting or Controlled Permeability for Responsive Drug Delivery.

Polymersomes have been extensively investigated for drug delivery as nanocarriers for two decades due to a series of advantages including high stability under physiological conditions, simultaneous encapsulation of hydrophilic and hydrophobic drugs inside inner cavities and membranes, respectively, and facile adjustment of membrane and surface properties, as well as controlled drug release through incorporation of stimuli-responsive components. Despite these features, polymersome nanocarriers frequently suffer from nontargeting delivery and poor membrane permeability. In recent years, polymersomes have been functionalized for more efficient drug delivery.

X-ray-responsive prodrugs and polymeric nanocarriers for multimodal cancer therapy.

Radiotherapy as one of the most important cancer treatment modalities has been widely used in the therapy of various cancers. The clinically used radiation ( X-ray) for radiotherapy has the advantages of precise spatiotemporal controllability and deep tissue penetration. However, traditional radiotherapy is frequently limited by the high side effects and tumor hypoxia.