Spatiotemporally Coupled Photoactivity of Phthalocyanine–Peptide Conjugate Self‐Assemblies for Adaptive Tumor Theranostics

Abstract

Spatiotemporally coupled tumor phototheranostic platforms offer a flexible and precise system that takes the biological interaction between tumors and photoactive agents into consideration for optimizing treatment, which is highly consistent with precision medicine. However, the fabrication of monocomponent‐based photoactive agents applicable to multifold imaging techniques and multiple therapies in a facile way remains challenging. In this study, we developed simple phthalocyanine–peptide (PF) conjugate‐based monocomponent nanoparticles with spatiotemporally coupled photoactivity for adaptive tumor theranostics. The self‐assembled PF nanoparticles possess well‐defined spherical nanostructures and excellent colloidal stability along with supramolecular photothermal effects. Importantly, the PF nanoparticles showed switchable photoactivity triggered by their interactions with the cell membrane, which enables an adaptive transformation from photothermal therapy (PTT) and photoacoustic imaging (PAI) to photodynamic therapy (PDT) and corresponding fluorescence imaging (FI). Theranostic modalities are integrated in a spatiotemporally coupled manner, providing a facile, biocompatible and effective route for localized tumor phototherapy. This study offers a flexible and versatile strategy to integrate multiple theranostic modalities into a single component so that it can realize its full potential and thereby amplify its therapeutic efficacy, creating promising opportunities for the design of theranostics and further highlighting their clinical prospects to the diagnosis and treatment of cancers.

Biological Evaluation of Naproxen–Dehydrodipeptide Conjugates with Self-Hydrogelation Capacity as Dual LOX/COX Inhibitors

“…The challenge of drug delivery is to transport enough drug molecules to the target sites, whilst minimizing adverse effects in healthy and non-target tissues. Two main approaches in this field have been exploited: (1) the use of a delivery vehicle, such as nanoparticles [1][2][3][4][5][6], and (2) the covalent modification of a drug with a small moiety, such as peptide-drug conjugates [7][8][9]. Peptide-drug conjugates are a conventional class of therapeutic agent that are formed through covalent attachment of specific peptide sequences to established drugs via suitable linker and linkage strategies.…”

Target-driven supramolecular self-assembly for selective amyloid-β photooxygenation against Alzheimer's disease

“…Since the self-assembly is based on the synergy of noncovalent interactions, it is easily subject to environmental variations. 36,[43][44][45] Considering the high binding affinity of Ab with KLVFF, Ab deposition in the brain of AD patients could trigger the disassembly of PKNPs. To test this hypothesis, the morphology change of PKNPs was rst detected by TEM.…”

“…34,49 More importantly, PKNPs permit disassembly upon specic interaction with Ab, leading to smart transformation from photothermal activity to photodynamic activity. 35,36 As a consequence, PKNPs achieve selective photooxygenation of Ab without affecting non-specic proteins (insulin, bovine serum albumin (BSA), and human serum albumin (HSA)). In this way, PKNPs can realize both improved BBB permeability and highly selective photooxygenation of Ab by the transformation of morphology (Scheme 1).…”

Assembled small organic molecules for photodynamic therapy and photothermal therapy

“…In vitro cell experiments show ergosterol/Ce6 nanoparticles have remarkably phototoxicity upon light irradiation. For the in vivo experiments, the anticancer efficiency of ergosterol/Ce6 nanoparticles can be as high as 86.4%, which is much higher than that of ergosterol nanoparticles (51.0%) or Ce6 PDT alone (59.5%). 59 Combined chemotherapy with PDT shows great potential for clinical application.…”