Bladder Cancer Photodynamic Therapeutic Agent with Off‐On Magnetic Resonance Imaging Enhancement

Abstract

Acting as an extracellular matrix protein receptor, V 3 integrin becomes an appealing target for photodynamic therapy of bladder cancer. Here, specific V 3 -integrin-targeting porphyrinato-gadolinium complexes (Gd-PEG-R n ) are demonstrated as off-on theranostic agents, where R n are specific peptides. Among them, Gd-PEG-R 3 shows both impressive phototherapeutic index and robust in vivo magnetic resonance imaging (MRI) signal enhancement. Significant selectivity of Gd-PEG-R 3 is proven by its high V 3 integrin binding affinity in positive bladder cancer cells. All these findings support Gd-PEG-R 3 as a promising bi-functional medical agent with both MRI contrasting ability and photodynamic therapeutic potential for curing bladder cancer.Despite photodynamic therapy (PDT) providing an efficient strategy in medical treatment, [1] scientists are keen to progress on from single-function PDT agents to more elaborate drugs. The term "theranostic" characterizes a class of multifunctional compounds with both therapeutic and diagnostic functions. In particular, the combination of PDT with magnetic resonance imaging (MRI) seems to have promising potential, especially for those working under two-photon excitation. [2,3] With bifunctional drugs attracting more attention, the balance between

Chiroptical Spectroscopic Studies on Lanthanide Complexes with Valinamide Derivatives in Solution

“…Gd complexes are known as an efficient MRI (magnetic resonance imaging) probe agent because of its strong spin‐magnetism with seven f‐electrons in the center metal. Most Gd complexes take the same molecular structures as a series of other lanthanide complexes, and are useful to elucidate the electronic structure localized on the ligand as energy donor species .…”

68Ga-Labeled Magnetic-NIR Persistent Luminescent Hybrid Mesoporous Nanoparticles for Multimodal Imaging-Guided Chemotherapy and Photodynamic Therapy

“…An amount of 100 μL of HMNPs-BSA in PBS solution (pH 7.4, 2 mg mL –1 ) was intravenously administrated into the male LNCaP tumor-bearing mice. MR Images were obtained by a TSE sequences as we previously described …”

“…MR Images were obtained by a TSE sequences as we previously described. 40 Synthesis of 68 Ga-Labeled HMNPs-BSA. For 68 Ga labeling, 250 μL of HMNPs-BSA in 0.1 M HEPES buffer (pH 7.4, 2 mg mL −1 ) was mixed with 500 μL of 68 GaCl 3 (2−3 mCi) and incubated at 70 °C for 30 min on a thermomixer at 500 rpm.…”

Emerging photodynamic/sonodynamic therapies for urological cancers: progress and challenges

“…The relatively hydrophobic R 2 was conjugated with a hydrophilic peptide RrRK, resulting in an amphiphilic R 3 with an improved cell membrane permeability. Based on this earlier report, Xie et al synthesized a porphyrinato-gadolinium complex Gd-PEG-R 3 , introducing PEG linker for better biocompatibility [ 44 ]. The Gd-PEG-R 3 complex, showed high efficiency of PDT to selectively kill BC cells at the cellular level and inhibit bladder tumors in xenograft-bearing nude mice, and enhanced the in vivo “off–on” MRI signal for its low initial T 1 relaxivity increasing over 17 times upon α V β 3 binding.…”

“…Targeted drug delivery to tumor tissue has long been a critical issue in medicine [75], which consists of two parts, one is to increase drug accumulation in tumors and the other is to reduce non-specific distribution of drugs. Modification of PSs (or sonosensitizers) with targeting peptides to target proteins overexpressed on the surface of tumor cells is one of the most straightforward strate- gies [41][42][43][44]. In addition, nanoparticles endowed with the ability to release drugs in response to endogenous or exogenous stimulus through nanobiotechnology have also been employed to increase drug accumulation in tumor tissue [76][77][78][79][80].…”