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Synthesis and biological evaluation of phthalocyanine-peptide conjugate for EGFR-targeted photodynamic therapy and bioimaging
摘要： To improve the biocompatibility and tumor selectivity, we employed an epidermal growth factor receptor (EGFR) binding peptide (namely GE11, with a sequence of Tyr-His-Trp-Tyr-Gly-Tyr-Thr-Pro-Gln-Asn-Val-Ile) as a tumor directing vector for the delivery of zinc(II) phthalocyanine for targeted photodynamic therapy and bioimaging. The photophysical properties, cellular uptake, in vitro cytotoxicity, and in vivo biodistribution of this phthalocyanine-peptide conjugate (namely Pc-GE11) have been evaluated. Pc-GE11 exhibited higher cellular uptake on EGFR-overexpressing epidermoid carcinoma A431 cells when compared with that on human breast adenocarcinoma MCF7 cells (low EGFR expression). Moreover, pretreatment of A431 cells with GE11 peptide inhibited the cellular uptake of Pc-GE11 significantly and it exhibited exclusive light-activated cytotoxicity toward A431 cells. Furthermore, Pc-GE11 showed much higher tumor accumulation than the non-targeted control compound containing a random peptide sequence (Tyr-Trp-Gly-Pro-Asn-Ile-His-Tyr-Tyr-Thr-Gln-Val) after intravenous administration in A431-tumor bearing mice, indicating the potential application of this GE11 peptide-conjugated photosensitizer for targeted photodynamic therapy and bioimaging.
关键词： EGFR-targeted,tumor selectivity,phthalocyanine-peptide conjugate,photodynamic therapy,bioimaging
更新于2025-09-23 15:21:21
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Photodynamic therapy of cancer with liposomal photosensitizers
摘要： The photodynamic reaction involves the light-induced generation of an excited state in a photosensitizer molecule (PS), which then results in the formation of reactive oxygen species in the presence of oxygen, or a direct modification of a cellular molecule. Most PSs are porphyrinoids, which are highly lipophilic, and are administered usually in liposomes to facilitate their effective delivery to target cells. The currently available liposomal formulations are Visudyne R(cid:2) and Fospeg R(cid:2). Novel PSs were developed and tested for their photodynamic activity against cancer cells. Several compounds were highly phototoxic to oral cancer cells both in free and liposome-encapsulated form, with nanomolar IC50 values. The lowest IC50s (7–13 nM) were obtained with a PS encapsulated in cationic liposomes.
关键词： photosensitizer,liposome,photodynamic therapy,cytotoxicity,porphyrazine
更新于2025-09-23 15:21:21
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Efficacy of different photoprotection strategies in preventing actinic keratosis new lesions after photodynamic therapy. The ATHENA study: A two-center, randomized, prospective, assessor-blinded pragmatic trial
摘要： Background: Treatment of actinic keratosis (AK) and field cancerization with photodynamic therapy (PDT) is an effective therapeutic approach with a significant reduction in the number of AK lesions (-75% or more) associated with a significant cosmetic improvement of the photodamaged skin. Recently, also the daylight PDT (DL-PDT) has proven to be as effective as the conventional PDT (C-PDT) but with a better tolerability. After C-PDT and DL-PDT it is advised to use photoprotection strategies to improve the clinical evolution and prevent appearance of new AK lesions that usually appear 3-6 months after the last phototherapy session. However, there are no robust clinical data regarding the type of photoprotection to be used (SPF level, duration of treatment ect.) after successful PDT. Study Aim: In the present study (ATHENA trial) we evaluated the efficacy and tolerability of a topical product based on 0.8% piroxicam and 50+ solar filters (ACTX), applied twice a day as sequential therapy after C-PDT) or day-light photodynamic therapy (DL-PDT) on the evolution of AK lesions number compared to the use of very high photoprotection products commonly used in this clinical setting (SPF50+ or SPF100+ associated with photolyase) (Standard Sunscreens: SS group). Subjects and Methods: We conducted a multicenter, randomized, two-arm, prospective controlled, assessor-masked outcome evaluation, parallel group (1:1), pragmatic study of 6 months duration in patients with multiple AK lesions suitable for photodynamic therapy. The objectives of the study were the evaluation of the evolution of the number of AK lesions during the period of treatment/application of the study products, and the Investigator global clinical assessment score (IGA score; 4: marked improvement, 3: good, 2: moderate; 1 no improvement; 0: worsening) after 2, 3 and 6 months after the last PDT session. A total of 68 subjects (50 men, 18 women; mean age 70 years), 34 assigned to treatment with ACTX and 34 to treatment with SS (17 treated with a SPF50+ and 17 with a photolyase-containing SPF100+ products), were enrolled in the study. Results: The number of AK lesions present before C-PDT/DL-PDT was 11.8±5.8 in the ACTX group and 12.4±6.9 in the SS group. In both groups, there was a progressive reduction of AK lesions observed at baseline (-86% and -87% after 2 months and -88% and -83% at month 3 in ACTX and in the SS group, respectively). At month 6, AK mean lesion number was 1.8±1.6 in the ACTX and 3.2±2.3 in the SS group; this difference was statistically significant (p=0.03). The IGA score at the end of the study was 3.2 in ACTX and 2.7 in the SS group (p=0.05). The percentage of subjects with an IGA score of 4/3 (very good or good) was 81% in the ACTX and 55% in the SS group (p=0.06). Conclusion: in subjects with AK treated with C- or DL-PDT, a "medicalized" photoprotection treatment is associated with a favorable clinical outcome with progressive reduction of lesions. In contrast to a very high photoprotection (SPF50+or SPF100+/photolyase), the use of piroxicam 0.8%/SPF 50 + is associated with a significant greater improvement in clinical evolution of AK lesions. (Trial number: ISRCTN16168548).
关键词： Actinic Keratosis,Piroxicam,Cancerization Field,Photodynamic Therapy
更新于2025-09-23 15:21:21
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Indocyanine Green-Conjugated Magnetic Prussian Blue Nanoparticles for Synchronous Photothermal/Photodynamic Tumor Therapy
摘要： Indocyanine green (ICG) is capable of inducing a photothermal effect and the production of cytotoxic reactive oxygen species for cancer therapy. However, the major challenge in applying ICG molecules for antitumor therapy is associated with their instability in aqueous conditions and rapid clearance from blood circulation, which causes insufficient bioavailability at the tumor site. Herein, we conjugated ICG molecules with Prussian blue nanoparticles enclosing a Fe3O4 nanocore, which was facilitated by cationic polyethyleneimine via electrostatic adsorption. The nanocarrier-loaded ICG formed stable aggregates that enhanced cellular uptake and prevented fluorescence quenching. Moreover, the strong superparamagnetism of the Fe3O4 core in the obtained nanocomposites further improved cellular internalization of the drugs guided by a localized magnetic field. The therapeutic efficacy of this nanoplatform was evaluated using tumor models established in nude mice, which demonstrated remarkable tumor ablation in vivo due to strong photothermal/photodynamic effects. This study provides promising evidence that this multifunctional nanoagent might function as an efficient mediator for combining photodynamic and photothermal cancer therapy.
关键词： Indocyanine green,Combination therapy,Photothermal therapy,Photodynamic therapy,Prussian blue nanoparticles
更新于2025-09-23 15:21:01
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Plasmonic nano-dumbbells for enhanced photothermal and photodynamic synergistic damage of cancer cells
摘要： The longitudinal surface plasmon resonance of light-irradiated gold nanorods (Au NRs) is generated to enhance the local electric ?elds of Au NR-based nano-dumbbells (NDs), tailored speci?cally by coating mesoporous silica at two poles of Au NRs and embedding photosensitizer indocyanine green (ICG) into the mesopores. The assembled NDs possess a superior uniformity and water dispersity with a strong plasmonic absorption around 800 nm. Time-domain ?nite-difference calculations indicate that the enhanced local electric ?eld of NDs is predominantly distributed in the dumbbells at two poles of Au NRs, which improves the photonic performance of ICG signi?cantly. Illuminated by an 800 nm laser, the fabricated NDs demonstrate an enhanced combination of photothermal and photodynamic effects in comparison to either Au NRs or ICG alone. Synergistic damaging of photothermal and photodynamic combination to nasopharyngeal carcinoma cells has been corroborated experimentally, thus causing substantial cell death under a lower incident near-infrared laser power. This study concludes that the plasmonic NDs combined synergistically with ef?cient photothermal and photodynamic effects are highly promising in cancer therapy.
关键词： photodynamic therapy,photothermal therapy,cancer cells,gold nanorods,indocyanine green,Plasmonic nano-dumbbells
更新于2025-09-23 15:21:01
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Synergistic interactions of cadmium-free quantum dots embedded in a photosensitised polymer surface: efficient killing of multidrug-resistant strains at low ambient light levels
摘要： Cadmium-free quantum dots (QD) were combined with crystal violet photosensitising dye and incorporated into medical grade polyurethane via a non-covalent dipping process known as ‘swell-encapsulation-shrink’. The antibacterial efficacy of the prepared quantum dot-crystal violet polyurethane substrates (QD + CV PU) was investigated under low power visible light illumination at similar intensities (500 lux) to those present in clinical settings. The antibacterial performance of QD + CV PU was superior to the constituent polymer substrates, eliminating ~99.9% of an environmental P. aeruginosa strain, a clinical P. aeruginosa strain from a cystic fibrosis patient and a clinical E. coli strain. The nature of the reactive oxygen species (ROS) involved in antibacterial activity of the QD + CV PU surface was investigated using ROS inhibitors and time-resolved optical spectroscopy. The photo-physical interaction of the green-emitting QDs with CV lead to a combination of Type I and II electron transfer and energy transfer processes, with the highly potent ROS singlet oxygen playing a dominant role. This study is the first to demonstrate highly efficient synergistic killing of clinical and environmental strains of intrinsically resistant and multi-drug resistant Gram-negative bacteria using light-activated surfaces containing biocompatible cadmium-free QDs and crystal violet dye at ambient light levels.
关键词： photodynamic therapy,antibacterial,reactive oxygen species,surfaces,quantum dots
更新于2025-09-23 15:21:01
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Monitoring of Virulence Factors and Metabolic Activity in Aggregatibacter Actinomycetemcomitans Cells Surviving Antimicrobial Photodynamic Therapy via Nano-Chitosan Encapsulated Indocyanine Green
摘要： Aggregatibacter actinomycetemcomitans is an etiological agent frequently found in both chronic and aggressive periodontitis as well as peri-implantitis. This study assessed the effect of antimicrobial photodynamic therapy (aPDT), as an alternative treatment modality, by nano-chitosan encapsulated indocyanine green (CNPs/ICG), as a photosensitizer, on the virulence features of cell-surviving aPDT against A. actinomycetemcomitans. The cell cytotoxicity effect of CNPs/ICG was evaluated on primary human gingival fibroblast cells. A. actinomycetemcomitans ATCC 33384 photosensitized with CNPs/ICG was irradiated with diode laser at a wavelength of 810 nm for 1 min (31.2 J/cm2), and then bacterial viability measurements were done. The biofilm formation ability, metabolic activity, and antimicrobial susceptibility profiles were assessed for cell-surviving aPDT. The effect of aPDT on the expression of the fieF virulent gene, encoding the ferrous-iron efflux pump, was evaluated by the quantitative real-time PCR. CNPs/ICG-aPDT resulted in a significant reduction of cell viability (91%), biofilm formation capacity (53%), and metabolic activity (48%) of A. actinomycetemcomitans when compared to the control group (P < 0.05). Moreover, fieF gene expression was downregulated by 14.8 folds after the strains were treated with aPDT. The virulence of A. actinomycetemcomitans strain reduced in cells surviving aPDT with CNPs/ICG, indicating the potential implications of aPDT for the treatment of A. actinomycetemcomitans infections in periodontitis and peri-implantitis in vivo.
关键词： peri-implantitis,nano-chitosan,Aggregatibacter actinomycetemcomitans,antimicrobial photodynamic therapy,indocyanine green,periodontitis
更新于2025-09-23 15:21:01
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Arene Ruthenium Metalla-Assemblies with Anthracene Moieties for PDT Applications
摘要： The synthesis and characterization of three metalla-rectangles of the general formula [Ru4(η6-p-cymene)4(μ4-clip)2(μ2-Lanthr)2][CF3SO3]4 (Lanthr: 9,10-bis(3,3’-ethynylpyridyl) anthracene; clip = oxa: oxalato; dobq: 2,5-dioxido-1,4-benzoquinonato; donq: 5,8-dioxido-1, 4-naphthoquinonato) are presented. The molecular structure of the metalla-rectangle [Ru4(η6-p-cymene)4(μ4-oxa)2(μ2-Lanthr)2]4+ has been con?rmed by the single-crystal X-ray structure analysis of [Ru4(η6-p-cymene)4(μ4-oxa)2(μ2-Lanthr)2][CF3SO3]4 · 4 acetone (A2 · 4 acetone), thus showing the anthracene moieties to be available for reaction with oxygen. While the formation of the endoperoxide form of Lanthr was observed in solution upon white light irradiation, the same reaction does not occur when Lanthr is part of the metalla-assemblies.
关键词： photodynamic therapy,metalla-assemblies,singlet oxygen,arene ruthenium,anthracene
更新于2025-09-23 15:21:01
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Photophysical Properties of Nitrated and Halogenated Phosphorus Tritolylcorrole Complexes: Insights from Theory
摘要： The photophysical properties of a series of nitrated and halogenated phosphorus tritolylcorrole complexes were studied in dichloromethane solvent by using the density functional theory. Particular emphasis was given to the absorption spectra, the energy gap between the excited singlet and triplet states, and the magnitude of the spin-orbit couplings for a series of possible intersystem crossing channels between those excited states. The proposed study provides a better description of the photophysical properties of these systems while giving insights into their possible use as photosensitizers in photodynamic therapy.
关键词： photodynamic therapy,phosphorus tritolylcorrole,heavy atom effect,density functional theory,spin-orbit coupling
更新于2025-09-23 15:21:01
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Antimicrobial photodynamic therapy as adjunct to non-surgical periodontal treatment in smokers: a randomized clinical trial
摘要： Objectives This study aims to investigate the additional influence of multiple applications of antimicrobial photodynamic therapy (aPDT) in smokers with chronic periodontitis. Materials and methods Twenty smokers with chronic periodontitis were treated in a split-mouth design study with aPDT adjunct to Scaling and Root Planing (SRP) or SRP. aPDT was performed by using a laser light source with 660 nm wavelength associated with a photosensitizer. The applications were performed in four episodes (at days 0, 2, 7, and 14). All patients were monitored for 90 days. Plaque index, probing depth, clinical attachment level, and bleeding on probing were performed at baseline, 30, and 90 days after the SRP. Gingival crevicular fluid and subgingival plaque samples were collected for immunological and microbiological analysis, respectively. Data obtained were statistically analyzed. Results aPDT as an adjunct to SRP did not demonstrate statistically significant advantages on clinical parameters when compared with SRP alone. No statistic significant differences between groups were observed (p < 0.05). Levels of anti-inflammatory cytokines and bacterial species were comparable in both groups at day 90 after treatment. Conclusion Periodontal treatment with SRP + aPDT in multiples episodes was not able to promote additional clinical, immunological, and microbiological benefits in smokers when compared SRP alone in patients with chronic periodontitis. Clinical relevance Multiple episodes of aPDT adjunctive to non-surgical treatment did not improve significantly the clinical, immunological, and microbiological parameters when compared with SRP alone. More randomized clinical trials are needed to evaluate adjuvant therapies for scaling and root planning in smokers with chronic periodontitis. ClinicalTrials.gov Identifier: NCT03039244
关键词： Photodynamic therapy,Periodontitis,Smoking,Laser
更新于2025-09-23 15:21:01