Study of the stabilization of zinc phthalocyanine in sol-gel TiO2 for photodynamic therapy applications (original) (raw)
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Investigation of in vitro PDT activities of zinc phthalocyanine immobilised TiO 2 nanoparticles
International Journal of Pharmaceutics, 2017
Phthalocyanines (Pcs) are commonly used as Photosensors (PSs) in Photodynamic Therapy (PDT) applications due to their intense absorption in the far red-near IR spectral region with a high extinction coefficient and high ability for generating singlet oxygen. Pcs targetspecifically tumors, and do not show any considerable toxic effects under the absence of light. In particular, their chemical versatility has allowed the introducion a number of substituent at the periferal or axial positions which provide modulating photophysical properties, increases the solubility of these compounds in organic solvents. Nanoparticles increase the bioavailability, stability, and transport of PSs to target tissue. TiO2 nanoparticles are prefered in these applications because of their non toxic, low cost and high chemical stability properties. In our study, a Zinc Phthalocyanine (ZnPc) was used as a photosensor. The design of ZnPc integrated TiO2 nanoparticles is intended to make PSs a more effective PDT agent. With the aim to examine the nuclear imaging/treatment potentials of ZnPc and TiO2-ZnPc in hepatocellular carcinoma (HepG2), colorectal adenocarcinoma (HT29) tumor and human healthy lung (WI38) cell lines in vitro study ZnPc and TiO2-ZnPc were also labeled with 131 I. It is determined that 131 I-TiO2-ZnPc nanoparticle show a potential as an agent for the imaging/treatment of hepatocellular cancer by in vitro. The toxicity studies revealed that TiO2 nanoparticle decreases the toxicity of ZnPc. In vitro PDT results show that TiO2-ZnO has a potential as a PDT agent in colon tumor treatment. Consequently, synthesized ZnO and TiO2-ZnPc could be promising candidates as theranostic agents.
Chemical biology & drug design, 2017
In recent years, phthalocyanines (Pcs) have been widely used as photosensitizer in photodynamic therapy applications. Because of their strong absorptions in the near-infrared region (640-700 nm). The integration of phthalocyanine derivatives to a nanoparticle is expected to be efficient way to improve the activity of the photosensitizer on the targeted tissue. It is known that the integrated molecules not only show better accumulation on tumor tissue but also reduce toxicity in healthy tissues. In this study, the ZnPc molecule was synthesized and integrated to the TiO2 nanoparticle, to investigate the potential of PDT and its cytotoxicity. Additionally, ZnPc and ZnPc-TiO2 molecules were labelled with 131 I and it was aimed to put forth the nuclear imaging/therapy potentials of 131 I labeled ZnPc/ZnPc-TiO2 by determining in vitro uptakes in mouse mammary carcinoma (EMT6), human cervical adenocarcinoma (HeLa). In result of our study, it was observed that the radiolabeling yields of th...
Chemical Biology & Drug Design, 2017
In recent years, phthalocyanines (Pcs) have been widely used as photosensitizer in photodynamic therapy applications. Because of their strong absorptions in the near-infrared region (640-700 nm). The integration of phthalocyanine derivatives to a nanoparticle is expected to be efficient way to improve the activity of the photosensitizer on the targeted tissue. It is known that the integrated molecules not only show better accumulation on tumor tissue but also reduce toxicity in healthy tissues. In this study, the ZnPc molecule was synthesized and integrated to the TiO 2 nanoparticle, to investigate the potential of PDT and its cytotoxicity. Additionally, ZnPc and ZnPc-TiO 2 molecules were labelled with 131 I and it was aimed to put forth the nuclear imaging/therapy potentials of 131 I labeled ZnPc/ZnPc-TiO 2 by determining in vitro uptakes in mouse mammary carcinoma (EMT6), human cervical adenocarcinoma (HeLa). In result of our study, it was observed that the radiolabeling yields of the synthesized ZnPc and ZnPc-TiO 2 with 131 I were quite high. In vitro uptake studies shown that 131 I-ZnPc-TiO 2 could be a potential agent for nuclear imaging/treatment of breast and cervical cancers. According to PDT results ZnPc-TiO 2 might have as to be a potential PDT agent in the treatment of ovary tumor. ZnPc and ZnPc-TiO 2 might be used as theranostic agents.
Antitumor activity of photodynamic therapy performed with nanospheres containing zinc-phthalocyanine
Journal of Nanobiotechnology, 2013
Background: The increasing incidence of cancer and the search for more effective therapies with minimal collateral effects have prompted studies to find alternative new treatments. Among these, photodynamic therapy (PDT) has been proposed as a very promising new modality in cancer treatment with the lowest rates of side effects, revealing itself to be particularly successful when the photosensitizer is associated with nanoscaled carriers. This study aimed to design and develop a new formulation based on albumin nanospheres containing zinc-phthalocyanine tetrasulfonate (ZnPcS 4 -AN) for use in the PDT protocol and to investigate its antitumor activity in Swiss albino mice using the Ehrlich solid tumor as an experimental model for breast cancer.
Journal of Photochemistry and Photobiology A: Chemistry, 1995
Phthalo-and naphthalocyanines are of interest as sensitizers for the photodynamic therapy of tumors because of their strong absorption in the 680 and 760 nm ranges respectively. Both zinc phthalocyanine and naphthalocyanine tetrasulfonates (ZnPcS4 and ZnNcS4) were aggregated and photochemically inactive in aqueous buffer of pH 7.4, while in 10 mM cetyl pyridinium chloride in buffer they were monomeric and active. Therefore all these studies were carded out using the buffered detergent. The triplet lifetimes of ZnPcS4 and ZnNcS4 under argon were 490 and 110 p.s respectively, with oxygen bimolecular quenching constants of 4.2 × 109 and 2.0 × 10 s M-1 s-l respectively. Triplet decay curves in argon, air and 100% oxygen were first order, suggesting that there was little back reaction of the triplet states with oxygen as has been observed with some naphthalocyanines. The quantum yield of singlet oxygen generation by ZnPcS4 was 0.70 and that for ZnNcS4 was 0.25. Both compounds sensitized the photo-oxidation of furfuryl alcohol, cysteine, histidine, methionine, tryptophan, tyrosine and guanosine; ZnPcS4 was three times more efficient than ZnNcS4. These reactions were 50% inhibited by about 0.5 mM azide, suggesting the involvement of singlet oxygen. Both sensitizers photobleached on illumination, with quantum yields of 1.7 × 10-s for ZnPcS4 and 4.2 × 10-3 for ZnNcS4.
Applied Sciences
Efforts to enhance the utility of photodynamic therapy as a non-invasive method for treating certain cancers have often involved the design of dye sensitizers with increased singlet oxygen efficiency. More recently, however, sensitizers with greater selectivity for tumor cells than surrounding tissue have been targeted. The present study provides an approach to the modification of the known photosensitizer zinc phthalocyanine (ZnPc), to enhance its solubility and delivery to cancer cells. Targeting a photosensitizer to the site of action improves the efficacy of the sensitizer in photodynamic therapy. In this work we used PLGA-b-PEG to encapsulate a new zinc phthalocyanine derivative, 2(3), 9(10), 16(17), 23(24)-tetrakis-(4’-methyl-benzyloxy) phthalocyanine zinc(II) (ZnPcBCH3), to enhance uptake into A549 cells, a human lung cancer cell line. ZnPcBCH3 exhibited the same photochemical properties as the parent compound ZnPc but gave increased solubility in organic solvents, which allo...
Zinc(II) phthalocyanine loaded PLGA nanoparticles for photodynamic therapy use
International Journal of Pharmaceutics, 2006
Sophisticated delivery systems, such as nanoparticles, represent a growing area in biomedical research. Nanoparticles (Np) were prepared using a solvent emulsion evaporation method (SEEM) to load zinc(II) phthalocyanine (ZnPc). Np were obtained using poly (d,l latic-co-glycolic acid) (PLGA). ZnPc is a second generation of photoactive agents used in photodynamic therapy.ZnPc loaded PLGA nanoparticles were prepared by SEEM, characterized and available in cellular culture. The process yield and encapsulation efficiency were 80 and 70%, respectively. The nanoparticles have a mean diameter of 285 nm, a narrow size distribution with polydispersive index of 0.12, smooth surface and spherical shape. ZnPc loaded nanoparticles maintains its photophysical behavior after encapsulation. Photosensitizer release from nanoparticles was sustained with a moderate and burst effect of 15% for 3 days. The photocytotoxicity of ZnPc loaded PLGA Np was evaluated on P388-D1 cells what were incubated with Zn...
Metal phthalocyanine as photosensitizer for photodynamic therapy (PDT)
Science in China Series B: Chemistry, 2001
A series of sulfonated (S) phthalimidomethyl (P) zinc phthalocyanines (Pc) was synthesized in a reaction, in which both kinds of substituents were introduced to ZnPc simultaneously. The products were separated by HPLC. The five different fractions obtained were further purified by a membrane separation method, and then characterized by UV/Vis, IR, element analysis and the abilities to generate singlet oxygen upon irradiation by light as well as a preliminary determination of in vitro antitumor activities. The results show that one of the five separating parts with formula of ZnPcS 2 P 2 exhibited rather good PDT activity. The compound was further characterized by NMR, MS and thermal analysis. Studies on in vivo antitumor activities of ZnPcS 2 P 2 as photosensitizer show that its inhibitory rate was up to 89.8% and 90.8% for S 180 and U 14 solid tumors transplanted in mice respectively when the dosage of drug was 2 mg/kg and the dosage of laser light with 670 nm wavelength was 72 J/cm 2 . Several structural factors influenced on the PDT activities were discussed.
Nowadays the problem of antimicrobial resistance is the most important cause of morbidity and mortality in the treatment of infectious diseases worldwide. Treatment options for antimicrobial-resistant microorganisms are quite limited. Therefore, alternative treatment strategies are needed to control infectious diseases. Antimicrobial photodynamic therapy (aPDT) is one of the new treatment modalities proposed for a wide variety of infections. In the basic principle of aPDT, photosensitizers (PS) produce free radicals by irradiating them with harmless light at the appropriate wavelength, and this causes microorganism cell cytotoxicity. In this study, light emitting diodes (LED) (630–700 nm, 17.4 mW/cm2) were used on Gram-positive Staphylococcus aureus (S. aureus) and Gram-negative Escherichia coli (E. coli) at different light doses under the minimum inhibitory concentration (MIC) values of SubPc and SubPc-integrated TiO2 nanoparticles (SubPc-TiO2) concentration. Both compounds show good phototoxicity toward S. aureus when high light doses (16, 24 J/cm2) were applied. In addition, SubPc-TiO2 were found to be more effective than SubPc in aPDT of S. aureus. In E. coli, the success of aPDT has been shown to be dependent on the increased light dose (20, 30 J/cm2) for both compounds. As a result, the aPDT activity of SubPc-TiO2 is more effective than SubPc in increasing light doses.