Displaying publications 21 - 40 of 60 in total

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  1. Chee CF, Lee HB, Ong HC, Ho AS
    Chem Biodivers, 2005 Dec;2(12):1648-55.
    PMID: 17191961
    In our screening program for new photosensitizers from the Malaysian biodiversity, we found five pheophorbide-related compounds from the leaves and stems of Aglaonema simplex. Detailed spectroscopic analyses showed that compounds 1-3 and 5 are pheophorbide and hydroxy pheophorbide derivatives of chlorophyll a and b. Compound 4, identified as 15(1)-hydroxypurpurin-7-lactone ethyl methyl diester, was isolated for the first time from the Araceae family. An MTT-based short-term survival assay showed that all five compounds exhibit moderate-to-strong photocytotoxic activities towards human leukemia (HL60) and two oral squamous carcinoma cell lines (HSC-2 and HSC-3). Compounds 4 and 5 showed the strongest photocytotoxicities, with IC(50) values of 0.30-0.41 muM (Table 2). Compounds 1-3 with Et chains at C(17(3)) were less photocytotoxic than the parent pheophorbide a (5).
    Matched MeSH terms: Photosensitizing Agents/isolation & purification*; Photosensitizing Agents/pharmacology; Photosensitizing Agents/chemistry
  2. Saberi FNM, Liew YM, Sukumaran P, Ung NM
    Photodiagnosis Photodyn Ther, 2023 Sep;43:103715.
    PMID: 37481146 DOI: 10.1016/j.pdpdt.2023.103715
    Head and neck cancer patients are prone to dental caries after radiotherapy. An ex-vivo study was conducted to assess the feasibility of optical coherence tomography (OCT) to detect tooth demineralization due to caries in irradiated teeth. Thirty-nine human molar teeth were subjected to caries lesion induction through irradiation (Group 1), pH cycling (Group 2-1), and both (Group 2-2). The OCT signal attenuation coefficient, µR was assessed and validated against microhardness test and scanning electron microscope (SEM). The µR for Group 1 increased from 10 Gy to 40 Gy, and subsequently decreased after irradiated to 50 Gy and 60 Gy due to damaged enamel microstructure. In Group 2-1, the µR decreased with duration of pH cycling from day 1 to day 14 due to the increase of porosity in enamel layer. However, the µR showed decreasing trend from day 14 to day 28 of pH cycling, resulted from mineral deposition in the enamel layer. Although no significant difference was found in the µR between Group 2-1 and 2-2, SEM of Group 2-2 demonstrated visually higher porosity and larger gaps between microstructures. Irradiation may accelerate caries damage to tooth microstructure by increasing its porosity and brittleness, but larger sample size may be needed to further prove the effect. OCT could potentially be used for early detection of tooth demineralization in vivo based on the measurable µR changes for all groups which are shown negatively correlated with microhardness value (p 
    Matched MeSH terms: Photosensitizing Agents
  3. Samat N, Tan PJ, Shaari K, Abas F, Lee HB
    Anal Chem, 2014 Feb 4;86(3):1324-31.
    PMID: 24405504 DOI: 10.1021/ac403709a
    Photodynamic therapy (PDT) is an alternative treatment for cancer that involves administration of a photosensitive drug or photosensitizer that localizes at the tumor tissue followed by in situ excitation at an appropriate wavelength of light. Tumour tissues are then killed by cytotoxic reactive oxygen species generated by the photosensitizer. Targeted excitation and photokilling of affected tissues is achieved through focal light irradiation, thereby minimizing systemic side effects to the normal healthy tissues. Currently, there are only a small number of photosensitizers that are in the clinic and many of these share the same structural core based on cyclic tetrapyrroles. This paper describes how metabolic tools are utilized to prioritize natural extracts to search for structurally new photosensitizers from Malaysian biodiversity. As proof of concept, we analyzed 278 photocytotoxic extracts using a hyphenated technique of liquid chromatography-mass spectrometry coupled with principal component analysis (LC-MS-PCA) and prioritized 27 extracts that potentially contained new photosensitizers for chemical dereplication using an in-house UPLC-PDA-MS-Photocytotoxic assay platform. This led to the identification of 2 new photosensitizers with cyclic tetrapyrrolic structures, thereby demonstrating the feasibility of the metabolic approach.
    Matched MeSH terms: Photosensitizing Agents/analysis*; Photosensitizing Agents/isolation & purification; Photosensitizing Agents/therapeutic use
  4. Greco G, Di Piazza S, Chan J, Zotti M, Hanna R, Gheno E, et al.
    Photodiagnosis Photodyn Ther, 2020 Mar;29:101575.
    PMID: 31614222 DOI: 10.1016/j.pdpdt.2019.10.010
    BACKGROUND: A large number of systemic diseases can be linked to oral candida pathogenicity. The global trend of invasive candidiasis has increased progressively and is often accentuated by increasing Candida albicans resistance to the most common antifungal medications. Photodynamic therapy (PDT) is a promising therapeutic approach for oral microbial infections. A new formulation of 5-aminolevulinic acid (5%ALA) in a thermosetting gel (t) (5%ALA-PTt) was patented and recently has become available on the market. However, its antimicrobial properties, whether mediated or not by PDT, are not yet known. In this work we characterised them.

    METHODS: We isolated a strain of C. albicans from plaques on the oral mucus membrane of an infected patient. Colonies of this strain were exposed for 1 24 h, to 5%ALA-PTt, 5%ALA-PTt buffered to pH 6.5 (the pH of the oral mucosa) (5%ALA-PTtb) or not exposed (control). The 1 h-exposed samples were also irradiated at a wavelength of 630 nm with 0.14 watts (W) and 0.37 W/cm2 for 7 min at a distance of <1 mm.

    RESULTS AND CONCLUSION: The 5% ALA-PTt preparation was shown to be effective in reducing the growth of biofilm and inoculum of C. albicans. This effect seems to be linked to the intrinsic characteristics of 5%ALA-TPt, such acidic pH and the induction of free radical production. This outcome was significantly enhanced by the effect of PDT at relatively short incubation and irradiation times, which resulted in growth inhibition of both treated biofilm and inoculum by ∼80% and ∼95%, respectively.

    Matched MeSH terms: Photosensitizing Agents/administration & dosage; Photosensitizing Agents/pharmacology*
  5. Khaniabadi PM, Shahbazi-Gahrouei D, Aziz AA, Dheyab MA, Khaniabadi BM, Mehrdel B, et al.
    Photodiagnosis Photodyn Ther, 2020 Sep;31:101896.
    PMID: 32585402 DOI: 10.1016/j.pdpdt.2020.101896
    BACKGROUND: Theranostic agents can combine photosensitizers and contrast agents into a single unit for photothermal therapy (PTT) and magnetic resonance imaging (MRI). The possibility of treating and diagnosing malignant cancers without any ionizing radiation could become an option. This study investigates the theranostic potential of Fe3O4 nanoparticles (IONs) for the diagnosis and treatment of cancer by developing a single integrated nanoprobe.

    METHODS: Oleylamin-coated IONs (ION-Ol) were synthesized and surface of the IONs was modified using protoporphyrin (PP) and trastuzumab (TZ) to develop the TZ-conjugated SPION-porphyrin [ION-PP-TZ]. The structure, morphology, size, and cytotoxicity of all samples were investigated using Fourier-transform infrared spectroscopy (FT-IR), Transmission electron microscopy (TEM), X-ray powder diffraction (XRD), WST-1 assay, respectively. In addition to MRI and in vitro laser irradiation (808 nm, 200 mW) to determine the r2 values and photothermal ablation.

    RESULTS: The sizes of monodispersed nanoparticles were measured in rang 5.74-7.17 nm. No cytotoxicity was observed after incubating MCF 7 cells under various Fe concentrations of nanoparticles and theranostic agents. The transverse relaxation time of the protoporphyrin conjugated to IONs (52.32 mM-1s-1) exceeded that of ION-Ol and TZ-conjugated ION-PP. In addition, the in vitro photothermal ablation of ION-PP-TZ revealed a 74 % MCF 7 cell reduction after 10 min of at the highest Fe concentration (1.00 mg Fe/mL).

    CONCLUSIONS: In summary, the water-soluble ION-PP-TZ is a promising bimodal agent for the diagnosis and treatment of human epidermal growth factor receptor 2-positive breast cancer cells using a T2 MRI contrast agent and photothermal therapy.

    Matched MeSH terms: Photosensitizing Agents/pharmacology; Photosensitizing Agents/therapeutic use
  6. Chin Y, Lim SH, Zorlu Y, Ahsen V, Kiew LV, Chung LY, et al.
    PLoS One, 2014;9(5):e97894.
    PMID: 24840576 DOI: 10.1371/journal.pone.0097894
    Phthalocyanines are excellent photosensitizers for photodynamic therapy as they have strong absorbance in the near infra-red region which is most relevant for in vivo activation in deeper tissular regions. However, most phthalocyanines present two major challenges, ie, a strong tendency to aggregate and low water-solubility, limiting their effective usage clinically. In the present study, we evaluated the potential enhancement capability of glycerol substitution on the photodynamic properties of zinc (II) phthalocyanines (ZnPc). Three glycerol substituted ZnPc, 1-3, (tetra peripherally, tetra non-peripherally and mono iodinated tri non-peripherally respectively) were evaluated in terms of their spectroscopic properties, rate of singlet oxygen generation, partition coefficient (log P), intracellular uptake, photo-induced cytotoxicity and vascular occlusion efficiency. Tetrasulfonated ZnPc (ZnPcS4) was included as a reference compound. Here, we showed that 1-3 exhibited 10-100 nm red-shifted absorption peaks with higher molar absorptivity, and at least two-fold greater singlet oxygen generation rates compared to ZnPcS4. Meanwhile, phthalocyanines 1 and 2 showed more hydrophilic log P values than 3 consistent with the number of glycerol attachments but 3 was most readily taken up by cells compared to the rest. Both phthalocyanines 2 and 3 exhibited potent phototoxicity against MCF-7, HCT-116 and HSC-2 cancer cell-lines with IC50 ranging 2.8-3.2 µM and 0.04-0.06 µM respectively, while 1 and ZnPcS4 (up to 100 µM) failed to yield determinable IC50 values. In terms of vascular occlusion efficiency, phthalocyanine 3 showed better effects than 2 by causing total occlusion of vessels with diameter <70 µm of the chorioallantoic membrane. Meanwhile, no detectable vascular occlusion was observed for ZnPcS4 with treatment under similar experimental conditions. These findings provide evidence that glycerol substitution, in particular in structures 2 and 3, is able to improve the photodynamic properties of ZnPc.
    Matched MeSH terms: Photosensitizing Agents/pharmacokinetics; Photosensitizing Agents/chemistry*
  7. Zeeshan T, Qamar Z, Abdul NS, Soman C, Bamousa B, Marrapodi MM, et al.
    Technol Health Care, 2024;32(4):2685-2696.
    PMID: 38339947 DOI: 10.3233/THC-231814
    BACKGROUND: Commercially available oral rinses contain active ingredients with concentration that is claimed by manufacturers to be effective as antiplaque agent. To date there has been no mention of the effect of oral rinse on the adherence of early plaque colonizers in plaque formation and the concentration to be used before/after meals.

    OBJECTIVE: The chief aim of the study was to evaluate microbial retention on the salivary pellicle on treatment with oral rinses (CHX & EO)/PS (mimicking after meals use of mouth wash/PS).

    METHODS: Noordini's Artifical Mouth model was used for developing the single species biofilm with early microbial colonizers of oral biofilm (A. viscosus, Strep. mitis and Strep. sanguinis respectively). The microbial retention on use of oral rinses comprising of CHX and EO as an active ingredients respectively was compared with Curcumin PS. For evaluating the microbial retention, the pellicle with microbial inoculation was developed on the glass beads in the mouth model. Subsequently the respective single specie biofilm was exposed to the mouth wash and PS after inoculation. It mimicked as use of mouth wash/PS after meals. The bacterial count in the dental biofilm was evaluated on serial dilution (CFU/ml). Sterile deionized water was used as a negative control. For qualitative analysis, Scanning electron microscope (SEM) was used to evaluate the microbial count.

    RESULTS: From the data it was observed that for the treatment of single species experimental biofilm with commercially available mouth rinses (CHX & EO) and PS (curcumin), there was significant retention for S.mitis, S.sanguinis and A.viscosus. There was no significant difference observed between PS and CHX treated single species biofilm. Whereas a significant difference was observed between EO treated biofilms and CHX/PS treated biofilms (p⩽ 0.05).

    CONCLUSION: It can be concluded from the results that curcumin PS and CHX should not be used after meals whereas EO containing mouth rinse can be used to maintain the oral mocroflora.

    Matched MeSH terms: Photosensitizing Agents/administration & dosage; Photosensitizing Agents/pharmacology
  8. Voon SH, Kiew LV, Lee HB, Lim SH, Noordin MI, Kamkaew A, et al.
    Small, 2014 Dec 29;10(24):4993-5013.
    PMID: 25164105 DOI: 10.1002/smll.201401416
    Animal models, particularly rodents, are major translational models for evaluating novel anticancer therapeutics. In this review, different types of nanostructure-based photosensitizers that have advanced into the in vivo evaluation stage for the photodynamic therapy (PDT) of cancer are described. This article focuses on the in vivo efficacies of the nanostructures as delivery agents and as energy transducers for photosensitizers in animal models. These materials are useful in overcoming solubility issues, lack of tumor specificity, and access to tumors deep in healthy tissue. At the end of this article, the opportunities made possible by these multiplexed nanostructure-based systems are summarized, as well as the considerable challenges associated with obtaining regulatory approval for such materials. The following questions are also addressed: (1) Is there a pressing demand for more nanoparticle materials? (2) What is the prognosis for regulatory approval of nanoparticles to be used in the clinic?
    Matched MeSH terms: Photosensitizing Agents/therapeutic use*; Photosensitizing Agents/chemistry
  9. Tan PJ, Appleton DR, Mustafa MR, Lee HB
    Phytochem Anal, 2012 Jan-Feb;23(1):52-9.
    PMID: 21692117 DOI: 10.1002/pca.1324
    Photodynamic therapy is a treatment modality that involves site-directed generation of cytotoxic reactive oxygen species by light-activated photosensitisers.
    Matched MeSH terms: Photosensitizing Agents/isolation & purification*; Photosensitizing Agents/pharmacology; Photosensitizing Agents/radiation effects; Photosensitizing Agents/chemistry
  10. Liew HS, Mai CW, Zulkefeli M, Madheswaran T, Kiew LV, Delsuc N, et al.
    Molecules, 2020 Sep 12;25(18).
    PMID: 32932573 DOI: 10.3390/molecules25184176
    Photodynamic therapy (PDT) is emerging as a significant complementary or alternative approach for cancer treatment. PDT drugs act as photosensitisers, which upon using appropriate wavelength light and in the presence of molecular oxygen, can lead to cell death. Herein, we reviewed the general characteristics of the different generation of photosensitisers. We also outlined the emergence of rhenium (Re) and more specifically, Re(I) tricarbonyl complexes as a new generation of metal-based photosensitisers for photodynamic therapy that are of great interest in multidisciplinary research. The photophysical properties and structures of Re(I) complexes discussed in this review are summarised to determine basic features and similarities among the structures that are important for their phototoxic activity and future investigations. We further examined the in vitro and in vivo efficacies of the Re(I) complexes that have been synthesised for anticancer purposes. We also discussed Re(I) complexes in conjunction with the advancement of two-photon PDT, drug combination study, nanomedicine, and photothermal therapy to overcome the limitation of such complexes, which generally absorb short wavelengths.
    Matched MeSH terms: Photosensitizing Agents/pharmacology*; Photosensitizing Agents/chemistry
  11. Lai D, Zhou A, Tan BK, Tang Y, Sarah Hamzah S, Zhang Z, et al.
    Food Chem, 2021 Nov 01;361:130117.
    PMID: 34058659 DOI: 10.1016/j.foodchem.2021.130117
    To overcome the poor water solubility of curcumin, a curcumin-β-cyclodextrin (Cur-β-CD) complex was prepared as a novel photosensitizer. Fourier-transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), and X-ray diffraction (XRD) were used to verify the formation of Cur-β-CD. Furthermore, the ROS generation capacity and photodynamic bactericidal effect were measured to confirm this Cur-β-CD complex kept photodynamic activity of curcumin. The result showed Cur-β-CD could effectively generate ROS upon blue-light irradiation. The plate count assay demonstrated Cur-β-CD complex possess desirable photodynamic antibacterial effect against food-borne pathogens including Staphylococcus aureus, Listeria monocytogenes and Escherichia coli. The cell morphology determined by scanning electron microscope (SEM) and transmission electron microscope (TEM) showed Cur-β-CD could cause cell deformation, surface collapse and cell structure damage of the bacteria, resulting in the leakage of cytoplasmic; while agarose gel electrophoresis and SDS-PAGE further illustrated the inactivation mechanisms by Cur-β-CD involve bacterial DNA damage and protein degradation.
    Matched MeSH terms: Photosensitizing Agents/pharmacology; Photosensitizing Agents/chemistry*
  12. Jong WW, Tan PJ, Kamarulzaman FA, Mejin M, Lim D, Ang I, et al.
    Chem Biodivers, 2013 Aug;10(8):1475-86.
    PMID: 23939795 DOI: 10.1002/cbdv.201200303
    Photodynamic therapy (PDT) is a medical treatment that involves the irradiation of an administered photosensitizing drug with light of a particular wavelength to activate the photosensitizer to kill abnormal cells. To date, only a small number of photosensitizers have been clinically approved for PDT, and researchers continue to look for new molecules that have more desirable properties for clinical applications. Natural products have long been important sources of pharmaceuticals, and there is a great potential for discovery of novel chemotypes from under-explored biodiversities in the world. The objective of this study is to mine the terrestrial plants in Sarawak, Borneo Island, for new photosensitizers for PDT. In a screening program from 2004 to 2008, we prepared and studied 2,400 extracts from 888 plants for their photosensitizing activities. This report details the bioprospecting process, preparation and testing of extracts, analysis of the active samples, fractionation of four samples, and isolation and characterization of photosensitizers.
    Matched MeSH terms: Photosensitizing Agents/pharmacology; Photosensitizing Agents/chemistry*
  13. Akram Z, Al-Shareef SA, Daood U, Asiri FY, Shah AH, AlQahtani MA, et al.
    Photomed Laser Surg, 2016 Apr;34(4):137-49.
    PMID: 26982216 DOI: 10.1089/pho.2015.4076
    The aim of this study was to assess the bactericidal efficacy of antimicrobial photodynamic dynamic therapy (aPDT) as an adjunct to scaling and root planing (SRP) against periodontal pathogens.
    Matched MeSH terms: Photosensitizing Agents/administration & dosage*; Photosensitizing Agents/therapeutic use
  14. Siriviriyanun A, Tsai YJ, Voon SH, Kiew SF, Imae T, Kiew LV, et al.
    Mater Sci Eng C Mater Biol Appl, 2018 Aug 01;89:307-315.
    PMID: 29752102 DOI: 10.1016/j.msec.2018.04.020
    In this study, nanohybrid materials consisting of graphene oxide (GO), β‑cyclodextrin (CD) and poly(amido amine) dendrimer (DEN) were successfully prepared by covalent bonding. GO-CD and GO-CD-DEN were found to be potential nanocarriers for anticancer drugs including chemotherapeutics (doxorubicin (DOX), camptothecin (CPT)) and photosensitizer (protoporphyrin IX (PpIX)). GO-CD possessed 1.2 times higher DOX-loading capacity than GO due to inclusion of additional DOX to the CD. The drug loading on GO-CD-DEN increased in the order: DOX 
    Matched MeSH terms: Photosensitizing Agents/metabolism; Photosensitizing Agents/pharmacology; Photosensitizing Agents/chemistry*
  15. Dheyab MA, Aziz AA, Khaniabadi PM, Jameel MS
    Photodiagnosis Photodyn Ther, 2021 Mar;33:102177.
    PMID: 33429101 DOI: 10.1016/j.pdpdt.2021.102177
    The production of nanomaterials integrating diagnostic and therapeutic roles within one nanoplatform is important for medical applications. Such theranostics nanoplatforms could provide information on imaging, accurate diagnosis and, at the same time, could eradicate cancer cells. Fe3O4@Au core@shell nanoparticles (Fe3O4@AuNPs) have gained broad attention due to their unique innovations in magnetic resonance imaging (MRI) and photothermal therapy (PTT). Seed-mediated growth procedures were used to produce the Fe3O4@AuNPs. In these processes, complicated surface modifications, resulted in unsatisfactory properties. This work used the ability of the sonochemical approach to synthesize highly efficient theranostics agent Fe3O4@AuNPs with a size of approximately 22 nm in 5 min. The inner core of Fe3O4 acts as an MRI agent, whereas the photothermal effect stands accomplished by near-infrared absorption of the gold shell (Au shell), which results in the eradication of cancer cells. We have shown that Fe3O4@AuNPs have great biocompatibility and no major cytotoxicity has been identified. Relaxivity value (r2) of synthesized Fe3O4@Au NPs, measured at 233 mM-1s-1, is significantly higher than those reported previously. The as-synthesized NPs have shown substantial photothermal ablation ability on MCF-7 in vitro under near-infrared laser irradiation. Consequently, Fe3O4@AuNPs synthesized in this study have great potential as an ideal candidate for MR imaging and PTT.
    Matched MeSH terms: Photosensitizing Agents
  16. Kamarulzaman FA, Shaari K, Ho AS, Lajis NH, Teo SH, Lee HB
    Chem Biodivers, 2011 Mar;8(3):494-502.
    PMID: 21404433 DOI: 10.1002/cbdv.201000341
    In our screening program for new photosensitizers from Malaysian biodiversity for photodynamic therapy (PDT) of cancer, MeOH extracts of ten terrestrial plants from Cameron Highlands in Pahang, Peninsular Malaysia, were tested. In a short-term 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay, 20 μg/ml each of these extracts were incubated in a pro-myelocytic leukemia cell-line, HL60, with or without irradiation with 9.6 J/cm(2) of a broad spectrum light. Three samples, Labisia longistyla, Dichroa febrifuga, and Piper penangense, were photocytotoxic by having at least twofold lower cell viability when irradiated compared to the unirradiated assay. The extract of the leaves of Piper penangense, a shrub belonging to the family Piperaceae and widely distributed in the tropical and subtropical regions in the world, was subsequently subjected to bioassay-guided fractionation using standard chromatography methods. Eight derivatives of pheophorbide-a and -b were identified from the fractions that exhibited strong photocytotoxicity. By spectroscopic analysis, these compounds were identified as pheophorbide-a methyl ester (1), (R,S)-13(2) -hydroxypheophorbide-a methyl ester (2 and 3), pheophorbide-b methyl ester (4), 13(2) -hydroxypheophorbide-b methyl ester (5), 15(2) -hydroxylactone pheophorbide-a methyl ester (6), 15(2) -methoxylactone pheophorbide-a methyl ester (7), 15(2) -methoxylactone pheophorbide-b methyl ester (8).
    Matched MeSH terms: Photosensitizing Agents/isolation & purification*; Photosensitizing Agents/pharmacology; Photosensitizing Agents/chemistry
  17. Abu N, Ali NM, Ho WY, Yeap SK, Aziz MY, Alitheen NB
    Anticancer Agents Med Chem, 2014 Jun;14(5):750-5.
    PMID: 24164045
    The Noni fruit, or scientifically known as Morinda citrifolia can be found in various parts of the world, especially in the pacific region. It is a small evergreen bushy-like tree originated from the Rubiaceae family. The plant has been used by polynesians as a medicinal herb for more than 2000 years. A substantial amount of phytochemicals can be found in the roots of this plant. Among all, damnacanthal has been found to be the most interesting, versatile and potent compound. Damnacanthal or chemically known as,3- hydroxy-1-methoxyanthraquinone-2-caboxaldehyde (C16H10O5), appears as pale yellow crystals with a melting point of 210-211 °C. This compound is of particular interest due to its striking pharmacological properties. Damnacanthal was shown to inhibit the oncogene Ras, p56lck tyrosine kinase, NF-KB pathway and induce apoptosis in vitro. This review aims to discuss the biological properties of damnacanthal, specifically on its anti-cancer activity that has been reported.
    Matched MeSH terms: Photosensitizing Agents/pharmacology; Photosensitizing Agents/therapeutic use; Photosensitizing Agents/chemistry
  18. Qidwai A, Khan S, Md S, Fazil M, Baboota S, Narang JK, et al.
    Drug Deliv, 2016 May;23(4):1476-85.
    PMID: 26978275 DOI: 10.3109/10717544.2016.1165310
    Topical photodynamic therapy (PDT) is a promising alternative for malignant skin diseases such as basal-cell carcinoma (BCC), due to its simplicity, enhanced patient compliance, and localization of the residual photosensitivity to the site of application. However, insufficient photosensitizer penetration into the skin is the major issue of concern with topical PDT. Therefore, the aim of the present study was to enable penetration of photosensitizer to the different strata of the skin using a lipid nanocarrier system. We have attempted to develop a nanostructured lipid carrier (NLC) for the topical delivery of second-generation photosensitizer, 5-amino levulinic acid (5-ALA), whose hydrophilicity and charge characteristic limit its percutaneous absorption. The microemulsion technique was used for preparing 5-ALA-loaded NLC. The mean particle size, polydispersity index, and entrapment efficiency of the optimized NLC of 5-ALA were found to be 185.2 ± 1.20, 0.156 ± 0.02, and 76.8 ± 2.58%, respectively. The results of in vitro release and in vitro skin permeation studies showed controlled drug release and enhanced penetration into the skin, respectively. Confocal laser scanning microscopy and cell line studies respectively demonstrated that encapsulation of 5-ALA in NLC enhanced its ability to reach deeper skin layers and consequently, increased cytotoxicity.
    Matched MeSH terms: Photosensitizing Agents/administration & dosage*; Photosensitizing Agents/metabolism; Photosensitizing Agents/chemistry
  19. Kamarulzaman EE, Gazzali AM, Acherar S, Frochot C, Barberi-Heyob M, Boura C, et al.
    Int J Mol Sci, 2015 Oct 12;16(10):24059-80.
    PMID: 26473840 DOI: 10.3390/ijms161024059
    Photodynamic therapy (PDT) is a cancer treatment modality that requires three components, namely light, dioxygen and a photosensitizing agent. After light excitation, the photosensitizer (PS) in its excited state transfers its energy to oxygen, which leads to photooxidation reactions. In order to improve the selectivity of the treatment, research has focused on the design of PS covalently attached to a tumor-targeting moiety. In this paper, we describe the synthesis and the physico-chemical and photophysical properties of six new peptide-conjugated photosensitizers designed for targeting the neuropilin-1 (NRP-1) receptor. We chose a TPC (5-(4-carboxyphenyl)-10,15, 20-triphenyl chlorine as photosensitizer, coupled via three different spacers (aminohexanoic acid, 1-amino-3,6-dioxaoctanoic acid, and 1-amino-9-aza-3,6,12,15-tetraoxa-10-on-heptadecanoic acid) to two different peptides (DKPPR and TKPRR). The affinity towards the NRP-1 receptor of the conjugated chlorins was evaluated along with in vitro and in vivo stability levels. The tissue concentration of the TPC-conjugates in animal model shows good distribution, especially for the DKPPR conjugates. The novel peptide-PS conjugates proposed in this study were proven to have potential to be further developed as future NRP-1 targeting photodynamic therapy agent.
    Matched MeSH terms: Photosensitizing Agents/chemical synthesis; Photosensitizing Agents/pharmacology*; Photosensitizing Agents/chemistry
  20. Savelyev AG, Sochilina AV, Babayeva G, Nikolaeva ME, Kuziaeva VI, Prostyakova AI, et al.
    Biomater Sci, 2025 Feb 11;13(4):980-992.
    PMID: 39801275 DOI: 10.1039/d4bm01174k
    Photocrosslinkable hydrogels based on hyaluronic acid are promising biomaterials high in demand in tissue engineering. Typically, hydrogels are photocured under the action of UV or blue light strongly absorbed by biotissues, which limits prototyping under living organism conditions. To overcome this limitation, we propose the derivatives of well-known photosensitizers, namely chlorin p6, chlorin e6 and phthalocyanine, as those for radical polymerization in the transparency window of biotissues. Taking into account the efficiency of radical generation and dark and light cell toxicity, we evaluated water miscible pyridine phthalocyanine as a promising initiator for the intravital hydrogel photoprinting of hyaluronic acid glycidyl methacrylate (HAGM) under irradiation near 670 nm. Coinitiators (dithiothreitol or 2-mercaptoethanol) reduce the irradiation dose required for HAGM crosslinking from ∼405 J cm-2 to 80 J cm-2. Patterning by direct laser writing using a scanning 675 nm laser beam was performed to demonstrate the formation of complex shape structures. Young's moduli typical of soft tissue (∼270-460 kPa) were achieved for crosslinked hydrogels. The viability of human keratinocytes HaCaT cells within the photocrosslinking process was shown. To demonstrate scaffolding across the biotissue barrier, the subcutaneously injected photocomposition was crosslinked in BALB/c mice. The safety of the irradiation dose of 660-675 nm light (100 mW cm-2, 15 min) and the non-toxicity of the hydrogel components were confirmed by histomorphologic analysis. The intravitally photocrosslinked scaffolds maintained their shape and size for at least one month, accompanied by slow biodegradation. We conclude that the proposed technology provides a lucrative opportunity for minimally invasive scaffold formation through biotissue barriers.
    Matched MeSH terms: Photosensitizing Agents/administration & dosage; Photosensitizing Agents/pharmacology; Photosensitizing Agents/chemistry
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