The influence of positive or negative charges in the passive and iontophoretic skin penetration of porphyrins used in photodynamic therapy

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Abstract

Meso-tetra-(N-methylpiridinium-4-yl)-porphyrin (TMPyP) and meso-tetra-(4-sulfonatophenyl)-porphyrin (TPPS4) are photosensitizing drugs (PS) used in photodynamic therapy (PDT). Based on the fact that these compounds present similar chemical structures but opposite charges at pH levels near physiological conditions, this work aims to evaluate the in vitro and in vivo influence of these electrical charges on the iontophoretic delivery of TMPyP and TPPS4, attempting to achieve maximum accumulation of PS in skin tissue. The iontophoretic transport of these drugs from a hydrophilic gel was investigated in vitro using porcine ear skin and vertical, flow-through diffusion cells. In vivo experiments using rats were also carried out, and the penetration of the PSs was analyzed by fluorescence microscopy to visualize the manner of how these compounds were distributed in the skin after a short period of iontophoresis application. In vitro, both passive and iontophoretic delivery of the positively charged TMPyP were much greater (20-fold and 67-fold, respectively) than those of the negatively charged TPPS4. TPPS 4 iontophoresis in vivo increased the fluorescence of the skin only in the very superficial layers. On the other hand, iontophoresis of the positively charged drug expressively increased the rat epidermis and dermis fluorescence, indicating high amounts of this drug throughout the skin layers. Moreover, TMPyP was homogeneously distributed around and into the nuclei of the skin cells, suggesting its potential use in topical PDT. © 2010 Elsevier Inc. All rights reserved.

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Gelfuso, G. M., Gratieri, T., Souza, J. G., Thomazine, J. A., & Lopez, R. F. V. (2011). The influence of positive or negative charges in the passive and iontophoretic skin penetration of porphyrins used in photodynamic therapy. European Journal of Pharmaceutics and Biopharmaceutics, 77(2), 249–256. https://doi.org/10.1016/j.ejpb.2010.11.018

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