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c(RGDfK)‐ and ZnTriMPyP‐Bound Polymeric Nanocarriers for Tumor‐Targeted Photodynamic Therapy
Author(s) -
las Heras Elena,
BoixGarriga Ester,
Bryden Francesca,
Agut Montserrat,
Mora Margarita,
Sagristá M. Lluïsa,
Boyle Ross W.,
Lange Norbert,
ll Santi
Publication year - 2020
Publication title -
photochemistry and photobiology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.818
H-Index - 131
eISSN - 1751-1097
pISSN - 0031-8655
DOI - 10.1111/php.13238
Subject(s) - nanocarriers , photodynamic therapy , photosensitizer , phototoxicity , chemistry , covalent bond , peg ratio , in vitro , selectivity , pyridinium , biophysics , combinatorial chemistry , biochemistry , drug delivery , organic chemistry , biology , finance , economics , catalysis
Active targeting strategies are currently being extensively investigated in order to enhance the selectivity of photodynamic therapy. The aim of the present research was to evaluate whether the external decoration of nanopolymeric carriers with targeting peptides could add more value to a photosensitizer formulation and increase antitumor therapeutic efficacy and selectivity. To this end, we assessed PLGA‐PLA‐PEG nanoparticles (NPs) covalently attached to a hydrophilic photosensitizer 5‐[4‐azidophenyl]‐10,15,20‐tri‐( N ‐methyl‐4‐pyridinium)porphyrinato zinc (II) trichloride (ZnTriMPyP) and also to c(RGDfK) peptides, in order to target α v β 3 integrin‐expressing cells. In vitro phototoxicity investigations showed that the ZnTriMPyP‐PLGA‐PLA‐PEG‐c(RGDfK) nanosystem is effective at submicromolar concentrations, is devoid of dark toxicity, successfully targets α v β 3 integrin‐expressing cells and is 10‐fold more potent than related nanosystems where the PS is occluded instead of covalently bound.