AI Article Synopsis

  • A fluorinated phthalocyanine was compared to its non-fluorinated version to assess how fluorination affects their photophysical, photochemical, and redox properties, as well as their biological activity.
  • The study explored the drugs' abilities to interact with biological membranes and proteins, while developing a water-dispersible formulation using Pluronic triblock copolymer micelles to enhance delivery and reduce self-aggregation.
  • The results indicated that the incorporation of phthalocyanines into micelles improved cellular uptake and photocytotoxicity, with the fluorinated variant showing the best efficacy in tumor growth inhibition, leading to complete regression in some mice.

Article Abstract

A fluorinated phthalocyanine and its non-fluorinated analogue were selected to evaluate the potential enhancement of fluorination on photophysical, photochemical and redox properties as well as on biological activity in cellular and animal models. Due to the pharmacological relevance, the affinity of these phthalocyanines towards biological membranes (logP) as well as their primary interaction with human serum albumin (HSA) or low-density lipoprotein (LDL) were determined. Water-dispersible drug formulation of phthalocyanines via Pluronic-based triblock copolymer micelles was prepared to avoid self-aggregation effects and to improve their delivery. The obtained results demonstrate that phthalocyanines incorporation into tunable-polymeric micelles significantly enhanced their cellular uptake and their photocytotoxicity. The improved biodistribution and photodynamic efficacy of the phthalocyanines-triblock copolymer conjugates was also confirmed in vivo in CT26 bearing BALB/c mice. PDT with both compounds led to tumor growth inhibition in all treated animals. Fluorinated phthalocyanine 2 turned out to be the most effective anticancer agent as the tumors of 20% of mice treated regressed completely and did not appear for over one year after treatment.

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http://dx.doi.org/10.1016/j.ejmech.2016.08.035DOI Listing

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