Functional Polymeric Systems as Delivery Vehicles for Methylene Blue in Photodynamic Therapy

Mariana V Junqueira1, Fernanda B Borghi-Pangoni1, Sabrina B S Ferreira1

  • 1Postgraduate Program in Pharmaceutical Sciences, Laboratory of Research and Development of Drug Delivery Systems, Department of Pharmacy, and ‡Postgraduate Program in Chemistry, Department of Chemistry, State University of Maringá , Maringá, Paraná, Brazil.

Insights

This study developed functional polymeric systems containing methylene blue (MB) for photodynamic therapy (PDT) to combat antibiotic resistance. The optimized gel formulation showed good MB release and produced reactive oxygen species, indicating potential for wound treatment.

Area of Science:

  • Pharmaceutical Sciences
  • Biomaterials Engineering
  • Photomedicine

Background:

  • Antibiotic-resistant microorganisms pose a significant global health threat, necessitating novel therapeutic strategies.
  • Photodynamic therapy (PDT), utilizing a photosensitizer, light, and oxygen, offers a promising alternative by generating cytotoxic reactive oxygen species.
  • Methylene blue (MB), a phenothiazine photosensitizer, is explored for its therapeutic potential.

Purpose of the Study:

  • To develop functional polymeric systems for enhanced topical delivery of methylene blue (MB) for photodynamic therapy (PDT).
  • To optimize MB-loaded poloxamer/Carbopol gels using Design of Experiments for wound applications.
  • To evaluate the physicochemical, release, permeation, and photodynamic efficacy of the developed MB-loaded gels.

Main Methods:

  • Formulation of poloxamer 407 and Carbopol 934P gels with varying MB concentrations using Design of Experiments (2(3) + central point).
  • Characterization of sol-gel transition temperature, rheological properties, and in vitro MB release kinetics.
  • Ex vivo skin permeation and retention studies, in vitro photodynamic activity assessment (tryptophan degradation), and Artemia salina toxicity testing.

Main Results:

  • Optimized MB-loaded gels exhibited gelation temperatures between 25-37 °C, suitable for physiological application.
  • The formulation containing 20% poloxamer 407, 0.15% Carbopol 934P, and 0.25% MB demonstrated the most favorable in vitro release profile (42.57% at 24 h).
  • This optimized system showed minimal skin permeation (0.38% at 24 h), effective reactive oxygen species generation, and a significant increase in Artemia salina mortality (61.29%) when exposed to light, indicating photodynamic efficacy.

Conclusions:

  • Functional polymeric systems containing methylene blue were successfully developed for potential topical photodynamic therapy.
  • The optimized gel formulation exhibits desirable release characteristics and demonstrates photodynamic activity, suggesting its potential as an alternative to antibiotics.
  • Further investigation into the in vivo efficacy of this MB-loaded polymeric system for treating infections caused by antibiotic-resistant microorganisms is warranted.