Lumichrome, a photodegradation product of riboflavin, is an endogenous compound in humans. The compound is more photostable and a more efficient photogenerator of singlet oxygen than riboflavin. It absorbs radiation in the UVA and blue-light region, which can be an advantage in antibacterial photodynamic therapy (aPDT) of superficial infections. The aim of this study was to investigate the in vitro aPDT effect of various lumichrome pharmaceutical formulations. Solutions of lumichrome (10-5 – 10-3M) were prepared in plain phosphate buffered saline (PBS) or in PBS solutions containing cyclodextrins, DMSO, PEG 400 or polyoxamers (Pluronic®). Supersaturated solutions of lumichrome in PBS were prepared via the cosolvent and solvent evaporation method. Phototoxic effects of selected lumichrome preparations were studied in planktonic Gram-positive (E. faecalis) and Gram-negative (E. coli) bacteria models. The UVA/blue light source emitted mainly in the range 340-440 nm. Lumichrome was up to tenfold more phototoxic against Grampositive than to Gram-negative bacteria. Bacterial eradication was induced after exposure of lumichrome formulations (PBS, PEG 400 and HP CD) combined with 24 J/cm2 UVA/blue light. Increasing the concentration of lumichrome did not enhance the phototoxic effect, probably due to radiation attenuation in the highly absorbing solution (inner filter effect). Cyclodextrins were efficient enhancers of the lumichrome solubility in aqueous solutions, but inhibited the phototoxic effect. The study demonstrates that assuming the use of an optimized formulation, lumichrome has potential as a UVA/blue light photosensitizer in aPDT.
Influence of formulation on photoinactivation of bacteria by lumichrome
Valerón Bergh VJ, Bruzell E, Hegge AB, Tønnesen HH.
Die Pharmazie 2015; 70 (9): 574-580(7).