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Photochem Photobiol Sci ; 18(2): 487-494, 2019 Feb 13.
Artigo em Inglês | MEDLINE | ID: mdl-30534717

RESUMO

Chagas is a parasitic endemic disease caused by the protozoan Trypanosoma cruzi. It represents a strong threat to public health due to its strong resistance against commonly available drugs. We studied the in vitro ability to inactivate the trypomastigote form of this parasite using photodynamic inactivation of microorganisms (or antimicrobial Photodynamic Therapy, aPDT). For this, we chose to use the photosensitizer hypericin (Hyp) formulated in ethanol/water (1% v/v) and Hyp loaded in the dispersion of different aqueous nanocarrier systems. These included polymeric micelles of F-127 and P-123 (both Pluronic™ surfactants), and liposomal vesicles of phospholipid 2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC). These systems with Hyp had their activity compared against trypomastigote forms under light and in the dark. Hyp revealed a high level of effectiveness to eradicate protozoa in vitro. Samples at concentrations higher than 0.8 µmol L-1 of Hyp in Pluronic micelles showed efficacy even in the dark, with the EC50 around (6-8) µmol L-1. Therefore, Hyp/Pluronics can be used also as a chemotherapeutic agent. The best result for EC50 is at approximately 0.31 µmol L-1 for illuminated systems of Hyp in F-127 micelles. For Hyp in P-123 micelles under light, the results also led to a low EC50 value of 0.36 µmol L-1. The highest value of EC50 was 2.22 µmol L-1, which was found for Hyp/DPPC liposomes under light. For the Hyp-free (ethanol/water, 1% v/v)/illuminated group, the EC50 value was 0.37 µmol L-1, which also is a value that shows effectiveness. However, in free-form, Hyp is not protected against blood components, unlike when Hyp is loaded into the nanocarriers.


Assuntos
Portadores de Fármacos/química , Nanoestruturas/química , Perileno/análogos & derivados , Trypanosoma cruzi/efeitos dos fármacos , Trypanosoma cruzi/efeitos da radiação , Antracenos , Micelas , Perileno/química , Perileno/farmacologia , Poloxâmero/análogos & derivados , Poloxâmero/química
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