Cellular Photodynamic Toxicity of Hematoporphyrin in Various Nanocarrier Systems

Yu-Tsai      Yang; Chin-Tin      Chen; Hsiung-Fei      Chien; Tsuimin      Tsai

doi:10.2174/157341311798220718

Abstract

In this study, we investigated the cellular uptake of Hematoporphyrin (Hp) encapsulated in nanocarriers by human lung adenocarcinoma A549 cells and the photodynamic toxic effects on those cells. The nanocarriers included liposomes, micelles, and nanoparticles. The Hp was encapsulated in liposomes through a film hydration and extrusion method. Hp was encapsulated in micelles through a film hydration method. The Hp loaded nanoparticles were prepared using an emulsification-diffusion process. The Hp in nanocarriers was characterized by laser light scattering to determine particle size and zeta potential of the surface charge. The cellular uptake of nanocarriers was measured by fluorescence spectrometry. The photodynamic toxicity of various Hp nanocarriers was evaluated in human lung epithelial carcinoma A549 cells using a light-emitting diode (LED) device at a wavelength of 630± 5 nm. The averaged size of all nanocarriers was between 112 and 135 nm. The surface charge observed for all formulations, particularly the micelles showed lower negative valued than those of other systems. Cellular uptake and photocytotoxicity of the four Hp preparations in serum free medium were in the following order: micelle-Hp > nanoparticle-Hp > liposome-Hp > free Hp. In the presence of serum protein, the photodynamic toxicity of all formulations significantly decreased.

Keywords: Liposomes, micelles, nanoparticles, photodynamic therapy, photosensitizers, protein binding, Hematoporphyrin, nanocarrier systems