Characterization of biodegradable poly(D,L-lactide-co-glycolide) nanoparticles loaded with bacteriochlorophyll-a for photodynamic therapy.

OBJECTIVE: Bacteriochlorophyll-a (BChl-a) was incorporated into nanoparticles of poly(D,L-lactide-co-glycolide) (PLGA), in order to evaluate this photosensitizer when associated with this specific drug delivery system (DDS) to analyze its physical and spectral properties. BACKGROUND DATA: It has been suggested in the literature that BChl-a is a potential sensitizer in photodynamic tumor therapy and until now has only been investigated in organic media. METHODS: Nanoparticles loaded with the photosensitizer BChl-a were prepared by the solvent evaporation technique. Parameters such as particle size, drug encapsulation efficiency, external morphology, and in vitro release behavior were evaluated. The photophysical properties (absorption, fluorescence, fluorescence quantum yields, and singlet oxygen quantum yields) of BChl-a, were investigated in toluene and when encapsulated in nanoparticles. RESULTS: Scanning electron microscopy and dynamic light scattering revealed that particles loaded with BChl-a are spherical in shape, and they have a diameter of 660 nm and a low tendency to aggregate. The encapsulation efficiency obtained in this procedure was 69%. Spectroscopic analysis showed an absorption band centered at 782 nm in nanoparticles used as a DDS. Fluorescence quantum yield (phi(F) = 0.19) and higher efficiency in singlet oxygen production (Phi(Delta) = 0.26) was also observed. CONCLUSIONS: The results suggest that this DDS is potentially useful for the delivery and release of BChl-a as a photosensitizer in photodynamic therapy (PDT) protocols due to its excellent biodegradability, biocompatibility, and maintenance of its spectroscopic properties when compared with other dyes in homogenous media. The biocompatible DDS medium is a new proposal and will make feasible the use of BChl-a as a dye for PDT, improving the utilization of non-organic media to deliver this kind of molecule.

Photobiological and ultrastructural studies of nanoparticles of poly(lactic-co-glycolic acid)-containing bacteriochlorophyll-a as a photosensitizer useful for PDT treatment.

The interaction of polymeric nanoparticles formulated from the biodegradable polymer poly(DL-lactide-co-glycolide) loaded with bacteriochlorophyll-a was studied in homogeneous solution and in vitro in the presence of a macrophage cell line (P388-D1-ATCC). Photodynamic therapy (PDT) activity after different laser doses also was investigated. Scanning electron microscopy analysis of cell phagocyte nanoparticles showed that after 30 min of incubation most of the nanoparticles are in a clear adhesion process to the cell surface. The majority of nanoparticles became phagocytic after 2 hr of incubation time. After laser irradiation of the dye-containing system a total photodamage by nanoparticle phagocyte cells was observed and the cell survival was quantified by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide test. Our results indicate that polymeric nanoparticles work as an efficient drug delivery system for PDT drugs. This approach can be widely used for many other hydrophobic photosensitizers with higher aggregation tendency in neoplastic cell treatment.