Anthraquinone encapsulation into polymeric nanocapsules as a new drug from biotechnological origin designed for photodynamic therapy

Abstract

Photodynamic therapy has been applied for the treatment of many diseases, especially skin diseases. However, poor aqueous solubility and toxicity of some photosensitizer drugs are the main disadvantages for their direct clinical applications. Thus, biotechnology and nanotechnology are important tools in the development of new ways of obtaining photoactive compounds that are biocompatible. We investigated the potential of a new nanostructured photosensitizer, an anthraquinone derivative produced by biotechnological process; then we associated nanotechnology to obtain a nanostructured anthraquinone active molecule. For this, it was prepared a classical nanocapsule formulations containing poly(lactide-co-glycolide) (PLGA) coating for encapsulation of anthraquinone derivative. These formulations were characterized by their physicochemical, morphological, photophysical properties, and stability. We performed in vitro biocompatibility and photodynamic activity assays of free and nanostructured anthraquinone. Nanocapsule formulations containing anthraquinone derivative showed a nanometric profile with particle size around 250 nm, negative zeta potential around −30 mV, and partially monodisperse. Besides that, characteristic spherical morphology of nanocapsules and homogeneous particle surface were observed by AFM analyses. The in vitro biocompatibility assay showed absence of cytotoxicity for all tested RD/NC concentrations and also for unloaded/NC in NIH3T3 cells. In vitro photoactivation assay using NIH3T3 cells showed that nanocapsules promoted greater drug uptake by NIH3T3 cells, around of 87%, of cell death compared to free drug showed around 48% of cell death. The anthraquinone derivative showed potential for use in PDT. Besides the association with nanocapsules improved cell uptake of photosensitizer resulting in increased cell death compared to free anthraquinone.