Biodegradable nanoparticles containing benzopsoralens : an attractive strategy for modifying vascular function in pathological skin disorders

Abstract

Psoralens are often used to treat skin disorders such as psoriasis, vitiligo and others. The toxicity and fast degradation of these drugs can be diminished by encapsulation in drug delivery systems (DDS). Nanoparticles (NPs) containing the benzopsoralen (BP) (3-ethoxy carbonyl-2H-benzofuro[3,2-e]-1-benzopiran-2-one) were prepared by the solvent evaporation technique, and parameters such as particle size, zeta potential, drug encapsulation efficiency, and external morphology were evaluated. The analysis revealed that the NPs are spherical and possessed a smooth external surface with diameter of 815 ± 80 nm, they present low tendency toward aggregation, as confirmed by their zeta potential (+17.3±2.9 mV) and the encapsulation efficiency obtained was 74%. The intracellular distribution of NPs as well as their uptake by tissues was monitored by using laser confocal microscopy and transmission electron microscopy. The use of benzopsoralen in association with ultraviolet light (360 nm) revealed morphological characteristics of cell damage such as cytosolic vesiculation, mitochondria condensation, and swelling of both the granular endoplasmic reticulum and the nuclear membrane. The primary target of DDS and drugs in vascular system are endothelial cells and an attractive strategy for modifying vascular function in various pathological states of skin disorders, cancer and inflammation. The result presented in this work indicates that PLGA NP could be a promising delivery system for benzopsoralen in connection with ultraviolet irradiation therapy (PUVA) for further application in different therapies.