Abstract
Ferulic acid (FA) is an antioxidant compound that can prevent ROS-related diseases, but due to its poor solubility, therapeutic efficacy is limited. One strategy to improve the bioavailability is nanomedicine. In the following study, FA delivery through polymeric nanoparticles (NPs) consisting of polylactic acid (NPA) and poly(lactic-co-glycolic acid) (NPB) is proposed. To verify the absence of cytotoxicity of blank carriers, a preliminary in vitro assay was performed on retinal pericytes and endothelial cells. FA-loaded NPs were subjected to purification studies and the physico-hemical properties were analyzed by photon correlation spectroscopy. Encapsulation efficiency and in vitro release studies were assessed through high performance liquid chromatography. To maintain the integrity of the systems, nanoformulations were cryoprotected and freeze-dried. Morphology was evaluated by a scanning electron microscope. Physico-chemical stability of resuspended nanosystems was monitored during 28 days of storage at 5 °C. Thermal analysis and Fourier-transform infrared spectroscopy were performed to characterize drug state in the systems. Results showed homogeneous particle populations, a suitable mean size for ocular delivery, drug loading ranging from 64.86 to 75.16%, and a controlled release profile. The obtained systems could be promising carriers for ocular drug delivery, legitimating further studies on FA-loaded NPs to confirm efficacy and safety in vitro.
Highlights
Oxidative stress is able to involve morphological and functional alterations to retinal tissues, playing a key role in the onset and progression of retinal diseases, such as agerelated macular degeneration (AMD), glaucoma, diabetic retinopathy (DR), and retinal vein occlusion (RVO) [1]
To assess if NPA or NPB could induce cytotoxicity, MTT bioassay was performed on primary cultures of micro-capillaries pericytes and endothelial cells
The results showed that DNA synthesis of endothelial cells in single culture was reduced by 30% compared to cells co-cultured with pericytes
Summary
Oxidative stress is able to involve morphological and functional alterations to retinal tissues, playing a key role in the onset and progression of retinal diseases, such as agerelated macular degeneration (AMD), glaucoma, diabetic retinopathy (DR), and retinal vein occlusion (RVO) [1]. Thanks to the pluri-pharmacological effects, these molecules might be able to slow down and prevent the progression of the aforementioned pathologies [2,3]. The most attractive polyphenol effects in these diseases are wielded on oxidative stress pathways, where they are able to suppress the harmful effect of the reactive oxygen species (ROS) [4]. For this reason, antioxidant molecules are gaining importance as a promising therapeutic strategy in treatment/prevention of eye chronic disease.
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