Abstract
The present study aimed to develop a novel formulation containing glutathione (GSH) as an oral antioxidant therapy for the treatment of oxidative stress-related intestinal diseases. To this purpose, solid lipid microparticles (SLMs) with Dynasan 114 and a mixture of Dynasan 114 and Dynasan 118 were produced by spray congealing technology. The obtained SLMs had main particle sizes ranging from 250 to 355 µm, suitable for oral administration. GSH was efficiently loaded into the SLMs at 5% or 20% w/w and the encapsulation process did not modify its chemico-physical properties, as demonstrated by FT-IR, DSC and HSM analysis. Moreover, in vitro release studies using biorelevant media showed that Dynasan 114-based SLMs could efficiently release GSH in various intestinal fluids, while 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay demonstrated the good radical scavenging activity of this formulation. Dynasan 114-based SLMs exhibited an excellent biocompatibility on intestinal HT-29 cells at concentrations up to 2000 μg/mL. SLMs containing GSH alone or together with another antioxidant agent (catalase) were effective in reducing intracellular reactive oxygen species (ROS) levels. Overall, this study indicated that spray congealed SLMs are a promising oral drug delivery system for the encapsulation of one or more biological antioxidant agents for local intestinal treatment.
Highlights
Oxidative stress is defined as an imbalance between oxidant and antioxidant species, with overproduction of reactive oxygen species (ROS) and other free radicals, a disruption of redox signaling and/or molecular damage [1]
Solid lipid microparticles (SLMs) with Dynasan 114 and a mixture of Dynasan 114 and Dynasan 118 were produced by spray congealing technology
GSH was efficiently loaded into the solid lipid microparticles (SLMs) at 5% or 20% w/w and the encapsulation process did not modify its chemico-physical properties, as demonstrated by FT-IR, Differential Scanning Calorimetry (DSC) and Hot Stage Microscopy (HSM) analysis
Summary
Oxidative stress is defined as an imbalance between oxidant and antioxidant species, with overproduction of reactive oxygen species (ROS) and other free radicals, a disruption of redox signaling and/or molecular damage [1]. ROS overproduction has been implicated in the pathogenesis of diverse gastrointestinal diseases including inflammatory bowel disease (IBD), gastroesophageal reflux disease (GERD), gastritis, enteritis, colitis and associated cancers as well as pancreatitis and liver cirrhosis [3]. When the antioxidant capacity of the intestinal mucosa is compromised, the use of active substances able to decrease ROS can be beneficial, either associated or not with anti-inflammatory medicines [4]. The thiol group is a potent reducing agent, making GSH one of the strongest physiological antioxidants [5]. Intracellular GSH exists mainly (98%) in the thiol-reduced form, while the oxidized form glutathione disulfide (GSSG, Figure 1) is usually around 1% [6]. In case of diseases and oxidative stress, the total GSH content and the GSH/GSSG ratio can drastically decrease [6]
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