Abstract
Intra-articular administration of drugs to the joint in the treatment of joint disease has the potential to minimize the systemic bioavailability and the usual side-effects associated with oral drug administration. In this work, a drug delivery system is proposed to achieve an anti-inflammatory local effect using resveratrol (RSV). This study aims to develop microcapsules made of poly-(ε-caprolactone) (PCL) by ultrasonic atomization to preserve the antioxidant activity of RSV, to prevent its degradation and to suppress the inflammatory response in activated RAW 264.7 macrophages. An experimental design was performed to build a mathematical model that could estimate the effect of nozzle power and polymer concentration on particle size and encapsulation efficiency. RSV-loaded microcapsules showed adequate morphology, particle size, and loading efficiency properties. RSV formulations exhibited negligible cytotoxicity and an efficient amelioration of inflammatory responses, in terms of Nitric Oxide (NO), ROS (Reactive Oxygen Species), and lipid peroxidation in macrophages. Thus, RSV-loaded microcapsules merit consideration as a drug delivery system suitable for intra-articular administration in inflammatory disorders affecting the joint.
Highlights
Trans-resveratrol (3,5,4 -trihydroxystilbene; RSV) is a phytoalexin that has been found as a secondary metabolite in numerous vascular plants (Figure 1)
The phenomenon of oxidative stress and, as a consequence, the damage to cells and tissues by free radicals has been demonstrated to play a critical role in a wide number of pathologies including, among others, rheumatoid arthritis, where the oxidative stress is even considered a pathogenic marker of the disease [1,2]
The present work has successfully established the preparation of RSV-loaded microcapsules made of PCL by ultrasonic atomization, with a size and morphology suitable for local administration into the joint by intra-articular administration
Summary
Trans-resveratrol (3,5,4 -trihydroxystilbene; RSV) is a phytoalexin that has been found as a secondary metabolite in numerous vascular plants (Figure 1). The groups 3- and 5-OH, in ring A, and the double link with 4-oxo function, in ring C, provide the antioxidant capacity of RSV. The phenomenon of oxidative stress and, as a consequence, the damage to cells and tissues by free radicals has been demonstrated to play a critical role in a wide number of pathologies including, among others, rheumatoid arthritis, where the oxidative stress is even considered a pathogenic marker of the disease [1,2]. The antioxidant power of Pharmaceutics 2019, 11, 249 to play a critical role in a wide number of pathologies including, among others, rheumatoid arthritis, where the oxidative stress is even considered a pathogenic marker of the disease [1,2].
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