Development, Characterization, and In Vitro Evaluation of Resveratrol-Loaded Poly-(ε-caprolactone) Microcapsules Prepared by Ultrasonic Atomization for Intra-Articular Administration

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 loca...

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Bibliographic Details
Published in:Pharmaceutics 2019-05, Vol.11 (6), p.249
Main Authors: Luzardo-Álvarez, Asteria, Lamela-Gómez, Iván, Otero-Espinar, Francisco, Blanco-Méndez, José
Format: Article
Language:English
Subjects:
antioxidant
Antioxidants
Bioavailability
Biological products
Cartilage
Cytokines
Disease
drug delivery system
Drug delivery systems
Drug dosages
Inflammation
microcapsules
Morphology
Oxidative stress
Particle size
photodegradation
Polymers
Polyvinyl alcohol
resveratrol
Rheumatoid arthritis
site-specific delivery
ultrasound
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Summary: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.
ISSN:1999-4923
1999-4923
DOI:10.3390/pharmaceutics11060249