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

1
Department of Pharmacology, Pharmacy and Pharmaceutical Technology, School of Sciences, Campus de Lugo, University of Santiago de Compostela, 27002 Lugo, Spain
2
Department of Pharmacology, Pharmacy and Pharmaceutical Technology, School of Pharmacy, Campus de Santiago de Compostela, University of Santiago de Compostela, 14875 Santiago de Compostela, Spain
*
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Pharmaceutics 2019, 11(6), 249; https://doi.org/10.3390/pharmaceutics11060249
Received: 23 April 2019 / Revised: 22 May 2019 / Accepted: 23 May 2019 / Published: 28 May 2019
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. View Full-Text
Keywords: drug delivery system; microcapsules; photodegradation; ultrasound; antioxidant; site-specific delivery; resveratrol drug delivery system; microcapsules; photodegradation; ultrasound; antioxidant; site-specific delivery; resveratrol
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Luzardo-Álvarez, A.; Lamela-Gómez, I.; Otero-Espinar, F.; Blanco-Méndez, J. Development, Characterization, and In Vitro Evaluation of Resveratrol-Loaded Poly-(ε-caprolactone) Microcapsules Prepared by Ultrasonic Atomization for Intra-Articular Administration. Pharmaceutics 2019, 11, 249.

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