Abstract
Osteoarthritis (OA) is a degenerative joint disease. An objective of the nanomedicine and drug delivery systems field is to design suitable pharmaceutical nanocarriers with controllable properties for drug delivery and site-specific targeting, in order to achieve greater efficacy and minimal toxicity, compared to the conventional drugs. The aim of this review is to present recent data on natural bioactive compounds with anti-inflammatory properties and efficacy in the treatment of OA, their formulation in lipid nanostructured carriers, mainly liposomes, as controlled release systems and the possibility to be intra-articularly (IA) administered. The literature regarding glycosaminoglycans, proteins, polyphenols and their ability to modify the cell response and mechanisms of action in different models of inflammation are reviewed. The advantages and limits of using lipid nanoformulations as drug delivery systems in OA treatment and the suitable route of administration are also discussed. Liposomes containing glycosaminoglycans presented good biocompatibility, lack of immune system activation, targeted delivery of bioactive compounds to the site of action, protection and efficiency of the encapsulated material, and prolonged duration of action, being highly recommended as controlled delivery systems in OA therapy through IA administration. Lipid nanoformulations of polyphenols were tested both in vivo and in vitro models that mimic OA conditions after IA or other routes of administration, recommending their clinical application.
Highlights
Several studies indicated that local joint inflammation induced by endogenous molecular products derived from cellular stress and extracellular matrix degradation acted through innate inflammatory network and could influence the integrity and function of articular cartilage [12,13]
GAGs are a family of long chain polysaccharides with a linear structure, consisting of repetitive hexosamine-uronic acid units highly sulphated in variable positions, excepting hyaluronic acid or hyaluronan (HA)
In vitro studies using chondrocyte lines and cartilage explants demonstrated the capacity of flavonoids to suppress matrix metalloproteinases (MMPs) expression through mechanisms not involving mitogen-activated protein kinase (MAPK) inhibition, signalling molecules, such as nuclear transcription factor-κB
Summary
Publisher’s Note: MDPI stays neutral with regard to jurisdictional claims in published maps and institutional affiliations. Liposomes possess many biophysical and physicochemical properties suitable for IA administration, such as sustained release, ability for self-assembly and capacity to load large quantities of drugs [23,37] Due to their ability to incorporate hydrophilic and hydrophobic molecules, good biocompatibility, low toxicity, activation and targeted delivery of bioactive compounds to the site of action, liposomes offer many advantages, such as the protection and efficiency of encapsulated material, solubilization of lipophilic molecules, prolongation of the duration of action and present targeting options. Data regarding their anti-inflammatory activity and mechanisms of action, and their lipid nanoformulation as efficient delivery systems are the main topics reviewed here. Natural Bioactive Compounds with Anti-Inflammatory Activity and Mechanisms of Action
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