Chondroitin Sulphate for the Treatment of Osteoarthritis

Abstract

The aim of this review is to illustrate the structural biology and functions of chondroitin sulphate (CS) in the light of recent glycobiological studies suggesting its new fundamental biological functions, and to evaluate the literature on CS concerning the pathobiology of osteoarthritis (OA), to ascertain whether this agent should be classified as a symptomatic slow-acting drug (SYSADOA), a compound that has a slow onset of action in alleviating OA symptoms. A previous review [Volpi, N. The pathobiology of osteoarthritis and the rationale for the use of chondroitin sulfate for its treatment. Curr. Drug Targets Immune Endocr. Metabol. Disord., 2004, 4, 119] has been published on this topic and this article intends to extend and update CS data and its use in the treatment of OA.CS exhibits a wide range of biological activities and from a pharmacological point of view, it produces a slow but gradual reduction of the clinical symptoms of OA, and these benefits last for a long period after the end of treatment. Furthermore, many animal studies and clinical trials have proved the efficacy of CS as a structure-modifying OA drug agent able to reverse, retard, or stabilize the pathology of OA, thereby providing symptomatic relief in the long-term treatment. In addition, there are fewer side effects when compared with other drugs used to treat the symptoms of OA, as well as a lack of toxicity associated with long-term use of these agents. These properties are also related to the oral absorption of this molecule as high-molecular mass compounds having clusters of sulphate groups and high charge density, capable of exerting their chondroprotective activity in vivo.

Quality of different chondroitin sulfate preparations in relation to their therapeutic activity

“…[25] It is well known that specific activity depends on the chondroitin sulfate structure and properties. [2][3][4][5][6][7][8][9][10][11][12][13][14][15][16][17][18] Additionally, chondroitin is administered orally during therapy and bioavailability and pharmacokinetic parameters have been reported to change depending on its structural characteristics and origin. [38][39][40] As a consequence, chondroitin sulfate with a low quality of content and properties, generally present in nutraceuticals, would be unable to exert comparable pharmacological effects to those of the pharmaceutical-grade chondroitin sulfate, and the same clinical effects would not be produced unless various chondroitin sulfate preparations have a similar structure.…”

“…[1] Biological role of chondroitin sulfate Recent evidence from glycobiology studies suggests that proteoglycans, and their complex polysaccharidic macromolecules, are not only structural components, but they also participate in and regulate many cellular events and physiological processes. [1,2] Growing recent evidence suggests that chondroitin sulfate (and dermatan sulfate) chains have intriguing functions in central nervous system development, wound repair, infection, growth factor signalling, morphogenes and cell division, differentiation and migration, in addition to osteoarthritis (OA; see below) and their conventional structural roles (for more complete and specialized papers see references [2][3][4][5][6][7][8][9][10][11][12][13][14][15][16][17][18] ).…”

Self-assembled poly(ε-caprolactone)-g-chondroitin sulfate copolymers as an intracellular doxorubicin delivery carrier against lung cancer cells

“…CS has many promising properties such as biocompatibility, biodegradability, anti-inflammatory, and as a good structure/ disease-modifying antiosteoarthritis drug (S/DMOAD). 16 Our previous study successfully introduced the methacrylate groups to CS (CSMA) for preparing a pH-sensitive hydrogel. 17 The vinyl groups on CSMA could be used to react with PCL end-capped double bonds to produce a graft copolymer (CSMA-g-PCL).…”

Antitumor Efficacy of Doxorubicin Released from Crosslinked Nanoparticulate Chondroitin Sulfate/Chitosan Polyelectrolyte Complexes

“…CS has been applied for sitespecific drug delivery to the colon [3] and osteoarthritis. [4] Though there are many promising properties of CS that can be used for DDS, unfortunately, its highly soluble character under physiological conditions limits its application as a solid state drug carrier. Owing to its anionic character, the formation of PECs through electrostatic interactions with an oppositely charged substance may be an alternative strategy for maintaining CS in a solid form for DDS.…”