Oral bioavailability of chondroitin sulfate (Condrosulf®) and its constituents in healthy male volunteers

Volpi, Nicola

doi:10.1053/joca.2002.0824

Cited by 132 publications

(127 citation statements)

References 40 publications

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“…The concentrations of glcN in serum after oral and intravenous administration range from 1 to 20 mg/mL, while CS concentrations are in the 5-200 mg/mL range. [25][26][27] Yet, ongoing studies from our laboratory do show some reductions in the cyclic load-induced degradation of a chondral explant for even a reduced (by 50%) concentration of supplement, and yet, it seems inviting to propose in vivo studies at clinical concentrations to see if this supplement may have incremental, positive effects on the already documented effects of physiological levels of cyclic loading on changes in the mechanical properties of joint cartilage. 5 Another potential utility for these types of in vitro studies may be in the area of tissueengineered cartilage.…”

Section: Discussionmentioning

confidence: 99%

High levels of glucosamine–chondroitin sulfate can alter the cyclic preload and acute overload responses of chondral explants

Wei

Haut

2009

Journal Orthopaedic Research

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A recent study by our laboratory showed that 14 days of low intensity, intermittent cyclic preloading of chondral explants elevated the concentration of proteoglycans (PGs) to cause a mechanical stiffening of the explants prior to an acute overload and limit the extent of tissue damage. Longer term loading to 21 days resulted in tissue degradation prior to the acute traumatic event and excessive damage from an acute overload. Previous studies by others showed that bathing chondral explants in a supplement of glucosaminechondroitin sulfate (glcN-CS) upregulated the synthesis of tissue PGs, particularly in stressed tissue, and the supplement served as an antiinflammatory agent. Our current hypothesis was that the supplementation of culture media with a high concentration of glcN-CS would upregulate the production of tissue PG and limit or mitigate long-term degradation of chondral explants under cyclic preloading and limit tissue damage in an acute overload. We showed that, in the presence of supplement, cyclic preloading significantly increased tissue PG content and matrix modulus by about 65 and 300%, respectively, at 21 days, resulting in a reduction of matrix damage and cell death following an acute overload. These data show a biological action of high concentrations of this supplement and its effect on the mechanical properties in this in vitro model. In vitro studies of impact loading 1,2 on cartilage show cell death and matrix damage. In contrast, in vitro and in vivo studies showed positive aspects of low intensity, intermittent compressive loading, such as increased biosynthesis of proteoglycans (PGs). [3][4][5] Changes in PG and collagen contents of cartilage significantly alter the mechanical properties of this tissue. 6 Thus, it is reasonable to assume that cyclic preloading of cartilage can alter its mechanical properties and help determine the extent of matrix damage and cell death that will occur due to the blunt force overloading of a joint, such as during an acute knee ligament rupture. 7 Recent studies in our laboratory show that low intensity, intermittent cyclic preloading of chondral explants prior to an acute overload yields an increase in the synthesis of tissue PGs, resulting in a less severe traumatic insult for an acute overload. 8 Between 14 and 21 days of cyclic preloading, the explants experience a significant PG loss that leads to a dramatic loss in mechanical properties. Acute overloading of the explanted tissue then yields matrix damage and cell death significantly greater than nonpreloaded controls. A recent study by others shows a significant loss of tissue PG and cell death with production of matrix metalloproteinase (MMP-3) adjacent to damaged collagen fibers under cyclic compression at 0.5 Hz for intensities of 1 and 5 MPa over 24 h. 9 Similarly, under 0.5 MPa of 1 Hz cyclic loading, a significant increase in the MMP-2 and -9 synthesis was found after 3 h. 10 The combination of glucosamine-chondroitin sulfate (glcN-CS) was shown in in vitro studies to function as a ''...

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Section: Discussionmentioning

confidence: 99%

High levels of glucosamine–chondroitin sulfate can alter the cyclic preload and acute overload responses of chondral explants

Wei

Haut

2009

Journal Orthopaedic Research

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“…[7][8][9][10] Furthermore, glycosaminoglycans with a low molecular mass and charge density are preferentially absorbed. 8,11) In case of CS, some reports have been issued concerning its oral administration, metabolisms and chondroprotective function in arthritis.…”

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confidence: 99%

Effects of Low Molecular Weight Chondroitin Sulfate on Type II Collagen-Induced Arthritis in DBA/1J Mice

Cho

Sim

Jeong

et al. 2004

Biological & Pharmaceutical Bulletin

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Chondroitin sulfate (CS) is a glycosaminoglycan, which is composed of an alternating sequence of sulfated and/or unsulfated residue of D-glucuronic acid (GlcA) and D-N-acetylgalactosamine (GalNAc) linked by b(1→3) and b(1→4) bonds.1) CS is a major class of glycosaminoglycans required for the formation of proteoglycans found in the joint cartilage. It has been well established that basic damage to the arthritic cartilage involves the alteration of proteoglycans and collagen fibers.

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“…The pharmacokinetic parameters of CS determined in healthy male volunteers [Volpi, 2002] after oral administration showed a significant increase in CS plasma levels (more than 200%) compared with predose levels over a 24-h period. The peak concentrations were observed 2 h after dosage and the increase is significant from 2 to 6 h after dosage.…”

Section: Introductionmentioning

confidence: 93%

“…Indeed, desulfated chondroitin in mouse [Kusano et al 2007] has a very rapid uptake, with a peak occurring within 15 min and a very rapid clearance returning to baseline after 3 h, whereas shark CS in male healthy volunteers has a slower uptake (peak at 8.7 h) and slower clearance (levels maintained until 16 h postadministration) [Volpi, 2003]. CS from bovine trachea presents a rapid increase in plasma of male healthy volunteers with a peak within 1 5 h after administration and a return to baseline after 10 h [Volpi, 2002].…”

Section: Introductionmentioning

confidence: 99%

Chondroitin sulfate in the treatment of osteoarthritis: from in vitro studies to clinical recommendations

Henrotin

Mathy

Sanchez

et al. 2010

Therapeutic Advances in Musculoskeletal

150

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Chondroitin sulfate (CS) is recommended as a therapeutic intervention in the multimodal approach of osteoarthritis (OA) management. CS has been studied extensively to describe its pharmacology (pharmacokinetic, in vitro and in vivo effects) and its clinical efficacy. Various results have been reported depending on the system of evaluation (model, dosage and duration) and the source of CS (origin and quality). The purpose of this review was to gather most of the available information about CS and to discuss its potency in OA management.

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Oral bioavailability of chondroitin sulfate (Condrosulf®) and its constituents in healthy male volunteers

Abstract: From this study and literature data, it appears that exogenous chondroitin sulfate (Condrosulf) is absorbed as a high molecular mass polysaccharide together with derivatives resulting from a partial depolymerization and/or desulfation.

Cited by 132 publications

References 40 publications

High levels of glucosamine–chondroitin sulfate can alter the cyclic preload and acute overload responses of chondral explants

High levels of glucosamine–chondroitin sulfate can alter the cyclic preload and acute overload responses of chondral explants

Effects of Low Molecular Weight Chondroitin Sulfate on Type II Collagen-Induced Arthritis in DBA/1J Mice

Chondroitin sulfate in the treatment of osteoarthritis: from in vitro studies to clinical recommendations

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