A novel Diclofenac-carrier for local treatment of osteoarthritis applying live-animal MRI

Journal of Controlled Release : Official Journal of the Controlled Release Society
Inbar Elron-GrossR Margalit

Abstract

The prevailing chronic treatment for osteoarthritis--oral administration of NSAIDs--is accompanied by severe adverse effects and risks of gastrointestinal (GI) toxicity. The working hypothesis of this study was that increased NSAID-efficacy and alleviation of adverse effects can be achieved by local administration of a new slow-release NSAID-carrier formulation. Diclofenac was the test NSAID and collagomers--novel vesicular-shaped microparticles based on collagen-lipid conjugates--were the carriers. Collagomers were stable in simulated synovial fluid and showed: high-efficiency drug encapsulation (85%); slow drug release (tau((1/2))=11 days); high affinity to target cells (Kd=2.6 nM collagen). In vitro activity of Diclofenac released from the carriers was similar to fresh drug solutions. Diclofenac-collagomer therapeutic effects were studied in osteoarthritis-induced rats, using live-animal MRI. A single intra-articular injection of the Diclofenac-collagomer formulation reduced inflammation over 3 weeks significantly vs. untreated animals (p<0.001), and vs. the conventional treatment which is free drug PerOs (p<0.03). Bypassing the GI, the novel treatment circumvents adverse effects of the conventional approach. In conclusion, ...Continue Reading

References

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Jan 31, 2008·Biochimica Et Biophysica Acta·Inbar Elron-GrossRimona Margalit
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Mar 14, 2008·International Journal of Pharmaceutics·Gregor CevcMatthias Rother

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Citations

Dec 7, 2013·Expert Opinion on Drug Delivery·Mi Lan Kang, Gun-Il Im
May 5, 2009·International Journal of Pharmaceutics·Inbar Elron-GrossRimona Margalit
Oct 5, 2010·British Journal of Pharmacology·Cf AlvesMh Napimoga
May 15, 2012·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Honglei XiLiang Fang
Oct 28, 2016·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Carolina Gómez-GaetePablo Torres-Vergara
Nov 12, 2016·Journal of Controlled Release : Official Journal of the Controlled Release Society·Maarten JanssenPieter J Emans
Aug 23, 2019·Journal of Materials Chemistry. B, Materials for Biology and Medicine·Yuejun YaoChangyou Gao
Oct 31, 2020·Advanced Drug Delivery Reviews·Marianna A TryfonidouLaura B Creemers
Mar 13, 2021·Advanced Therapeutics·Carlisle R DeJuliusCraig L Duvall

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