ArtMic™

ArtMic™ a DDS for OA

Until now no curative treatment is known for Osteoarthritis. The current pharmacological guidelines for Osteoarthritis management are based on oral treatments by analgesics or non-steroidal anti-inflammatory drugs and on intra-articular treatments in the aim to reduce pain and restore functions.

Due to rapid clearance of drugs in joint cavity, intra-articular injection of drug delivery systems (DDS) represents a solution to achieve a sustained release of drugs in joint cavity over several weeks or months. Intra-articular drug delivery using microspheres (MS) is still an experimental approach and clinical stage has not yet been reached.

 

Intra-articular MS described until now present in general 2 major limitations: an inflammatory response of joint tissue to injected materials and a too rapid drug delivery.

 

Occlugel has developed ArtMic™, for Intra-articular sustained drug delivery of anti-inflammatory drugs, with the objective to make it as less inflammatory as possible and slowly degradable.

  • Inflammatory response of joint tissue to ArtMic™, and their degradation were analysed after injection in the joint cavity of healthy sheep. One week after intra-articular injection, histological analysis indicated that ArtMic™ were localized beneath the synovial lining of joint capsule tissue. ArtMic™ were well tolerated by synovial tissue in the sheep model since their entrapment within synovium did not induce cell proliferation around particles and they did not enhance prostaglandins concentration in synovial fluid.
  • Degradation of ArtMic™, which parallels the drug delivery, was tuned from one day to 3 months to cover optimally the period of time of pain and inflammation which could vary clinically.

ArtMic™ seem suitable for long term sustained release of drugs in synovial tissue thanks to their synovial entrapment, the low intensity of the inflammatory reaction they triggered in synovium and their tunable degradation which achieves a delivery ranging from days to months. 

Bibliography

Bédouet, L., Moine, L., Pascale, F., Nguyen, VN., Labarre, D., Laurent, A. 2014. Synthesis of hydrophilic intra-articular microspheres conjugated to ibuprofen and evaluation of anti-inflammatory activity on articular explants. Int. J. Pharm. 459, 51-61

Bédouet, L., Pascale, F., Moine, L., Wassef, M., Ghegediban, SH., Nguyen, VN., Bonneau, M., Labarre, D., Laurent, A. 2013. Intra-articular fate of degradable poly(ethyleneglycol)-hydrogel microspheres as carriers for sustained drug delivery. Int. J. Pharm. 456, 536-544.