Improving osteoarthritis treatment through facilitated transport of bisphosphonates to chondrocytes by vitamin C

Value Proposition

Osteoarthritis is the most prevalent of all forms of arthritis and the second greatest cause of disability worldwide. The Centers for Disease Control and Prevention estimates that osteoarthritis affects over 30 million adults in the US. The cells which store and produce cartilage, chondrocytes, are therapeutic targets treating osteoarthritis. Bisphosphonates have chondroprotective effects, however the inability to target high levels of bisphosphonates into chondrocytes limits their protective potential.

Technology

Duke researchers have discovered a novel method for enhancing drug delivery to chondrocytes. This delivery method results in higher intracellular concentrations using lower loading doses, thereby eliminating the need for high doses of therapeutic compounds. Therapies for intra-articular diseases like osteoarthritis, where optimal drug access to avascular tissue is needed, will particularly benefit. Duke’s proprietary technology would safely enhance delivery of bisphosphonates facilitating improved treatment of osteoarthritis. Due to the transporter system used, various therapeutic agents could be coupled to this chaperone to enhance delivery into chondrocytes. In addition to intra-articular administration, this chaperone has the potential to enhance gastrointestinal absorption of oral bisphosphonates for the treatment of osteoporosis. Enhanced gastrointestinal absorption of chaperone-coupled bisphosphonates would provide the potential for therapeutic effectiveness at much lower oral doses compared with non-chaperone coupled bisphosphonates, thereby reducing the incidence of the gastrointestinal side effects associated with oral bisphosphonates.

Other Applications

This technology could be a platform for developing treatments for a variety of other diseases including Paget’s disease, abnormally increased bone turnover, periodontal disease, tooth loss, bone fractures, metastatic bone disease, hypercalcemia of malignancy, multiple myeloma, and chondrosarcoma.

Advantages

  • Improves cartilage uptake of active agents for treating joint diseases such as osteoarthritis and rheumatoid arthritis
  • Could reach therapeutic effectiveness with lower oral doses of bisphosphonates
  • A platform that could also be used to improve the uptake of imaging agents