Lacosamide protected cartilage in preclinical tests — ScienceDaily

Yale researchers found that the epilepsy drug lacosamide may simultaneously reduce pain and curb cartilage damage in osteoarthritis in preclinical studies, ScienceDaily reports.

A target for pain and cartilage destruction

The study, published in the journal Bioactive Materials, focuses on the Nav1.7 protein — a sodium channel involved in transmitting electrical signals in cells. It was previously associated primarily with nerve cells that transmit pain signals. The research team also found high Nav1.7 activity in chondrocytes — cells that maintain cartilage tissue.

In osteoarthritis, Nav1.7 activity rises substantially. According to the researchers, this may simultaneously intensify pain signals and contribute to cartilage destruction. Study leader Chuan-Ju Liu noted that blocking this protein could potentially affect both pain and the processes of joint degeneration.

The effect depended on the dose

The scientists tested drugs that inhibit sodium channels and identified lacosamide as a promising option. At an optimal low concentration, it stimulated the production of proteins associated with cartilage formation and suppressed tissue-destruction processes. At excessively high or excessively low concentrations, this effect weakened.

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Additionally, lacosamide stimulated the release of the signaling proteins HSP70 and midkine. HSP70 helps cells respond to stress and supports tissue repair, while midkine is involved in regulating inflammation and protecting joint tissue.

A hydrogel for sustained release

For local administration of the drug, the team created a temperature-sensitive hydrogel based on type II collagen. In a cool syringe, it remains liquid, but at body temperature it turns into a gel-like material. This gel retains lacosamide in the joint and gradually releases it over several weeks.

In the same preclinical studies, an injection of the lacosamide-containing gel once every four weeks prevented cartilage loss more effectively than daily oral use of the drug. Lacosamide is already approved for use in people with epilepsy, which, according to the study authors, may speed up the transition to clinical studies of osteoarthritis treatment.