Targeting Joint

Creative Biolabs has persisted for many years in the field of targeted delivery system development. Armed with advanced platforms and professional technical team, Creative Biolabs has accumulated extensive experience in the successful completion of many targeted delivery projects for specific organs or tissues. Now we provide a variety of targeted delivery system-related products and services for the joint-related disease treatment and diagnosis to meet our clients’ requirements.

Rheumatoid arthritis (RA) is a typical systemic disorder characterized by chronic progressive inflammation and destruction of peripheral joint. It is an autoimmune disease due to tissue abnormality, localized damage in different parts of cartilage, bone, tendon and ligament. Over the last decades, significant progress has been achieved in understanding this disease. The main process in RA pathology is inflammatory activation of the synovium, the lining tissue of diarthrodial joints, tendon sheaths and bursae. The macrophages are activated by inflammatory cytokines, which then leads to joints swelling, cartilage damage, erosion of bone, functional impairment and stiffness. Subsequently, degradation of articular cartilage and subchondral bone occur, which is mediated by the release of matrix-degrading enzymes and activation of osteoclasts, resulting in joint destruction and disability eventually. RA is a frequently occurring disease, but understanding of the disease is still insufficient, which causes a big therapeutic challenge.

Fig.1 Schematic representation of healthy knee joint structure and pathological changes of knee osteoarthritis.¹

Delivery System Targeting Joint

The conventional drugs used in the treatment of RA include non-steroidal anti-inflammatory drugs (NSAIDs), steroids and disease-modifying anti-rheumatic drugs (DMARDs). However, indiscriminate distribution of agents and lack of specificity to the organs/tissues by systemic administration often cause extraarticular adverse effects. In addition, high and frequent dosing is essential due to short half-life and insufficient concentration of therapeutic agents in site of action, which also resulted in severe side effects as well as high cost. To overcome these limitations, new therapeutic strategies such as nanoparticles (NPs) have been developed.

Fig.2 Various nano-therapeutic strategies based on different nanoparticles for osteoarthritis (OA) treatment.²

• Example

Folate (FA) receptor β as targeting ligand is highly overexpressed on activated macrophages but is limited in normal tissues. A Methotrexate (MTX) loaded liposome targeted FA by using SP-DS3 peptide linker is applied in RA treatment. The results showed that FA targeting liposomes enhanced the specific internalization in activated macrophages expressing FA receptor-β. FA targeted liposomes strongly accumulated in joints and was effective in preventing the onset of arthritis in collagen-induced arthritis (CIA) model. The FA was also used in albumin NPs, which presented the ability to increase the specific delivery of etoricoxib (ETX) in rat carrageenan induced arteritis models. Hyaluronic acid (HA)-based nanoparticulate systems have been developed for targeted drug delivery in RA. Using HA-5b-cholanic acid (CA) to form polymeric micelles for specific delivery of c-secretase inhibitors (DAPT), the study showed more cellular uptake of Cy5.5-labelled HA-NPs in activated macrophages compared with non-activated macrophages.

What Can We Do for You?

Today, the targeted delivery system has emerged as a promising tool in the novel treatment and diagnosis of various diseases. Experienced in targeted delivery system design and development, Creative Biolabs has perfected technical pipelines to provide all kinds of module delivery systems for joint-related disease. We would like to share our knowledge and passion in this field to promote the advances of your projects and research. Please contact us for more information and a detailed quote.

References

1. Mao, Liwei, et al. "Targeted treatment for osteoarthritis: drugs and delivery system." Drug Delivery 28.1 (2021): 1861-1876.
2. Guo, Xinjing, et al. "Recent advances in nano-therapeutic strategies for osteoarthritis." Frontiers in Pharmacology 13 (2022): 924387.

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