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Characterization of Intra-Cartilage Transport Properties of Cationic Peptide Carriers
Published on: August 10, 2020
Cartilage-targeted drug nanocarriers for osteoarthritis therapy
Luca Morici1, Eric Allémann1, Carlos Rodríguez-Nogales1
1School of Pharmaceutical Sciences, University of Geneva, Rue Michel-Servet 1, 1206 Geneva, Switzerland; Institute of Pharmaceutical Sciences of Western Switzerland, Rue Michel-Servet 1, 1206 Geneva, Switzerland.
Abstract:
Osteoarthritis (OA) is a joint disease common worldwide. Currently, no disease-modifying osteoarthritis drugs (DMOADs) have successfully passed clinical trials, often due to a lack of cartilage penetration. Thus, targeting the extracellular matrix (ECM) is a major priority. The design of cartilage-targeting drug delivery systems (DDSs) for intra-articular administration requires consideration of the physicochemical properties of articular cartilage, such as its porosity and negative fixed charge. Various positively charged biomaterials such as polyaminoacids, proteins, polymers, and lipids can be used as DDSs to enhance cartilage penetration. Cationic nanocarriers interact electrostatically with anionic glycosaminoglycans of the ECM, ensuring passive cartilage-targeting penetration and prolonged retention. Active targeting strategies involve DDSs surface decoration using antibodies or peptides with a strong affinity for collagen II and chondrocytes in the cartilage. This review presents all the relevant bio-physicochemical properties of healthy and OA cartilages, as well as state-of-the-art intra-articular cartilage-targeted DDSs, intending to better understand the recent advances in the application of cartilage-targeting delivery systems for OA therapy.
Insights
Developing effective osteoarthritis treatments requires overcoming cartilage penetration challenges. This review explores cartilage-targeting drug delivery systems (DDSs) using positively charged biomaterials for enhanced osteoarthritis therapy.
Area of Science:
- Biomaterials Science
- Drug Delivery
- Osteoarthritis Research
Background:
- Osteoarthritis (OA) is a prevalent global joint disease with no current disease-modifying drugs (DMOADs) due to poor cartilage penetration.
- Targeting the extracellular matrix (ECM) is crucial for OA therapy, necessitating specialized drug delivery systems (DDSs).
Purpose of the Study:
- To review the physicochemical properties of healthy and OA cartilage.
- To explore state-of-the-art intra-articular cartilage-targeted DDSs for OA therapy.
- To understand recent advances in DDSs for OA treatment.
Main Methods:
- Review of physicochemical properties of articular cartilage (porosity, negative charge).
- Analysis of positively charged biomaterials (polyaminoacids, proteins, polymers, lipids) for DDSs.
- Evaluation of passive (electrostatic interaction with GAGs) and active (antibody/peptide targeting) strategies for cartilage penetration.
Main Results:
- Positively charged DDSs leverage cartilage's negative charge for enhanced penetration and retention.
- Cationic nanocarriers interact electrostatically with ECM glycosaminoglycans.
- Active targeting via surface decoration with collagen II/chondrocyte-affinity molecules shows promise.
Conclusions:
- Understanding cartilage bio-physicochemical properties is key for designing effective DDSs.
- Positively charged DDSs offer a viable strategy for improving intra-articular drug delivery in OA.
- Advances in cartilage-targeted DDSs are critical for developing novel OA therapeutics.
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