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Updated: Nov 10, 2025

Characterization of Intra-Cartilage Transport Properties of Cationic Peptide Carriers
Published on: August 10, 2020
Candidates for Intra-Articular Administration Therapeutics and Therapies of Osteoarthritis
Eriko Toyoda1,2, Miki Maehara1,2, Masahiko Watanabe1,2
1Department of Orthopaedic Surgery, Surgical Science, Tokai University School of Medicine, 143 Shimokasuya, Isehara 259-1193, Japan.
Abstract:
Osteoarthritis (OA) of the knee is a disease that significantly decreases the quality of life due to joint deformation and pain caused by degeneration of articular cartilage. Since the degeneration of cartilage is irreversible, intervention from an early stage and control throughout life is important for OA treatment. For the treatment of early OA, the development of a disease-modifying osteoarthritis drug (DMOAD) for intra-articular (IA) injection, which is attracting attention as a point-of-care therapy, is desired. In recent years, the molecular mechanisms involved in OA progression have been clarified while new types of drug development methods based on gene sequences have been established. In addition to conventional chemical compounds and protein therapeutics, the development of DMOAD from the new modalities such as gene therapy and oligonucleotide therapeutics is accelerating. In this review, we have summarized the current status and challenges of DMOAD for IA injection, especially for protein therapeutics, gene therapy, and oligonucleotide therapeutics.
Insights
Disease-modifying osteoarthritis drugs (DMOADs) delivered via intra-articular injection are crucial for managing knee osteoarthritis. This review explores novel protein, gene, and oligonucleotide therapeutics for early-stage OA treatment.
Area of Science:
- Biomedical Engineering
- Pharmacology
- Orthopedics
Background:
- Knee osteoarthritis (OA) significantly impairs quality of life due to irreversible articular cartilage degeneration.
- Early intervention and lifelong management are critical for effective OA treatment.
- Intra-articular (IA) injection offers a promising point-of-care therapy for early OA.
Purpose of the Study:
- To review the current status and challenges of disease-modifying osteoarthritis drugs (DMOADs) for IA injection.
- To focus on emerging DMOAD modalities including protein therapeutics, gene therapy, and oligonucleotide therapeutics.
- To highlight advancements in treating early-stage knee OA.
Main Methods:
- Literature review of recent advancements in OA drug development.
- Analysis of molecular mechanisms underlying OA progression.
- Evaluation of novel therapeutic modalities for intra-articular delivery.
Main Results:
- Significant progress has been made in understanding OA molecular mechanisms.
- New drug development platforms based on gene sequences are established.
- Development of DMOADs using protein therapeutics, gene therapy, and oligonucleotide therapeutics is accelerating.
Conclusions:
- Novel therapeutic strategies are essential for managing irreversible cartilage degeneration in OA.
- IA injection of DMOADs represents a key area for future OA treatment.
- Continued research into protein, gene, and oligonucleotide therapeutics is vital for advancing OA care.

