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Screening of poly-beta amino ester coated emulsion of ketorolac for cartilage delivery
Tahani Saeedi1, Polina Prokopovich1
1Cardiff School of Pharmacy and Pharmaceutical Sciences, Cardiff, UK. prokopovichp@cf.ac.uk.
Abstract:
Osteoarthritis (OA) is a prevalent chronic health condition necessitating effective treatment strategies. Globally, there were 86 million people with incident knee osteoarthritis in 2020. Pain management remains the primary approach to OA as the nature of cartilage poses challenges for drug delivery. An emulsion-based delivery system, using a class of positively charged and hydrolysable polymers (poly-beta-amino-esters) to coat oil droplets containing drugs, has been shown to enhance and prolong drug localization in ex vivo cartilage models. As the properties of the polymers used in this technology strongly depend on the monomers used in the synthesis, this study presents the screening of a wide range of PBAEs as droplet coating agents and using ketorolac as a model of nonsteroidal anti-inflammatory drugs. The emulsions prepared with this PBAE library were characterized, and drug localisation and retention were evaluated in both native and glycosaminoglycan (GAG) depleted cartilage ex vivo models. Optimal candidates were identified and tested in an ex vivo model showing the ability to protect chondrocyte cell viability and increase both GAG and collagen contents in cartilage exposed to cytokine (IL-1α) simulating acute cartilage damage. This work demonstrates the potential of PBAE coated emulsion as a delivery system for effective drug delivery in OA treatment.
Insights
This study developed a novel poly-beta-amino-ester (PBAE) coated emulsion for osteoarthritis treatment. This advanced drug delivery system enhances drug localization in cartilage, protecting chondrocytes and promoting cartilage repair.
Area of Science:
- Biomaterials Science
- Drug Delivery Systems
- Osteoarthritis Research
Background:
- Osteoarthritis (OA) affects millions globally, with pain management being the primary treatment due to cartilage's drug delivery challenges.
- Current treatments struggle with effective drug localization and retention within cartilage tissue.
- Emulsion-based systems offer potential, but polymer properties are critical for efficacy.
Purpose of the Study:
- To screen poly-beta-amino-esters (PBAEs) as droplet coating agents for enhanced drug delivery in osteoarthritis.
- To evaluate the drug localization and retention capabilities of PBAE-coated emulsions in cartilage models.
- To assess the therapeutic potential of optimized PBAE emulsions in protecting chondrocytes and promoting cartilage repair.
Main Methods:
- Synthesis and characterization of a library of PBAEs for emulsion coating.
- Preparation of ketorolac-loaded emulsions using selected PBAEs.
- Evaluation of drug localization and retention in ex vivo native and GAG-depleted cartilage models.
- Assessment of chondrocyte viability and cartilage matrix content (GAG and collagen) in IL-1α-stimulated cartilage models.
Main Results:
- A library of PBAEs was screened, and optimal candidates for emulsion coating were identified.
- PBAE-coated emulsions demonstrated enhanced and prolonged drug localization within cartilage tissue.
- The optimized system protected chondrocyte viability and increased GAG and collagen content in damaged cartilage models.
Conclusions:
- PBAE-coated emulsions represent a promising strategy for effective drug delivery in osteoarthritis treatment.
- This delivery system shows potential for enhancing cartilage repair and protecting chondrocytes.
- Further development could lead to improved therapeutic outcomes for osteoarthritis patients.
