Abstract

Implants are readily applied as a convenient method of therapy. There is great interest in the prolonged release of active substances from implants. The objective of this work was to evaluate the dissolution kinetics of steroidal anti-inflammatory preparation (SAP) released from novel implants, and to test the influence of the technology on SAP release kinetics. The proposed long-acting preparations may overcome difficulties resulting from repeated injections and often visits to ambulatory clinic, as the stabilizing function of the artificial ligament would be enriched with pharmacological activity. The potential advantages provided by the new coatings of knee implants include the continuous, sustained, and prolonged release of an active substance. The study was carried out using a modified United States Pharmacopoeia (USP) apparatus 4. The amount of SAP was measured spectroscopically. It was revealed that the transport of the drug was mainly a diffusion process. The drug release kinetics was analyzed using zero-, first-, and second-order kinetics as well as Korsmeyer-Peppas, Higuchi, and Hixon-Crowell models. The highest values of the release rate constants were k0 = (7.49 ± 0.05) × 10−5 mg × min−1, k1 = (6.93 ± 0.05) × 10−6 min−1, and k2 = (7.70 ± 0.05) × 10−7 mg−1 × min−1 as calculated according to zero-, first-, and second-order kinetics equations, respectively. The values of the rate constants obtained for the slowest process were k0 = (3.63 ± 0.06) × 10−5 mg × min−1, k1 = (2.50 ± 0.03) × 10−6 min−1, and k2 = (2.80 ± 0.03) × 10−7 mg−1 × min−1. They may suggest the possibility of sustained release of betamethasone from the system. Due to the statistical analysis, differences were observed between most of the studied implants. Incubation, temperature, time of stabilization of layers, and the method of SAP deposition on the matrix affected the drug release.

Highlights

  • The optimal mechanical properties of musculoskeletal joints are ensured by cartilage and synovial fluid

  • The Korsmeyer-Peppas model was unsuitable for describing the release of the drug from implant F, and the Hixon-Crowell model was inappropriate to reflect the dissolution of steroidal anti-inflammatory preparation (SAP) from implants A and C

  • It could be concluded that diffusion was the dominant mechanism of betamethasone release from implants A–E

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Summary

Introduction

The optimal mechanical properties of musculoskeletal joints are ensured by cartilage and synovial fluid. The failure of these tissues as a result of various arthritis forms leads to the development. Materials 2019, 12, 1202 of diseases [1,2]. For the treatment of osteoarthritis (OA), non-steroidal and anti-inflammatory drugs (NSAIDs) are most commonly used [3,4]. The long-term use of painkillers and anti-inflammatory drugs can reduce the symptoms of illness but at the same time can accelerate the destruction of joints. Not just its symptoms, increases the recovery chance.

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