Abstract

FORMULATION AND EVALUATION OF DIACEREIN IMPLANTABLE IN SITU GEL FOR THE TREATMENT OF OSTEOARTHRITIS

Prof. Dr. A. Abdul Hasan Sathali* and A. Mohamed Noufal

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Abstract

Osteoarthritis is the most common form of arthritis and the leading cause of disability, with an unmet clinical need for symptomatic treatment. Diacerein inhibits the association with the activity of interleukin 1-β and is useful in the symptomatic treatment of osteoarthritis but also causes diarrhoea when administered orally. Diacerein has rapid clearance due to its short half-life and thus ensures the use of a sustained release formulation for long-term use to improve its patient compliance. Unlike other joint diseases, Osteoarthritis is localized in one or a few joints, which offers a unique opportunity for local Intra-articular treatment without the risk of systemic side effects. To avoid drug-related toxicity and ineffective anti- inflammatory drugs, there is an urgent need for an improved delivery system that increases bioavailability. The potential for Diacerein in-situ gel as an effective treatment for Osteoarthritis was investigated. It is composed of poloxamer 407 as the main polymer, hydroxypropyl methylcellulose K4, and carbopol 934 as the copolymer prepared by the traditional cold method and is characterized by various parameters. All characterization showed satisfactory results. In vitro drug release is performed using phosphate buffer pH 7.4 indicating controlled drug release. In addition, the distribution of Diacerein was even in a sterile and injectable in situ gel.

Keywords: Diacerein, In situ gel, Osteoarthritis, Intra-articular injection, Thermoresponsive gel.