Formulation and Evaluation of Diacerein Implantable in Situ Gel for the Treatment of Osteoarthritis

Mohamed Noufal, A (2021) Formulation and Evaluation of Diacerein Implantable in Situ Gel for the Treatment of Osteoarthritis. Masters thesis, College of Pharmacy, Madurai Medical College, Madurai.

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Abstract

The purpose of this research was to develop a novel injectable, biodegradable in situ drug delivery system of diacerein for the management of osteoarthritis. ❖ Twelve formulations of diacerein in situ gelling systems were prepared with thermo sensitive polymer Poloxamer-407 (10%) and other copolymers such as HK4M (0.5-1.5%), Carbopol 394 (0.5-1.5%) by traditional “cold method”. Diacerein is a semi-synthetic anthraquinone derivative used for the treatment of osteoarthritis kept as constant for each formulation (5% w/v). ❖ The formulated in situ gelling system were characterized for appearance, colour, pH, gelation temperature, gelation time, syringeability time, viscosity study and in vitro drug release. ❖ All the 12 formulations were clear and yellow in colour. ❖ The pH of all the formulations was in range from 7.0 to 7.4 and found to be satisfied. ❖ The prepared diacerein in-situ gels showed sol-to-gel transformation. The gelation temperatures were in the range of 34.8℃ to 37.3℃ and showed that the gelation times were in the range of 58 to 68 seconds. ❖ The formulations showed better syringeability time which can be easily injectable as injection into the synovial fluid. ❖ All the formulations showed the better viscosity behaviour at both refrigerator temperature and body temperature which was found to be in satisfactory range. ❖ The cumulative percentage of drug release of the prepared in situ gels was found to be in satisfactory range. The formulations F8, F9 and F12 were selected based on the long sustained release at 24 hours period of time. ❖ Formulation F8 showed the best controlled release and also possessed the optimum physiochemical behaviour such as gelation temperature, gelation time, syringeability time and viscosity. ❖ Based on the physiochemical behaviours such as gelation temperature, gelation time, syringeability time and viscosity and in vitro drug release formulation F8 was considered as best formulation. ❖ Isotonicity test was carried out for prepared diacerein in-situ gels F8 exhibited no change in the shape of blood cells (bulging or shrinkage) which reveals the isotonic nature of the formulation. ❖ Best formulation F8 was sterilized by gamma irradiation and accessed for sterility test. The microbiological evaluation assured the product’s sterility. ❖ The effect of gamma irradiation on gelation temperature, gelation time, syringeability time, drug release in vitro and drug content was evaluated and no significant changes in the said parameter between non-irradiated and irradiated formulations. ❖ The FTIR results proved that no interactions between the drug and polymers of in situ gelling system. ❖ The methodology adopted for the in situ gelling system is easy, convenient and cost effective. ❖ A novel drug delivery system for prolonged release of diacerein which can reduce dose, dosing frequency, associated side effects, cost of therapy and there by improve patient compliance was developed. ❖ This research demonstrated advantages of diacerein in-situ gel and may be suitable as an injectable drug delivery system for management of osteoarthritis to overcome the limitations of currently available formulation.

Item Type: Thesis (Masters)
Additional Information: 261911302
Uncontrolled Keywords: Formulation, Evaluation, Diacerein Implantable Situ Gel, Treatment, Osteoarthritis.
Subjects: PHARMACY > Pharmaceutics
Depositing User: Ramakrishnan J
Date Deposited: 15 Aug 2022 06:27
Last Modified: 18 Aug 2022 02:28
URI: http://repository-tnmgrmu.ac.in/id/eprint/20774

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