A Design and Development of Deflazacort pH Transition Injectable in-situ Implant for Rheumatoid Arthritis

Abstract

  Introduction: Rheumatoid arthritis is a chronic inflammatory disorder causing painful swelling and damaging various body systems. Deflazacort is a drug of choice for the treatment, but it exhibits lower mineral corticoid activity and lower bioavailability when administered orally. The novel formulation is required to achieve a successful release rate in a well-controlled manner and facilitate the drug's uptake. Methods: The in situ injectable implants prepared has the solution following cold method using drug deflazacort with Carbopol 934P, Hydroxy Propyl Methyl Cellulose K4M, Hydroxy Propyl Methyl Cellulose K15 M undergo a rapid transition to gel state by external stimuli like pH. The fabricated formulations were evaluated for pH measurement, rheological study, drug content, gelling capacity, in vitro permeability studies, and release kinetics. Results: Among all the batch formulations, F14, F17, and F18 exhibited good gelling properties and optimum viscosity. In vitro permeation studies of F14 showed drug release of 95.45% in 24 h. Further, the drug diffusion data of F14 revealed that it followed the Higuchi model, which suggests that the drug release occurred followed Non- Fickian diffusion kinetics which is ideal for injectable in situ implant formulations. Conclusion: The present study concluded that deflazacort injectable in situ implant formulations inhibit the initial burst release and sustain the drug delivery for 24 hours when administered intramuscularly or subcutaneously.