A pH-triggered delayed-release chronotherapeutic drug delivery system of aceclofenac for effective management of early morning symptoms of rheumatoid arthritis

Abstract

Context: Rheumatoid arthritis (RA) is differentiated as an early morning exacerbation of the core arthritis condition associated with increase in pain and stiffness in joints and necessitate for medication. Objective: The aim of the present work was to develop and optimise a pH-triggered delayed-release colon-specific aceclofenac microspheres and to accomplish chronotherapy of RA. Methods: A 3-factor, 3-level Box–Behnken design (BBD) was used to optimise selected variables. Developed formulation was evaluated for in vivo delayed response and anti-arthritis activity in rats. Results: The particle size and encapsulation efficacy of these microspheres were 117.36 ± 10.54 µm and 85.06 ± 5.85%, respectively. Optimised formulation was analysed by SEM, DSC, X-RPD and FTIR. The in vivo evaluation reveled delayed anti-inflammatory activity in carrageenan-induced rats and anti-arthritic activity in freund’s adjuvant-induced arthritis rats. Conclusion: The optimised aceclofenac microspheres formulation is potential for the chronotherapy of early morning symptoms of RA.

• Aceclofenac
• Box–Behnken design
• colon delivery
• delayed release
• eudragit S-100

Acknowledgements

All the authors are thankful to Dr Vasudha Bakshi, Head of the Institution, Prof. Prakash V. Diwan, Director and Dr Palla Rajeshwar Reddy, Chairman, School of Pharmacy, Anurag Group of Institutions, Hyderabad for their continuous support and providing research facilities.

Declaration of interest

The authors report no conflicts of interest.