FORMULATION AND EVALUATION OF NOVEL INSITU GEL SYSTEM IN THE MANAGEMENT OF RHEUMATOID ARTHRITIS

Abstract

Objective: To develop in-situ gel formulations of Lornoxicam for sustained release to reduce the dosing frequency in the treatment of rheumatoid arthritis. Methods: The method of ion-sensitive in-situ gel formation was used in this study. Lornoxicam in situ gel formulations were prepared by varying concentrations of sodium alginate as a bio-degradable gel-forming polymer, CaCl2 as a cross-linking agent, and chitosan, HPMCK4, HPMCK15, guar gum, gellan gum, xanthan gum, pectin were used as drug release rate controlling polymers. The formulations F11-F18 were assessed for physical appearance, pH, in vitro drug release, viscosity, in vitro gelling capacity, and drug content. FTIR, DSC, and in vivo drug kinetics studies were conducted for lornoxicam pure drug and optimized formulation. Results: Formulations showed an optimum viscosity that will allow ease of administration and swallowing. All formulations were shown pH between 6.7 to 7.3, floating lag time was 2-3 sec and floated for 12 h. In vitro, drug release studies were reporting that commercial sustained release formulation of lornoxicam released 99.92% drug in 8 h, and optimized formulation F11 released 99.52% of the drug over a 12 h extended period. FTIR studies revealed no interaction between drugs and excipients used. The results of in vivo kinetic studies are approving the better performance of the optimized formulation. The Cmax, Tmax, t1/2, and AUC values are confirming the same thing. Conclusion: Lornoxicam oral in situ gel containing chitosan as a drug release controlling polymer is a promising approach for the treatment of rheumatoid arthritis in a convenient dosage form with better patient compliance and therapeutic response.