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.

Advances in Ameliorating Rheumatoid Arthritis by Andrographolide Ethosome-Based Gel: Pharmacokinetic and Activity Study in Rats

“…These anti-arthritis studies aim to collect data on the efficacy of ethosomal andrographolide transdermal formulations in rheumatoid arthritis animal models. Rheumatoid arthritis is an autoimmune disease characterized by inflammation, progressive bone erosion, and cartilage damage, leading to synovial hypertrophy [35]. Therefore, the CFA model, which is the most extensively studied autoimmune model of the condition, was produced in Sprague Dawley rats.…”

Formulation and Characterisation of Gastroretentive in Situ Gel Loaded With Glycyrrhiza Glabra L. Extract for Gastric Ulcer

“…All the in situ gel formulations had a floating lag time of less than 2 min and floated for more than 12h shown in table 4. Therefore, the extended duration of floating was responsible for the sustained release of drugs from the in situ gel formulations [28]. The percentage of drug content of all the formulations was in the range of 83.55 to 95.…”

“…The in situ released calcium ion from the calcium citrate complex gets entrapped in polymeric chains, resulting in the cross-linking of polymeric chains to form a gel matrix. Thus, stiff gels were formed with formulations containing high concentrations of sodium alginate and gellan gum [28]. The viscosity order of the formulations from F1 to F10 is F1˂ F2˂ F4˂ F10˂ F7˂ F6˂ F3˂ F5˂ F9˂ F8 as shown in table 1.…”

Formulation Development and Characterization of Lafutidine Raft System

“…Pure drug i.e. Lafutidine was analysed using Differential scanning calorimetry; correspondingly, the physical mixture and the physical form of raft systems were also analysed and reported to evaluate any passivity of drug-excipient interaction [14].…”

“…IR spectra for pure lafutidine and with polymer were taken. FTIR spectra was run with the pellets prepared by KBr pellet method of pure drug, and with excipients, were recorded over a range of 4000-400 cm-1 [14].…”