METHODS: It was formulated using high pressure homogenization followed by probe sonication and formulation variables were optimized using Central Composite Design. The particle size (PS), zeta potential (ZP), entrapment efficiency (EE), drug release, cytotoxicity on NIH 3T3 fibroblasts cells and HaCaT keratinocytes cells and efficacy on RAW264.7 cells for optimized formulation was determined.
RESULTS: The PS, ZP and EE were found to be 85.26 nm, -23.7 ± 7.45 mV, 99.2 ± 2.62 % (Mes) and 84 ± 1.51 % (Cur), respectively. The good correlation between predicted and obtained value indicated suitability and reproducibility of experimental design. NLCs showed spherical shape as confirmed by TEM. In vitro drug release profile of prepared formulation showed that Mes exhibited 100 % release at 48 h, whereas Cur exhibited 82.23 ± 2.97% release at 120 h. Both the drugs exhibited sustained release upon incorporation into the NLCs. The absence of any significant cell death during MTT assay performed on NIH 3T3 fibroblasts cells and HaCaT keratinocytes cells indicated that NLCs' were safe for use. Furthermore, significant reduction in nitric oxide level during anti-inflammatory evaluation of formulation on RAW264.7 cells showed excellent potential for the formulation to treat inflammation. The formulation was found stable as no significant difference between the PS, ZP and EE of the fresh and aged NLCs was observed.
CONCLUSION: The outcomes of study deciphered successful formulation of Mes-Cur NLCs.
METHODS: The TNBS induced IBD Wistar rats were used as a model for the study. The microscopic and macroscopic parameters were studied in detail. Almost all the important IBD parameters were reported in this work.
RESULTS: The results demonstrated that the polysaccharides are efficient in carrying the drugs to the colon. Reduction in the level of ulcer index (UI), Myeloperoxidase (MPO), and Malondialdehyde MDA, confirmed the inhibitory activity on the development of Reactive oxygen species (ROS). The increased level of Tumor necrosis factor (TNFα) an expression of colonic inducible nitric oxide synthase (iNOS) was lowered in treatments as compared to TNBS control.
CONCLUSION: The different polymer-based mesalamine (DPBM) confirmed the efficient anti- inflammatory activity on IBD induced rats. The increased level of glutathione (GSH), and superoxide dismutase (SOD) also confirmed the effective anti-inflammatory effect. A significant decrease in the ulcer score and ulcer area was reported. The investigation revealed that chitosan is superior to pectin in IBD treatment likewise polysaccharide-based matrix systems are superior to the coated system.