Comparative pharmaceutical study on colon targeted micro-particles of celecoxib:in-vitro–in-vivoevaluation

Abstract

In order to target celecoxib which is a COX2 inhibitor, with potentials in the prevention and treatment of colitis and colon cancer, it was formulated as microparticles using the solvent/ evaporation method and various pH-dependent Eudragit polymers. The in-vitro evaluation of the prepared microparticles showed spherical and smooth morphology. The encapsulation efficiency and yield were high, indicating that the method used is simple and efficient at this scale. The in-vitro release study showed no release in the acidic medium for 2 h followed by the release of the drug in pH 6.8 in case of Eudragit L100-55 and L100 and pH 7.4 in case of Eudragit S100. The pharmacokinetic parameters were calculated and method validation was performed to insure that it is suitable and reliable. Pharmacokinetic parameters were investigated by determining the C max , T max , AUC 0-t , K el , and t 1/2 of the drug as a suspension and as microparticles. There was a significant difference (p50.05) in T max between the drug as a suspension and as microparticles. The effect of celecoxib on the degree of inflammation was examined on acetic acid induced colitis rat model and the drug was given as a suspension and as microparticles. The evaluation was done using macroscopical, microscopical and biochemical examination. There was a significant difference between the acetic acid control group and the treatment groups regarding all examination criteria in the order microparticles formulated using Eudragit S100 followed by Eudragit L100-55 while microparticles using Eudragit L100 and drug suspension showed almost the same results.

Pathways for Oral and Rectal Delivery of Gold Nanoparticles (1.7 nm) and Gold Nanoclusters into the Colon: Enteric-Coated Capsules and Suppositories

“…Bazan et al developed celecoxib-loaded Eudragit microparticles and carried out in vivo studies in a rat model. They found controlled release of celocoxib (a COX-2 inhibitor, a small molecule drug), and significant decreases in colon inflammation and inflammation markers [ 95 ].…”

Delivery of Potential Drugs to The Colon: Challenges and Strategies

“…Celecoxib is a class of selective cyclooxygenase 2 (COX-2) inhibitors used for colitis treatment, prevention, and as a chemoprotective agent in adenomatous polyposis-induced colorectal cancer (Arber et al, 2006;Bazan et al, 2016). The COX-2 inhibitor has safety and tolerability in IBD patients but it also has cardiovascular side effects when used for a long time (Miao et al, 2014).…”

New Insights of Oral Colonic Drug Delivery Systems for Inflammatory Bowel Disease Therapy

“…In vivo assays carried out in a mouse model of colitis showed that the oral administration of this formulation resulted in a better therapeutic activity, compared to other dexamethasone formulations. Bazan et al [52] developed celecoxib-loaded Eudragit microparticles and they carried out in vivo assays in a rat model. Results indicated that the microparticles formulated using Eudragit S100 and, to a lesser extent Eudragit L100-55, provided a controlled release of celocoxib, important reduction of colonic injury, and a decrease of colon inflammation and inflammation markers.…”