Open AccessEvaluation of in vivo efficacy and toxicity of prednisolone-loaded hydrogel-based drug delivery device
Author(s) -
Amitabha De,
P. K. Bhattacharya,
Sriparna Datta,
Arup Mukherjee
Publication year - 2013
Publication title -
international journal of pharmaceutical investigation
Language(s) - English
Resource type - Journals
eISSN - 2230-973X
pISSN - 2230-9713
DOI - 10.4103/2230-973x.121308
Subject(s) - prednisolone , colitis , inflammatory bowel disease , in vivo , pharmacology , toxicity , drug delivery , medicine , drug , myeloperoxidase , chemistry , inflammation , disease , biology , microbiology and biotechnology , organic chemistry
Drugs prescribed for the treatment of moderate to severe inflammatory bowel disease (IBD) are associated with number of side effects. Targeted drug delivery is essential for the treatment of inflammatory bowel disease in order to increase efficacy and reduce toxicity. The established delivery system is designed on enzyme and time-based release of poorly soluble prednisolone, a drug of choice for the treatment of moderate to severe inflammatory bowel disease. Their pharmacological evaluation was done in 2,4,6-trinitrobenzene sulphonic acid (TNBS)-induced model of colitis in rat. The drug was administered once daily for 3 consecutive days. Visible severity of colitis, tissue to bodyweight ratio, tissue histology along with nitric oxide (NO), malondialdehyde (MDA) and myeloperoxidase (MPO) activity of colonic tissue were studied to estimate the efficacy of the drug-loaded delivery system. The highest efficacy was observed for formulation in which Eudragit RS100 (EU) was used along with guar gum (GG) in a ratio 2:5 for the preparation of delivery device. An effective recovery was observed from the study of tissue histology of animals treated with the drug-loaded optimized formulation and the biochemical parameters supported it. The toxicity of prednisolone (PD) was reduced significantly as predicted from thymus to body weight ratio of treated animals. GG and EU RS100 provided a newer bipolymer combination for the colon-targeted delivery of PD which increased its efficacy and reduced the toxic side effects. The in vivo experiments presented effective amelioration from colitis in TNBS-induced animal model of colitis.