The present study aimed to statistically optimize a colon specific formulation of @entity1487 for the treatment of @entity694 . A 3(2) full factorial design was used for optimization. The independent variables employed were amount of pectin and amount of starch paste, each at three levels. The evaluated responses were @entity3358 , percent cumulative drug release (% @entity7958 ) at 5th h and t(90%) (time required for 90% of drug release). Drug release studies were carried out using change over media [pH 1.2, 7.4 and 6.5 in presence of 4% (w/v) @entity35 caecal contents]. The optimized formulation was subjected to in vivo roentgenographic studies in New Zealand white @entity95 to analyze the in vivo behaviour of the developed tablets. This formulation was also evaluated for cytotoxic potential using HT-29 @entity1 @entity694 cell lines. Pharmacokinetic studies in New Zealand white @entity95 were conducted to determine the extent of systemic exposure provided by the developed formulation in comparison to an immediate release tablet. The optimized formulation consisting of pectin (66.67%, w/w) and starch paste (15%, w/w) released negligible amount of drug at pH 1.2 and pH 7.4 whereas significant (p < 0.05) drug release was observed at pH 6.5 in presence of 4% (w/v) @entity35 caecal contents. Roentgenographic studies corroborated the in vitro observations, thus providing the "proof of concept". Pharmacokinetic studies revealed significant reduction in systemic exposure and @entity137 studies demonstrated enhanced cellular uptake of drug by the developed formulation. Shelf life of the formulation was found to be 2.83 years. The results of the study established pectin-based coated matrix tablet to be a promising system for the colon specific delivery of @entity1487 so as to treat @entity694 .

Novel microbially triggered colon specific delivery system of XXXX : statistical optimization, in vitro, in vivo, cytotoxic and stability assessment.

@entity1 :: ('9606', 'Species') :: ['human'] @entity3358 :: ('MESH:D018804', 'Disease') :: ['hardness'] @entity137 :: ('MESH:D064420', 'Disease') :: ['cytotoxicity'] @entity95 :: ('9986', 'Species') :: ['rabbits'] @entity35 :: ('10116', 'Species') :: ['rat'] @entity694 :: ('MESH:D003110', 'Disease') :: ['colon cancer', 'colon carcinoma'] @entity7958 :: ('1038', 'Gene') :: ['CDR'] @entity1487 :: ('MESH:D005472', 'Chemical') :: ['5-Fluorouracil', '5-FU']
@entity1487 :: (MESH:D005472,Chemical) :: ['5-Fluorouracil']
