Effect of co-administration of probiotics with guar gum, pectin and eudragit S100 based colon targeted mini tablets containing 5-Fluorouracil for site specific release

• Published in: Journal of drug delivery science and technology 2020-12, Vol.60, p.102004, Article 102004
• Main Authors: Kumar, Ankit, Gulati, Monica, Singh, Sachin Kumar, Gowthamarajan, K., Prashar, Rahul, Mankotia, Diksha, Gupta, Jay Prakash, Banerjee, Mayukh, Sinha, Shubham, Awasthi, Ankit, Corrie, Leander, Kumar, Rajan, Patni, Pooja, Kumar, Bimlesh, Pandey, Narendra Kumar, Sadotra, Manik, Kumar, Pardeep, Kumar, Rajesh, Wadhwa, Sheetu, Khursheed, Rubiya
• Format: Article
• Language: English
• Subjects: Colon targeted delivery; Mini tablets; Pharmacokinetics; Polysaccharides
• ISSN: 1773-2247
• DOI: 10.1016/j.jddst.2020.102004

Oral colon targeted mini-tablets containing 5-Fluorouracil (5-FU) were developed by using guar gum, pectin and Eudragit S100. Probiotics were co-administered to constantly replenish the gut microflora of colon that gets damaged due to pathophysiology of cancer and side effect of 5-FU. Replacement of microbial count ensures that the polysachharide used for sustaining the drug release gets digested to release the drug, once the formulation reaches the colon. The site-specific release of coated tablets was confirmed by dissolution studies in medium containing rat caecal contents (RCC), wherein, the formulation containing Eudragit S100, pectin and guar gum in the ratio of 04:03:03 w/w, showed less than 10% drug release in initial 5 h and immediate burst release (100%) between 5th to 10th hour. The cell line studies carried for pooled dissolution samples indicated that more than 90% cells were viable in all the cases till 5th hour. Significant (p