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Design and evaluation of matrix base with sigmoidal release profile for colon-specific delivery using a combination of Eudragit and non-ionic cellulose ether polymers

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Abstract

A pH- and time-controlled drug delivery system with sigmoidal release profile was developed using Eudragit (L100 or S100) in combination with hydroxy ethyl cellulose (HEC) or hydroxy propyl cellulose (HPC) for sigmoidal release of indomethacin in the potential treatment of colon cancer. The effect of varying proportions of polymer type on sigmoidal release was evaluated. The prepared tablets were also characterized for physical characteristics, in vitro drug release, release kinetics, and stability on storage. The gastrointestinal transit of formulations was also investigated in human subjects. Results from in vitro release studies indicated that due to the presence of pH-responsive polymers, a pH- and time-dependent release pattern was observed, which was characterized by negligible drug release in first 4–6 h followed by controlled release for 14–16 h in alkaline pH. In vivo studies indicated that HPC-based formulations had satisfactory matrix strength to withstand gastric and colonic transit, while HEC-based tablets disintegrated during transit through the small intestine. All the formulations were stable on storage. It was concluded that such a matrix design has good potential for drug delivery to colon with controlled release.

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Acknowledgments

The authors would like to thank Dr. Abhishek Gupta and the hospital staff of M.N. Budhrani Cancer Institute, Pune, India, for their kind cooperation and help during in vivo studies in human subjects.

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Authors and Affiliations

  1. Formulation Development & Pharmacokinetics Laboratory, Pharmacy Group, Birla Institute of Technology and Science, Pilani, 333 031, Rajasthan, India

    Laila Fatima Ali Asghar & Sajeev Chandran

  2. Advanced Drug Delivery System, Pharm. R&D, Lupin Research Park, 46/47A, Nande Village, Mulshi Taluka, Pune, 411042, Maharashtra, India

    Sajeev Chandran

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  1. Laila Fatima Ali Asghar
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Correspondence to Sajeev Chandran.

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Asghar, L.F.A., Chandran, S. Design and evaluation of matrix base with sigmoidal release profile for colon-specific delivery using a combination of Eudragit and non-ionic cellulose ether polymers. Drug Deliv. and Transl. Res. 1, 132–146 (2011). https://doi.org/10.1007/s13346-011-0016-4

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