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Formulation and development of di-dependent microparticulate system for colon-specific drug delivery

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Abstract

Colorectal cancer (CRC) is the third most common cancer globally and the second most common cause of cancer-related deaths. Site-specific delivery of drugs leads to an increase in the availability of drugs at the targeted region. The objective of the present investigation was to develop a dually functional microparticulate colon-targeted drug delivery system of meloxicam for potential application in the prophylaxis of colorectal cancer. Chitosan microspheres were prepared by using emulsification–chemical cross-linking technique. Formulation parameters studied include chitosan concentration, drug to polymer ratio, agitation speed, emulsifier concentration, quantity of cross-linking agent and time for cross-linking. In vitro evaluation of microspheres revealed premature release of drug in the upper part of gastrointestinal tract. Since coating of microspheres is difficult to accomplish (with reproducible results), they were compacted to tablets. Enteric coating of tableted microspheres was achieved using Eudragit® S100. In vitro evaluation and SEM studies depict that the microspheres remain intact during compression process. The developed system was further evaluated for in vivo pharmacokinetic and roentgenography studies. In vivo pharmacokinetic evaluation in rabbits reveal that the onset of drug absorption from the coated tableted microspheres (T lag time = 4.67 ± 0.58 h) was significantly delayed compared to uncoated tableted microspheres. In vivo roentgenographic study revealed that the system remained intact, until it reaches to the colonic region (5 h). Thus, from the results of the study, it can be revealed that the developed system could serve as a potential tool for efficient delivery of drug to the colonic region.

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Acknowledgments

The author is thankful to Nirma University, Ahmedabad, Gujarat, India, for providing financial assistance in form of minor research project. The author acknowledges Dr. Bhoomika Patel, Assistant Professor, Department of Pharmacology, Institute of Pharmacy, Nirma University for rendering required help for the in vivo evaluation.

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  1. Department of Pharmaceutics, Institute of Pharmacy, Nirma University, SG Highway, Chharodi, Ahmedabad, Gujarat, 382 481, India

    Mayur M. Patel

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Correspondence to Mayur M. Patel.

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In vivo pharmacokinetic studies of the developed CoDDS were carried out as per the protocol (IP/PCEU/FAC/14-1/018) approved by the Institutional Animal Ethics Committee, Nirma University, Ahmedabad, India.

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The authors declare that they have no conflict of interest.

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Patel, M.M. Formulation and development of di-dependent microparticulate system for colon-specific drug delivery. Drug Deliv. and Transl. Res. 7, 312–324 (2017). https://doi.org/10.1007/s13346-017-0358-7

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