Colon-specific drug delivery using ethylcellulose and chitosan in the coat of compression-coated tablets

Abstract

Background: This study investigates a new means to achieve colon-specific drug delivery. Objective: This study assesses the use of chitosan and ethylcellulose in the coat of a compression-coated tablet to achieve colon-specific drug delivery. The effects of chitosan type and its level as well as the coat thickness were evaluated.

Materials and methods: Caffeine-containing core tablets were prepared by direct compression. Three chitosan samples with different molecular weight and degree of deacetylation were used. Direct compression produced the finished coated tablet. The product was tested for its potential in colon-specific drug delivery by conducting release studies in simulated gastric and intestinal fluids. Enzymes harvested from rat cecal and colonic contents contributed to a medium to study drug release under colonic conditions.

Results: Essentially no drug was released until action on the tablet by either the acidic pH or the presence of enzymes in the release medium. Chitosan type had no effect on drug release as long as the coating level was the same. Lowering the chitosan level in the coat or increasing the coat thickness increased the lag time.

Discussion: The type of chitosan can be changed and yet the product is still susceptible to enzyme or pH effects. This indicates that chitosan present in the coat is still available for such action by the release medium. One can control the chitosan level or the thickness of the coat to achieve a desired delivery profile.

Conclusion: As colonic media can dramatically promote drug release, the potential for colon-specific drug delivery is confirmed.

Keywords::

• Direct compression
• bacteria-dependent drug delivery
• colon-specific drug delivery
• controlled release
• targeted drug delivery

Acknowledgements

The authors would like to thank Dr Todd Stutzman of Aptuit (Kansas City, MO) for preparation of the core tablets and Dr Matthew A. Howard of McNeil Consumer Healthcare for conducting the ANOVA. The authors wish to thank Dow Chemical Company, FMC Corporation, and Pfizer for the gifts of Ethocel, Avicel, and caffeine, respectively.

Declaration of interest

The UMKC Research Board provided financial support for this study.