Optimizing Prednisolone Loading into Distiller’s Dried Grain Kafirin Microparticles, and In vitro Release for Oral Delivery

• Main Authors: Esther T. L. Lau, Stuart K. Johnson, Barbara A. Williams, Deirdre Mikkelsen, Elizabeth McCourt, Roger A. Stanley, Ram Mereddy, Peter J. Halley, Kathryn J. Steadman
• Format: Article
• Language: English
• Published: MDPI AG 2017-05-01
• Series: Pharmaceutics
• Subjects: kafirin; distiller’s dried grains with solubles; microparticles; response surface methodology; simulated gastrointestinal conditions; colonic delivery
• Online Access: http://www.mdpi.com/1999-4923/9/2/17

Kafirin microparticles have potential as colon-targeted delivery systems because of their ability to protect encapsulated material from digestive processes of the upper gastrointestinal tract (GIT). The aim was to optimize prednisolone loading into kafirin microparticles, and investigate their potential as an oral delivery system. Response surface methodology (RSM) was used to predict the optimal formulation of prednisolone loaded microparticles. Prednisolone release from the microparticles was measured in simulated conditions of the GIT. The RSM models were inadequate for predicting the relationship between starting quantities of kafirin and prednisolone, and prednisolone loading into microparticles. Compared to prednisolone released in the simulated gastric and small intestinal conditions, no additional drug release was observed in simulated colonic conditions. Hence, more insight into factors affecting drug loading into kafirin microparticles is required to improve the robustness of the RSM model. This present method of formulating prednisolone-loaded kafirin microparticles is unlikely to offer clinical benefits over commercially available dosage forms. Nevertheless, the overall amount of prednisolone released from the kafirin microparticles in conditions simulating the human GIT demonstrates their ability to prevent the release of entrapped core material. Further work developing the formulation methods may result in a delivery system that targets the lower GIT.