Drug loaded and ethylcellulose coated mesoporous silica for controlled drug release prepared using a pilot scale fluid bed system

作者：Hacene Youcef Chakib; Singh Abhishek; Van den Mooter Guy^*

来源：International Journal of Pharmaceutics, 2016, 506(1-2): 138-147.

DOI：10.1016/j.ijpharm.2016.04.047

• Mesoporous silica
• Controlled drug release
• Fluid bed coating
• Drug loading
• Ethylcellulose
• PVP K30

The goal of this study was to test the feasibility to load non-ordered, non-spherical mesoporous silica with the model drug paracetamol, and subsequently coat the loaded particles using one single pilot scale fluid bed system equipped with a Wurster insert. Mesoporous silica particles (Davisil (R)) with a size ranging from 30 to 500 mm and an average pore diameter of 15 nm were loaded with paracetamol to 18.8% drug content. Subsequently, loaded cores were coated with ethylcellulose to obtain controlled drug release. Coating processing variables were varied following a full factorial design and their effect on drug release was assessed. Increasing coating solution feed rate and decreasing fluidizing air temperature were found to increase drug release rates. Increasing pore former level and decreasing coating level were found to increase drug release rates. The release medium's osmolality was varied using different sodium chloride concentrations, which was found to affect drug release rates. The results of this study clearly indicate the potential of non-ordered, non-spherical mesoporous silica as a reservoir carrier for the controlled release of drugs. Although non-spherical, we were able to reproducibly coat this carrier using a bottom spray fluid bed system. However, a major hurdle that needs to be tackled is the attrition the material suffers from during fluid bed processing.

• 出版日期2016-6-15