A Novel Inner Time and Outer pH-Dependent Dual Coated Multi-Particulate Approach for Colon Specific Delivery of Ibuprofen Beyond Ileocecal Segment in Reduced Colonic Bacterial Diversity
摘要
The purpose of the current novel study is to develop dual-coated multi-particulates with a combination of time-dependent inner and pH-dependent outer coating layers to control the release of the entrapped drug from the ascending colon onwards.
MethodsIbuprofen-loaded pellets prepared via powder layering technology were coated initially with time-dependent hydroxypropyl cellulose and ethyl cellulose-based inner polymeric layers and afterwards with the Eudragit L100 and Eudragit S100-based outer pH-dependent coating layers and evaluated.
ResultsThe best double-coated batch showed nominal in vitro release of 6.163 ± 0.23% in simulated upper GI conditions, with surface morphology collaborating with kinetics data. In-vivo animal X-Ray Roentgenography and plasma analysis studies revealed intact multi-particulates arriving inside the colon with maximum plasma concentration of 5.97 ± 0.41 μg/ml (Cmax), retarded till 12th hr (Tmax).
ConclusionResults suggest that these dual-coated multi-particulates can be more efficient for colon-specific targeting of various potent drugs.