The present study focused to optimize dual coated multiparticulates using Box-Behnken Experimental
Design and in-silico simulation using GastroPlusTM software. The optimized formulations (OB1 and OB2) were
comparatively evaluated for particle size, morphological, in vitro drug release, and in vivo permeation studies. In
silico simulation study predicted the in vivo performance of the optimized formulation based on in-vitro data.
Results suggested that optimized formulation was obtained using maximum content of Eudragit FS30D and
minimum drying time (2 min). In vitro data corroborated that curcumin release was completely protected from
premature drug release in the proximal part of gastro intestinal tract and successfully released to the colon (95%)
which was closely predicted (90.1 %) by GastroPlusTM simulation technique. Finally, confocal laser scanning
microscopy confirmed the in-vitro findings wherein maximum intensity was observed with OB1 treated group
suggesting successful delivery of OB1 to the colon for enhanced absorption as predicted in regional absorption
profile in ascending colon (30.9%) and caecum (23.2%). Limited drug absorption was predicted in small intestine
(1.5-8.7%). The successful outcomes of the research work minimized the release of curcumin in the upper gastric
tract and the maximized drug access to the colon (pH 7.4) as prime concern.
Keywords: Dual coated multiparticulates, experimental design, colon delivery, in silico simulation, in vivo CLSM study, GastroPlusTM
Rights & PermissionsPrintExport