In vitro -In vivo- In silico Simulation of Experimental Design Based Optimized Curcumin Loaded Multiparticulates System

Author(s): Sima Singh*, Afzal Hussain, Uma Ranjan Lal, Nisar Sayyad, Rajshekhar Karpoormath*, Manimbulu Nlooto

Journal Name: Current Pharmaceutical Design

Volume 24 , Issue 30 , 2018

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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 software.

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Article Details

Year: 2018
Published on: 08 December, 2018
Page: [3576 - 3586]
Pages: 11
DOI: 10.2174/1381612824666181022120252
Price: $65

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PDF: 33