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In vivo evaluation of an Ultra-fast Disintegrating Wafer matrix: A molecular simulation approach to the ora-mucoadhesivity

Reddy, D. ; Choonara, Y.E. ; Kumar, P. ; Govender, M. ; Indermun, S. ; du Toit, L.C. ; Meyer, L.C.R. ; Pillay, V. ;
  • 초록  

    The purpose of this study was to design and evaluate the performance of an Ultra-fast Disintegrating Wafer (U-D-WAF) loaded with highly water soluble diphenhydramine hydrochloride (DPH) through the oramucosa of the Large White Pig model. For the first time this work explored the oramucosivity of the U-D-WAF by detailed molecular modeling of the matrix on buccal tissue in order to mechanistically deduce the mucodhesivity. The U-D-WAF was formulated using a blend of hydroxypropylcellulose, poly(acrylic) acid, sodium starch glycolate and β -cyclodextrin in accordance with a Box-Benkhen experimental design for optimization prior to ex vivo permeation and in vivo release studies in the Large White Pig. Molecular simulation studies assess the mucoadhesivity of the U-D-WAF to the oramucosa. A mean Drug Entrapment Efficiency of 72.96 +/- 4.32%, disintegration time of 29.33 +/- 15.91 s and drug release after 60 s of 86.32 +/- 20.37% was recorded. Ex vivo permeation studies revealed cumulative drug permeation of 86.32 +/- 20.34% 60 s after onset. In vivo evaluation of the optimized U-D-WAF had a C max = 5 59 μgL -1 approximately 300 s after administration. The ultrafast disintegration of the U-D-WAF matrix with desirable mucoadhesivity in in vitro and in vivo studies makes it suitable for effective and rapid oramucosal drug delivery.


  • 주제어

    Oramucosal drug delivery .   Wafer matrix .   Rapid disintegration .   In vivo permeabilty .   Molecular modeling .   Mucoadhesivity.  

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