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Construction and in vitro characterization of an optimized porosity-enabled amalgamated matrix for sustained transbuccal drug delivery.

International Journal of Pharmaceutics 391(1-2):79 (2010) PMID 20176095

This research focused on constructing and characterizing an optimized porosity-enabled amalgamated matrix (P-EAM) for sustained transbuccal drug delivery. An interphase, co-particulate, co-solvent, homogenization technique and lyophilization guided through a Box-Behnken experimental design was employed in the fabrication, characterization and optimization of 15 P-EAMs. The effects of varying factor levels on the characteristic in vitro physicochemical performances of the P-EAMs were explored. Formulations had an average weight of 128.44+/-3.48 mg with a dimensional size of 8mm by 5mm. Surface morphology showed varieties of pore structures, widespread distributions and uneven interconnectors. Satisfactory drug-loading was achieved (53.14+/-2.19-99.02+/-0.74%). Overall amount of drug released in 8h was measured by the MDT(50%) value which ranged between 22.50 and 225.00 min. Formulation demonstrated significant levels of ex vivo bioadhesive strength measured as detachment force (F(det)=0.964+/-0.015 to 1.042+/-0.025 N) and work of adhesion (omega(adh)=0.0014+/-0.00005 to 0.0028+/-0.00008 J). The potential of the P-EAMs to initiate and sustain ex vivo transbuccal permeation of drug was shown and measured as a cumulative value of between 25.02+/-0.85 and 82.21+/-0.57% in 8h. Formulations were mesoporous in nature with pore sizes ranging from 40 to 100 A characterized by the presence of interconnectors. Statistical constraints were simultaneously set to obtain levels of independent variables that optimized the P-EAM formulation. Copyright (c) 2010 Elsevier B.V. All rights reserved.

DOI: 10.1016/j.ijpharm.2010.02.023