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KMID : 0043320120350050839
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Archives of Pharmacal Research
2012 Volume.35 No. 5 p.839 ~ p.850
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Preparation and characterization of a novel pH-sensitive coated microsphere for duodenum-specific drug delivery
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Zhou Dan
Zhu Xi
Wang Yang
Jin Yun
Xu Xuefan
Fan Tingting
Liu Yan
Zhang Zhirong
Huang Yuan
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Abstract
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The aim of this study is to develop a duodenum-specific drug delivery system on the basis of a pH-sensitive coating and a mucoadhesive inner core for eradication of Helicobacter pylori (H. pylori) in the ulcer duodenum. Hydroxypropyl methylcellulose acetate maleate (HPMCAM) was used as the pH-sensitive material, which dissolves around pH 3.0. The mucoadhesive microspheres loaded with furazolidone (FZD-ad-MS) were prepared by the emulsification-solvent evaporation method using Carbopol 971NP as the mucoadhesive polymer. The prepared pH-sensitive coated mucoadhesive microspheres (AM-coated-MS) were characterized in regards to particle size, drug loading efficiency, morphological change, drug stability, drug release and in vitro anti-H. pylori activity. The particle size was 160.97 ± 47.24 μm and 336.44 ± 129.34 μm, and the drug content was 42.33 ± 3.43% and 10.96 ± 1.29% for FZD-ad-MS and AM-coated-MS, respectively. The morphological changes in different pH media were characterized by scanning electron microscopy (SEM). HPMCAM coating improved the stability of the FZD-ad-MS and these particles were expected to remain intact until their arrival in the duodenum. The drug release was extremely suppressed at pH 1.2 for AM-coated-MS, but increased at pH 4.0 after regeneration of FZD-ad-MS. In addition, FZD-ad-MS exhibited excellent anti-H. pylori activity in vitro. Thus, the HPMCAM-coated microspheres developed in this study hold great promise for use as a duodenum-specific drug delivery system for H. pylori clearance.
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KEYWORD
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HPMCAM-coated mucoadhesive microspheres, Furazolidone-loaded mucoadhesive microspheres, Duodenum-specific, pH-Sensitive, Morphological changes, Drug release
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