期刊
AAPS PHARMSCITECH
卷 21, 期 2, 页码 -出版社
SPRINGER
DOI: 10.1208/s12249-019-1607-5
关键词
floating; gastroretentive; Bletilla striata polysaccharide; controlled release; Helicobacter pylori
资金
- National Natural Science Foundation of China [81603309]
- National Key Research and Development Program of China [2017YFC1700705]
- Sichuan Provincial Scholars for Science and Technology Activities for Overseas Researchers [2018-68]
- Key Projects of Central Universities [2018NZD18]
The purpose of this study was to investigate the potential of Bletilla striata polysaccharide (BSP, a natural glucomannan material) for the development of a gastroretentive drug delivery system for the first time. Novel BSP-based porous wafer was prepared for levofloxacin hydrochloride (LFH) delivery by combining floating, swelling, and mucoadhesion mechanisms. The influences of BSP and ethyl cellulose (EC) on drug release and mucoadhesive strength were studied by 3(2) factorial design. The optimized matrix was coated with polycaprolactone (PCL) electrospun membrane by electrospinning and heat treatment technology. The optimized formula (F6, coated) exhibited Q(4 h) of 41.20 +/- 1.90%, Q(8 h) of 76.49 +/- 1.69%, and mucoadhesive strength of 86.11 +/- 1.33 gf, and its drug release profile most closely resembled the Korsmeyer-Peppas model with anomalous diffusion driving mechanism. F6 (coated) also presented excellent buoyancy, preferred swelling characteristic due to the porous structure formed by freeze-drying. Meanwhile, the internal morphology, physical state, drug-excipient compatibility, and thermal behavior were recorded. The negligible cytotoxicity of F6 (coated) was observed in human gastric epithelial cell cultures. In the in vitro antimicrobial experiment, the prepared wafer exhibited obvious bacterial inhibition zone, and due to its longer gastric retention, the wafer also performed a more effective Helicobacter pylori clearance than free LFH in vivo.
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