Development and Characterization of PCL Electrospun Membrane-Coated Bletilla striata Polysaccharide-Based Gastroretentive Drug Delivery System

Development and Characterization of PCL Electrospun Membrane-Coated Bletilla striata Polysaccharide-Based Gastroretentive Drug Delivery System
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PCL电纺膜包被白及多糖胃滞留给药系统的开发和表征

DOI:
10.1208/s12249-019-1607-5
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发表时间:
2020-01
期刊:
影响因子:
3.3
通讯作者:
Qu Yan
Qu Yan
中科院分区:
医学3区
文献类型:
--
作者:
Li Zhouying;Zeng Rui;Yang Ling;Ren Xiaodong;Maffucci Katherine G;Qu Yan

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本研究首次探讨了白芨多糖(BSP)作为一种天然葡甘露聚糖材料用于胃滞留给药系统的可能性。利用漂浮、溶胀和粘膜粘附机制制备了新型的以牛磺酸为基质的盐酸左氧氟沙星(LFH)缓释片。采用32因子设计研究了BSP和乙基纤维素(EC)对药物释放和粘膜粘附强度的影响。采用静电纺丝和热处理技术对优化后的基体进行聚己内酯(PCL)静电纺丝膜包覆。优化处方(F6,包衣)的Q4 h为41.20 ± 1.90%,Q8 h为76.49 ± 1.69%,粘膜粘附强度为86.11 ± 1.33 gf,其释药曲线最接近具有异常扩散驱动机制的Korsmeyer-Peppas模型。F6(涂层)也表现出优异的浮力,由于冷冻干燥形成的多孔结构,优选的溶胀特性。同时,记录了内部形态、物理状态、药物-赋形剂相容性和热行为。在人胃上皮细胞培养物中观察到F6(包被)的细胞毒性可忽略不计。在体外抑菌实验中,制备的薄片具有明显的抑菌圈,并且由于其较长的胃滞留时间,在体内也比游离LFH更有效地清除幽门螺杆菌。图形摘要图形摘要
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 32 factorial design. The optimized matrix was coated with polycaprolactone (PCL) electrospun membrane by electrospinning and heat treatment technology. The optimized formula (F6, coated) exhibited Q4 h of 41.20 ± 1.90%, Q8 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. Graphical abstract Graphical abstract
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发表时间: 2015
期刊: Evidence-based complementary and alternative medicine : eCAM
影响因子: --
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