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首页> 外文期刊>Journal of drug targeting >Ex-vivo evaluation of alginate microparticles for Polymyxin B oral administration.
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Ex-vivo evaluation of alginate microparticles for Polymyxin B oral administration.

机译：藻酸盐微粒对多粘菌素B口服施用的ex-体内评价。

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摘要

A crosslinked alginate microparticle system for the targeting to the lymphatic system by Peyer's patches (PP) uptake was designed in order to improve the oral absorption of Polymyxin B (PMB). To verify mucoadhesion and PP uptake, microparticles labelled with fluorescein isothiocyanate (FITC) were prepared by spray-drying technique and crosslinking reactions with calcium ions and chitosan (CS), in vitro characterized and assayed by an ex vivo method. Microparticles showed a size less then 3 microm, an antibiotic loading level of 11.86 +/- 0.70%, w/w, a sustained drug release behaviour in simulated gastro-intestinal (GI) fluids and a preserved biological activity throughout the manufacture. The ex vivo study was performed by a perfusion method on intestinal tracts of just sacrificed adult rats. The recovered samples were analysed by epifluorescence microscope for mucoadhesion and PP uptake and by microbiological analysis for antibiotic activity preservation, providing evidence of mucoadhesion at the level of both PP and non-PP epithelium, uptake by PP and PMB microbiological activity in PP tissue. Furthermore, the study revealed the involvement of transport pathways across villous enterocytes.
机译：设计用于靶向淋巴系统的交联藻酸盐系统（PP）摄取，以改善多粘菌素B（PMB）的口服吸收。为了验证粘膜粘附和PP吸收，通过用钙离子和壳聚糖（Cs）的喷雾干燥技术和交联反应，制备用荧光素异硫氰酸酯（FITC）标记的微粒，体外用途和壳聚糖（Cs），以外的方法进行体外制备。微粒显示尺寸小于3微米，抗生素负载量为11.86 +/- 0.70％，w / w，在模拟的胃肠（Gi）流体中持续的药物释放行为以及整个制造中的保存的生物活性。通过刚处于处死成年大鼠的肠道灌注方法进行前体内研究。通过对粘膜粘附显微镜和PP吸收分析回收的样品，并通过微生物分析进行抗生素活性保存，在PP组织中通过PP和非PP上皮的水平提供粘液的含量，并在PP组织中摄取PP和PMB微生物活性。此外，该研究揭示了在绒毛肠细胞上涉及运输途径。

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