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首页> 外文期刊>Journal of biomedical materials research. Part B, Applied biomaterials. >The application of a crosslinked pectin-based wafer matrix for gradual buccal drug delivery.
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The application of a crosslinked pectin-based wafer matrix for gradual buccal drug delivery.

机译：交联的基于果胶的威化饼基质在逐步颊药物递送中的应用。

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The purpose of this study was to develop crosslinked wafer matrices and establish the influence of the crosslinker type and processing sequence on achieving gradual buccal drug delivery. Three sets of drug-loaded crosslinked pectin wafers were produced employing the model water-soluble antihistamine, diphenhydramine and were compared with noncrosslinked wafers. The formulations were crosslinked with CaCl(2), BaCl(2), or ZnSO(4) pre- or postlyophilization (sets 1 and 2) as well as pre- and postlyophilization (set 3), respectively. The surface morphology, porositometry, molecular vibrational transitions, textural attributes, thermal and in vitro drug release were characterized and supported by in silico molecular mechanics simulations. Results revealed that crosslinked wafers produced smaller pore sizes (107.63 ?) compared with noncrosslinked matrices (180.53 ?) due to molecular crosslinks formed between pectin chains. Drug release performance was dependent on the wafer crosslinking production sequence. Noncrosslinked wafers displayed burst-release with 82% drug released at t(30min) compared with first-order kinetic profiles obtained for prelyophilized crosslinked matrices (50% released at t(30min) followed by steady release). Wafers crosslinked postlyophilization displayed superior control of drug release (40% at t(30min)). Molecular mechanics simulations corroborated with the experimental data and established that Ba(++), having the largest atomic radii (1.35 ?) formed a number of ionic bridges producing wafers of higher porosity (0.048 cm(2)/g) and had more influence on drug release.
机译：这项研究的目的是开发交联的华夫饼基质，并建立交联剂类型和加工顺序对实现渐进颊药物输送的影响。使用模型水溶性抗组胺剂，苯海拉明生产了三套载有药物的交联果胶薄饼，并与非交联薄饼进行了比较。将制剂分别与CaCl（2），BaCl（2）或ZnSO（4）交联，然后分别进行冻干前后（第1和2组）以及冻干前后（第3组）。表面形态，孔隙率，分子振动跃迁，结构属性，热和体外药物释放均通过计算机模拟分子力学进行了表征和支持。结果表明，由于果胶链之间形成了分子交联，与未交联的基质（180.53？）相比，交联的晶片产生的孔径较小（107.63？）。药物释放性能取决于晶圆交联的生产顺序。与预冻干的交联基质获得的一级动力学曲线相比，非交联的威化饼显示出在t（30min）释放了82％的药物的突发释放（在t（30min）释放了50％，然后稳定释放）。晶圆交联的冻干后显示出对药物释放的优异控制（t（30分钟）时达到40％）。分子力学模拟与实验数据相符，并确定具有最大原子半径（1.35？）的Ba（++）形成了许多离子桥，产生了较高孔隙度（0.048 cm（2）/ g）的晶片，并且具有更大的影响力关于药物释放。

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