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首页> 美国卫生研究院文献>AAPS PharmSciTech >Preparation and Evaluation of Differently Sulfonated Styrene–Divinylbenzene Cross-linked Copolymer Cationic Exchange Resins as Novel Carriers for Drug Delivery
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Preparation and Evaluation of Differently Sulfonated Styrene–Divinylbenzene Cross-linked Copolymer Cationic Exchange Resins as Novel Carriers for Drug Delivery

机译：不同磺化苯乙烯-二乙烯基苯交联共聚物阳离子交换树脂作为新型药物载体的制备与评价

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摘要

The differently sulfonated styrene–divinylbenzene cross-linked copolymer cationic exchange resins were prepared by oil-in-water polymerization and varied degrees of sulfonation. Several characteristics of the obtained resins were evaluated, i.e., Fourier transform infrared spectra, the ion-exchange capacity, microscopic morphology, size, and swelling. The resin characteristics were altered in relation to the degree of sulfonation, proving that differently sulfonated resins could be prepared. The behavior of chlorpheniramine (CPM) loading and in vitro release in the USP simulated gastric (SGF) and intestinal fluids (SIF) of the obtained resins were also evaluated. The CPM loaded in the resinates (drug-loaded resins) increased with the increasing degree of sulfonic group and hence the drug binding site in the employed resins. The CPM release was lower from the resins with the higher degree of sulfonic group due to the increase in the diffusive path depth. The CPM release was obviously lower in SGF than SIF because CPM, a weak base drug, ionized to a greater extent in SGF and then preferred binding with rather than releasing from the resins. In conclusion, the differently sulfonated resins could be utilized as novel carriers for drug delivery.
机译：不同的磺化苯乙烯-二乙烯基苯交联共聚物阳离子交换树脂是通过水包油聚合和不同程度的磺化制备的。评价了获得的树脂的几个特征，即傅立叶变换红外光谱，离子交换容量，显微形态，尺寸和溶胀。相对于磺化度改变了树脂特性，证明可以制备不同的磺化树脂。还评估了所得树脂在USP模拟胃（SGF）和肠液（SIF）中的氯苯那敏（CPM）负载和体外释放行为。负载在树脂酸酯（载药的树脂）中的CPM随着磺酸基团度的增加而增加，因此随所用树脂中的药物结合位点而增加。由于扩散路径深度的增加，具有较高磺酸基度的树脂的CPM释放量较低。 SGF中的CPM释放明显低于SIF，因为CPM是一种弱碱药物，在SGF中离子化程度更高，因此更倾向于与树脂结合而不是从树脂中释放出来。总之，可以将不同磺化的树脂用作药物输送的新型载体。

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