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首页> 外文期刊>International Journal of Pharmaceutics >pH-sensitive hydrogels based on bovine serum albumin for oral drug delivery.
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pH-sensitive hydrogels based on bovine serum albumin for oral drug delivery.

机译:基于牛血清白蛋白的pH敏感水凝胶,用于口服药物递送。

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摘要

pH-sensitive bovine serum albumin (BSA) hydrophilic microspheres were prepared by free radical polymerization of methacrylate derivatized BSA and methacrylic acid sodium salt. Incorporation of both monomers in hydrogels was confirmed by Fourier transform infrared spectroscopy. Morphological analysis by scanning electron microscopy showed spherical shape and porous surface of all prepared samples. The microspheres showed high water affinity at neutral pH values and a narrow dimensional distribution. Network density of hydrogels depends on derivatization degree (DD%) of BSA and/or concentration of modified BSA in the polymerization feed. In order to employ the prepared samples such as pH-sensitive hydrogels, in vitro release studies, in media simulating biological fluids, were performed using diflunisal (DF) and beta-propranolol (PR) as model drugs. Experimental data showed that the release profiles depend on drug-matrix interactions and diffusional limitation awardable to crosslinking degree of microparticles. beta-Propranolol is quickly released at pH 1.0 and a complete release after 1 h at pH 6.8 was observed. In the case of diflunisal pH-sensitive release was observed. At pH 1.0 low amounts of drug were released (w/w<10% after 2 h). When the pH is 6.8, the diflunisal release increased in the amount (w/w>75% after 24 h).
机译:pH敏感的牛血清白蛋白(BSA)亲水性微球是通过甲基丙烯酸衍生的BSA和甲基丙烯酸钠盐的自由基聚合制备的。通过傅立叶变换红外光谱法证实了两种单体在水凝胶中的掺入。通过扫描电子显微镜的形态分析显示所有制备的样品的球形和多孔表面。微球在中性pH值下具有高的水亲和力,并且尺寸分布窄。水凝胶的网络密度取决于BSA的衍生化度(DD%)和/或聚合进料中改性BSA的浓度。为了使用制备的样品(例如pH敏感水凝胶),在体外模拟生物流体的介质中,以二氟尼沙尔(DF)和β-普萘洛尔(PR)作为模型药物进行了体外释放研究。实验数据表明,释放曲线取决于药物-基质相互作用和可归因于微粒交联度的扩散限制。 β-普萘洛尔在pH 1.0时迅速释放,在pH 6.8的条件下1小时后观察到完全释放。在双氟菊酯的情况下,观察到pH敏感释放。在pH 1.0时,释放出少量药物(2 h后w / w <10%)。当pH为6.8时,二氟菊酯的释放量增加(24小时后w / w> 75%)。

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