Iemma Francesca, Spizzirri U Gianfranco, Puoci Francesco, Muzzalupo Rita, Trombino Sonia, Cassano Roberta, Leta Sonia, Picci Nevio
Dipartimento di Scienze Farmaceutiche, Università della Calabria, 87036 Rende (CS), Italy.
Int J Pharm. 2006 Apr 7;312(1-2):151-7. doi: 10.1016/j.ijpharm.2006.01.010. Epub 2006 Feb 21.
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).
通过甲基丙烯酸酯衍生化的牛血清白蛋白(BSA)与甲基丙烯酸钠盐的自由基聚合反应制备了pH敏感型牛血清白蛋白亲水性微球。傅里叶变换红外光谱证实了两种单体均掺入到水凝胶中。扫描电子显微镜进行的形态分析表明,所有制备的样品均呈球形且表面多孔。微球在中性pH值下表现出高亲水性且尺寸分布狭窄。水凝胶的网络密度取决于BSA的衍生化程度(DD%)和/或聚合进料中改性BSA的浓度。为了将制备的样品用作pH敏感型水凝胶,使用双氯芬酸(DF)和β-普萘洛尔(PR)作为模型药物,在模拟生物流体的介质中进行了体外释放研究。实验数据表明,释放曲线取决于药物-基质相互作用以及归因于微粒交联程度的扩散限制。β-普萘洛尔在pH 1.0时快速释放,在pH 6.8时1小时后观察到完全释放。对于双氯芬酸,观察到pH敏感型释放。在pH 1.0时,释放的药物量较低(2小时后w/w<10%)。当pH为6.8时,双氯芬酸的释放量增加(24小时后w/w>75%)。