Department of Chemistry, Faculty of Science, Cairo University, Giza 12613, Egypt.
Cellulose & Paper Department, National Research Centre, El-Buhooth Street, Dokki 12622, Cairo, Egypt.
Int J Biol Macromol. 2020 May 1;150:228-237. doi: 10.1016/j.ijbiomac.2020.02.056. Epub 2020 Feb 7.
This work deals with assessing the efficient performance of sodium caseinate (SC) as protein-based drug delivery system of niacin (NA) than carboxymethyl cellulose (CMC). In this respect the hydrogels from complexation of chitosan with sodium caseinate (SC/Ch) or sodium carboxymethyl cellulose (CMC/Ch) were prepared. The Synthesized NA free and loaded hydrogels were characterized by many techniques for examining the interaction, morphology, swelling, encapsulation efficiency (EE) and loading (L) % of niacin, as well as cytotoxicity study. The finding data showed the promising behavior of SC/Ch hydrogel than CMC/Ch hydrogel, toward the amount of loaded NA (95.6%) and in vitro slow sustained release up to 24 h. Whereas, the entrapment efficiency of the CMC/Ch to nicotinic acid was reached 85.6%, and it possessed highly initial burst release followed by a slower release up to 24 h. At pH 7.4 (simulated intestinal fluid) both hydrogels provided higher level of releasing profile to NA than pH 2.1 (gastric fluid). The NA release from hydrogels followed Fickian and non-Fickian diffusion mechanism according to pH 7.4 and 2.1, respectively. It is interesting to note that, the data obtained are higher than those obtained from literature reported hydrogel, e.g., poly (2-hydroxyethyl methacrylate). Neutral red uptake and lactate dehydrogenase assays confirmed both hydrogels have good biocompatibility and could be used as nontoxic drug delivery system. So, we recommended SC/Ch hydrogel as an effective controlled niacin drug delivery system with reducing systemic side effects and improved intestinal targeting efficiency.
这项工作旨在评估以酪蛋白酸钠（SC）为载体制备烟酸（NA）药物传递系统的效率，优于羧甲基纤维素（CMC）。在这方面，制备了壳聚糖与酪蛋白酸钠（SC/Ch）或羧甲基纤维素钠（CMC/Ch）络合的水凝胶。通过多种技术对合成的无载和载药水凝胶进行了表征，以考察其相互作用、形态、溶胀、包封效率（EE）和载药量（L）%、以及细胞毒性研究。结果表明，与 CMC/Ch 水凝胶相比，SC/Ch 水凝胶对载药量（95.6%）和 24 小时内的体外缓慢持续释放具有更好的性能。而 CMC/Ch 对烟酰胺的包封效率达到 85.6%，并具有较高的初始突释释放，随后缓慢释放至 24 小时。在 pH 7.4（模拟肠液）下，两种水凝胶对 NA 的释放水平均高于 pH 2.1（胃液）。NA 从水凝胶中的释放遵循 pH 7.4 时的菲克扩散机制和 pH 2.1 时的非菲克扩散机制。有趣的是，所得数据高于文献报道的水凝胶，如聚（2-羟乙基甲基丙烯酸酯）。中性红摄取和乳酸脱氢酶试验证实，两种水凝胶均具有良好的生物相容性，可作为非毒性药物传递系统。因此，我们推荐 SC/Ch 水凝胶作为一种有效的烟酸控释药物传递系统，可减少全身副作用并提高肠道靶向效率。
