海藻酸醛-明胶纳米凝胶作为阿奇霉素可持续给药体系:开发、表征及体外评价

Samin A. Dastjerd, Melike Sessevmez, Erdal Cevherand Gülhayat Nasun-Saygılı
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引用次数: 0

摘要

本研究将阿奇霉素包埋在海藻酸醛明胶纳米凝胶中,以三种不同的药聚合物比合成了一种针对革兰氏阴性胞内伤寒沙门菌的肠道特异性可控治疗递送系统,并对该系统的理化性质和抗菌活性进行了研究。采用DLS和FT-IR对负载阿奇霉素的纳米凝胶进行表征。负载阿奇霉素的纳米凝胶水动力直径为118±4 nm, zeta电位为负(-34.2±1.5 mV)。我们通过红外光谱(FT-IR)观察到阿奇霉素在负载到AA-Gel纳米凝胶时从结晶态到无定形态的绝对转变,并且红外光谱测量表明AZM和纳米凝胶网络之间没有任何可检测到的化学和分子内相互作用。药物与聚合物的比例影响纳米凝胶的包封效率,当药物与聚合物的比例为1:3时,包封效率最高(86.3±2.3%)。AA-Gel纳米凝胶的体外阿奇霉素释放谱显示,在4小时内初始爆发释放,随后控制释放直到24小时。与游离阿奇霉素相比,纳米凝胶具有显著的抑菌活性。我们的研究结果表明,阿奇霉素纳米凝胶具有良好的理化、体外和离体特性,可以作为口服给药抗伤寒沙门氏菌的候选药物。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Alginic Aldehyde-Gelatin Nanogel as Sustainable Drug Delivery System of Azithromycin: Development, Characterization and In Vitro Evaluation
- The present study deals with the encapsulation of Azithromycin in alginic aldehyde and gelatin nanogel as an intestinal site-specific and controlled therapeutic delivery system against gram-negative intracellular Salmonella Typhi, which is synthesized through inverse miniemulsion technique in three different drug to polymer ratios, and exploration the physicochemical properties and antibacterial activity of the system. The characterizations of the azithromycin-loaded nanogel were done by DLS and FT-IR. The hydrodynamic diameter of the azithromycin-loaded nanogel is 118±4 nm with negative zeta potential (-34.2±1.5 mV). We observed absolute transition from the crystalline form of the azithromycin to amorphous state while was loaded to the AA-Gel nanogel by FT-IR, and the FT-IR measurements demonstrate that there are not any detectable chemical and intramolecular interactions between AZM and nanogel network. The encapsulation efficiency of the loaded nanogels were influenced by the ratio of drug to polymer, which the highest value (86.3±2.3%) was demonstrated for the 1:3 formulation. In vitro azithromycin release profile from AA-Gel nanogels presents an initial burst release over a period of 4 hours that is followed by controlled release until the 24 hours. Nanogels showed significant bacteriostatic activities in comparison to free azithromycin. Our results indicate proper physicochemical, in vitro and ex vivo features of the azithromycin nanogel, which can be a worthy candidate for oral administration against Salmonella Typhi.
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