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吐温 80 和泊洛沙姆 127 对胡椒堿传递用玉米醇溶蛋白纳米载体稳定化的影响。

Effect of Tween 80 and Pluronic 127 on the stabilization of zein nanocarriers for the delivery of piperine.

机构信息

Drug Delivery and Nanomedicine Research Laboratory, Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER)-Raebareli, Lucknow, India.

Drug Delivery and Nanomedicine Research Laboratory, Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER)-Raebareli, Lucknow, India.

出版信息

Food Res Int. 2024 Dec;197(Pt 1):115202. doi: 10.1016/j.foodres.2024.115202. Epub 2024 Oct 21.

DOI:10.1016/j.foodres.2024.115202
PMID:39593287
Abstract

In the current research work, zein-based polymeric nanocarriers were developed for the delivery of piperine, where the effect of non-ionic surfactants (Tween 80 and Pluronic F-127) on the stability and in vitro drug release characteristics were studied. Physiochemical characterization studies showed that the particle size of blank and drug-loaded surfactant stabilized zein nanoparticles were <200 nm and particles were spherical in shape. FTIR studies confirmed the successful incorporation of piperine within the zein nanoparticle without any alteration in primary structure of zein. The circular dichroism spectroscopy suggested that α-helix content of zein was reduced following the incorporation of drug within nanoparticles. The solubility of piperine was enhanced significantly in the gastrointestinal tract, and higher sustained release was observed for tween 80-stablized zein nanoparticles. The formulations were stable towards thermal treatment up to 90 °C, showed superior resistance towards aggregation even at ionic strength >50 mM NaCl, and did not show any aggregation even at the isoelectric pH. Tween 80-stablized zein nanoparticles showed good redispersibility index with the cryoprotectant mannose (5 % w/v) after lyophilization. The current research would contribute to the advancement of zein nanoparticles for the delivery of nutraceutical agents, which may be utilized in the food supplements or therapeutic agents to improve the human health.

摘要

在当前的研究工作中,开发了基于玉米醇溶蛋白的聚合物纳米载体来递送胡椒碱,研究了非离子表面活性剂(吐温 80 和泊洛沙姆 F-127)对其稳定性和体外药物释放特性的影响。物理化学特性研究表明,空白和载药表面活性剂稳定的玉米醇溶蛋白纳米粒的粒径均<200nm,且颗粒呈球形。傅里叶变换红外光谱研究证实了胡椒碱成功掺入玉米醇溶蛋白纳米粒中,而玉米醇溶蛋白的一级结构没有任何改变。圆二色性光谱表明,药物掺入纳米粒后,玉米醇溶蛋白的α-螺旋含量减少。胡椒碱在胃肠道中的溶解度显著提高,且吐温 80 稳定的玉米醇溶蛋白纳米粒呈现出更高的持续释放效果。制剂在高达 90°C 的热处理下稳定,即使在离子强度>50mM NaCl 下也表现出优异的抗聚集能力,即使在等电 pH 值下也没有发生聚集。在冻干后添加 5%(w/v)甘露糖作为冷冻保护剂,吐温 80 稳定的玉米醇溶蛋白纳米粒具有良好的再分散指数。该研究将为玉米醇溶蛋白纳米粒作为营养药物的递送系统提供参考,可用于食品补充剂或治疗剂,以改善人类健康。

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