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首页> 外文期刊>RSC Advances >Preactivated-thiolated polyacrylic acid/1-vinyl pyrrolidone nanoparticles as nicotine carriers for smoking cessation
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Preactivated-thiolated polyacrylic acid/1-vinyl pyrrolidone nanoparticles as nicotine carriers for smoking cessation

机译：作为尼古丁携带的尼古丁丙烯酮纳米粒子停止 - 硫醇聚丙烯酸/ 1-乙烯基吡咯烷酮纳米粒子

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This study aimed to develop nicotine-loaded mucoadhesive preactivated-thiolated polymeric nanoparticles (PNPs) for smoking cessation. 2-Mercaptonicotinic acid (2MNA) was coupled as dithionicotinic acid dimer and used in the preactivation of thiolated polyacrylic acid/vinyl pyrrolidone PNPs (thiolated AA/VP PNPs). Preactivated-thiolated AA/VP PNPs were synthesized through surfactant-free emulsion polymerization and coupling reactions. The structural attributes of the preactivated-thiolated AA/VP PNPs were characterized using Fourier-transform infrared spectroscopy and proton nuclear magnetic resonance spectroscopy. The particle size and zeta potential were evaluated by dynamic light scattering evaluation. The morphology of the preactivated-thiolated AA/VP PNPs was examined using scanning electron microscopy. In addition, the mucoadhesive properties, drug loading and release, and biocompatibility of the preactivated-thiolated AA/VP PNPs were assessed. The spherical preactivated-thiolated AA/VP PNPs were successfully synthesized with a particle size of 410.3 ± 7.4 nm and a negative surface charge. The preactivated-thiolated AA/VP PNPs exhibited superior mucoadhesive properties compared with the thiolated AA/VP PNPs. Drug loading by PNP to a nicotine ratio of 1?:?1 provided desirable loading capacity and % loading efficiency of 285.7 ± 36.7 μg mg ~(?1) and 57.1 ± 7.4%, respectively. More than 50% of the nicotine contained in the PNPs was rapidly released in the first hour, followed by a sustained release for up to 12 h. Moreover, the synthesized PNPs were non-toxic to human gingival cells. Therefore, the preactivated-thiolated AA/VP PNPs may be a candidate carrier of nicotine for smoking cessation.
机译：该研究旨在开发尼古丁含有的粘膜粘附的硫化聚合物纳米颗粒（PNPS），用于吸烟。 2-巯基辛酸（2MNA）作为二硫硅酸二聚体偶联，并用于硫醇化聚丙烯酸/乙烯基吡咯烷酮PNPS（硫醇化AA / VP PNP）的反应。通过无表面活性剂的乳液聚合和偶联反应合成预活性的AA / VP PNP。采用傅里叶变换红外光谱和质子核磁共振光谱表征预活性硫化AA / VP PNP的结构属性。通过动态光散射评估评估粒度和ζ电位。使用扫描电子显微镜检查预活性硫醇化AA / VP PNP的形态。此外，评估粘膜粘附性质，药物载体和释放，以及预活性硫化AA / VP PNP的生物相容性。以410.3±7.4nm的粒度和负表面电荷成功合成球形常用硫化AA / VP PNP。与硫化AA / VP PNP相比，预活性的硫化AA / VP PNP表现出优异的粘膜粘附性质。通过PNP将药物加载到尼古丁比为1？：1提供了所需的负载能力和285.7±36.7μgmg〜（α1）和57.1±7.4％的％负载效率。在第一个小时内，PNP中含有的超过50％的尼古丁迅速释放，然后持续释放到12小时。此外，合成的PNP对人牙龈细胞无毒。因此，预活性硫化的AA / VP PNP可以是尼古丁的候选载体，用于吸烟。

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