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海藻酸钠/壳聚糖纳米粒的合成与表征及其作为他莫昔芬控释给药系统的研究。

Synthesis and characterisation of alginate/chitosan nanoparticles as tamoxifen controlled delivery systems.

机构信息

Departamento de Farmacología, Facultad de Farmacia, Universidad Complutense de Madrid, Avenida Complutense s/n 28040, Madrid, Spain.

出版信息

J Microencapsul. 2013;30(4):398-408. doi: 10.3109/02652048.2012.746747. Epub 2013 Mar 14.

DOI:10.3109/02652048.2012.746747
PMID:23489017
Abstract

Polysaccharides have shown ideal features for their application in nanomedicine as nanoparticulated systems. Nanoparticles based on mixtures of alginate and chitosan (A/Q-50/50, formed by 50% alginate and 50% chitosan, and A/Q-70/30, formed by 70% alginate and 30% alginate) have been synthesised by an emulsification method and stabilised by amide bond formation. Tamoxifen (TMX) was loaded into these systems, and they were assayed as controlled delivery formulations. Results showed the formation of spherical nanoparticles with very small size (19-28 nm). The presence of amide bonds was determined by FT-IR and confirmed by Thermogravimetric analysis studies. TMX incorporation was achieved successfully (2-3 µg TMX per mg NP), and maximum TMX release took place between 8 and 24 h. This study shows that interaction between TMX and the system was dependent on nanoparticle composition, being the composition with higher proportion of alginate the one which showed the best release control of the drug.

摘要

多糖因其作为纳米颗粒系统的纳米医学应用的理想特性而受到关注。通过乳化方法合成了基于海藻酸钠和壳聚糖混合物的纳米粒子(A/Q-50/50,由 50%的海藻酸钠和 50%的壳聚糖组成,A/Q-70/30,由 70%的海藻酸钠和 30%的壳聚糖组成),并通过酰胺键形成进行稳定。将他莫昔芬(TMX)载入这些系统中,并将其作为控制释放制剂进行了评估。结果表明,形成了具有非常小尺寸(19-28nm)的球形纳米粒子。通过傅里叶变换红外光谱(FT-IR)确定了酰胺键的存在,并通过热重分析研究得到了证实。成功实现了 TMX 的掺入(每毫克 NP 有 2-3μg 的 TMX),并且 TMX 的最大释放发生在 8 到 24 小时之间。这项研究表明,TMX 与系统之间的相互作用取决于纳米粒子的组成,其中含有更高比例海藻酸钠的组成表现出对药物的最佳释放控制。

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