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壳聚糖-聚乙二醇-叶酸-Fe(III)配合物作为表没食子儿茶素没食子酸酯的纳米载体。

Chitosan-PEG-folate-Fe(III) complexes as nanocarriers of epigallocatechin-3-gallate.

机构信息

Grupo de Investigación en Ingeniería Biomédica EIA (GIBEC), Programa de Ingeniería Biomédica, Escuela de Ciencias de la Vida, Universidad EIA, km 2 + 200 Vía al Aeropuerto José María Córdova Envigado, Envigado, Colombia; Grupo de Investigación Ciencia de los Materiales, Instituto de Química, Facultad de Ciencias Exactas y Naturales, Universidad de Antioquia, Calle 70 No 52-21, Medellín, Colombia.

Grupo de Investigación Ciencia de los Materiales, Instituto de Química, Facultad de Ciencias Exactas y Naturales, Universidad de Antioquia, Calle 70 No 52-21, Medellín, Colombia.

出版信息

Int J Biol Macromol. 2020 Dec 15;165(Pt B):2909-2919. doi: 10.1016/j.ijbiomac.2020.10.166. Epub 2020 Oct 24.

Abstract

Controlled release nanocarriers systems are promising for the administration of epigallocatechin-3-gallate (EGCG) in the treatment and prevention of several diseases. Therefore, the stability and therapeutic effects of EGCG must be enhanced from an encapsulation strategy. Thus, this research aims to explore a method to prepare EGCG nanocarriers based on coordination complexes from Fe (III) ions and blends of modified chitosan (Ch) with polyethylene glycol (PEG) and folic acid (F). Different degrees of deacetylated Ch and conjugated with F were evaluated, whose values determined the final amount of Fe (III) in the complexes. All these complexes were amorphous with a polydispersity index (PDI) higher than 0.3. The assembling and homogeneity were improved adding tripolyphosphate (TPP), yielding particle sizes near 200 nm, and PDI values of 0.2, measured by DLS and TEM. The EGCG encapsulation efficiency was about 60%, and the loading capacity was in the range of 26% to 50%. The EGCG release profile displayed a controlled release without a burst effect, providing the best fit with the Korsmeyer-Peppas model, indicating interactions among EGCG and the polymer matrix. The above results reveal the potential of these nanocarriers as suitable systems for controlled release and have not yet been reported.

摘要

载药纳米载体系统在通过给药来治疗和预防多种疾病方面很有应用前景。因此,必须通过封装策略来提高表没食子儿茶素没食子酸酯(EGCG)的稳定性和治疗效果。因此,本研究旨在探索一种基于 Fe(III)离子与改性壳聚糖(Ch)与聚乙二醇(PEG)和叶酸(F)的混合物制备 EGCG 纳米载体的方法。评估了不同脱乙酰度的 Ch 和与 F 共轭的 Ch,其值决定了配合物中 Fe(III)的最终含量。所有这些配合物都是无定形的,多分散指数(PDI)高于 0.3。通过添加三聚磷酸钠(TPP)可以提高组装和均一性,得到接近 200nm 的粒径和 0.2 的 PDI 值,通过 DLS 和 TEM 测量。EGCG 的包封效率约为 60%,载药量在 26%到 50%之间。EGCG 的释放曲线显示出无突释效应的控制释放,与 Korsmeyer-Peppas 模型拟合度最好,表明 EGCG 与聚合物基质之间存在相互作用。上述结果表明,这些纳米载体作为控制释放的合适系统具有潜力,且尚未有报道。

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