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包裹于聚乳酸-羟基乙酸共聚物纳米粒中的巴西橡胶树富含C-糖基黄酮部分的体外抗疱疹作用

In vitro antiherpes effect of C-glycosyl flavonoid enriched fraction of Cecropia glaziovii encapsulated in PLGA nanoparticles.

作者信息

Caldas Dos Santos Talitha, Rescignano Nicoletta, Boff Laurita, Reginatto Flávio Henrique, Simões Cláudia Maria Oliveira, de Campos Angela Machado, Mijangos Carmen

机构信息

Institute of Polymer Science and Technology, ICTP - CSIC, Madrid 28006, Spain; Department of Pharmaceutical Sciences, Universidade Federal de Santa Catarina, Florianópolis 88040900, Brazil.

Institute of Polymer Science and Technology, ICTP - CSIC, Madrid 28006, Spain.

出版信息

Mater Sci Eng C Mater Biol Appl. 2017 Jun 1;75:1214-1220. doi: 10.1016/j.msec.2017.02.135. Epub 2017 Mar 3.

Abstract

In this work is reported a novel and promising approach for the preparation of C-glycosylflavonoid enriched fraction of Cecropia glaziovii (EFF-Cg) loaded PLGA nanoparticles (NP) with antiherpes properties. The purpose of this study was to evaluate and to compare the effect of two nonionic surfactants (poloxamer 188 (PLU) and polyvinyl alcohol (PVA)), and also an emulsion stabilized by solid particles of cellulose nanocrystal (CNC) in place of surfactants. The characterization of these nanoparticles was in terms of size, polydispersity index, zeta potential, morphology, thermogravimetric analysis (TGA), loading capacity and percent yield. Since TGA analysis revealed thermo stability especially for NP-PLU, this formulation was selected for the evaluation of drug release profile, cytotoxicity and antiherpes activity. The drug delivery profile demonstrated a sustained release through the polymer structure and a significant reduction of the polymer molecular weight at 21-day period. The cytotoxicity of these nanoparticles was determined on Vero cells, and the selected formulation did not exhibit cytotoxicity even at the highest tested concentration. The results demonstrated a potential antiherpetic effect of the EFF-Cg loaded NP at 48h of testing. In summary, EFF-Cg loaded NP exhibited a promising system for the effective drug delivery in the treatment of herpes infections.

摘要

本研究报道了一种制备载有具有抗疱疹特性的塞克罗皮亚·格拉齐奥维(Cecropia glaziovii)富含C-糖基黄酮部分(EFF-Cg)的聚乳酸-羟基乙酸共聚物(PLGA)纳米颗粒(NP)的新颖且有前景的方法。本研究的目的是评估和比较两种非离子表面活性剂(泊洛沙姆188(PLU)和聚乙烯醇(PVA))以及用纤维素纳米晶体(CNC)固体颗粒代替表面活性剂稳定的乳液的效果。这些纳米颗粒的表征包括尺寸、多分散指数、zeta电位、形态、热重分析(TGA)、载药量和产率百分比。由于TGA分析显示特别是NP-PLU具有热稳定性,因此选择该制剂评估药物释放曲线、细胞毒性和抗疱疹活性。药物递送曲线表明通过聚合物结构实现了持续释放,并且在21天期间聚合物分子量显著降低。在Vero细胞上测定了这些纳米颗粒的细胞毒性,即使在最高测试浓度下,所选制剂也未表现出细胞毒性。结果表明载有EFF-Cg的NP在测试48小时时具有潜在的抗疱疹作用。总之,载有EFF-Cg的NP在治疗疱疹感染方面展现出一种有前景的有效药物递送系统。

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