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负载花青素纳米颗粒的制备与表征

Formulation and Characterization of Anthocyanins-Loaded Nanoparticles.

作者信息

Dupeyrón Danay, Kawakami Monique, Rieumont Jacques, Carvalho José Carlos

机构信息

Laboratório de Pesquisa em Fármacos, Centro de Ciências Biológicas e da Saúde, Colegiado de Farmácia, Universidade Federal do Amapá. Rod. JK, km 2, 68902-380, Macapá- AP, Brazil.

出版信息

Curr Drug Deliv. 2017;14(1):54-64. doi: 10.2174/1567201813666160915102151.

Abstract

BACKGROUND

Açaí berry, from the Euterpe oleracea Mart. Palm, has been described as the most important fruit in the Brazilian Amazon. Several studies have reported that anthocyanins (ACNs), one of the components of the açaí, have enormous potential for pharmaceuticals applications. However, the bioavailability of anthocyanins is relatively low compared to that of other flavonoids. Then, in the present work, anthocyanins-loaded nanoparticles have been developed to overcome their poor bioavailability.

METHODS

A two-level factorial design with three factors was considered to evaluate the effect of EUDRAGIT ® L100, polyethylene glycol 2000 (PEG 2000) and polysorbate 80 on encapsulation efficiency (EE) of anthocyanins. Also, major parameters of nanoparticles were assessed by using mainly SEM microscopy and Dynamic light scattering.

RESULTS

PEG 2000 was the only individual factor that has statistical significance (95% confidence level). The process yields (PY) were found in between 67% and 92%; the particle size and morphology analysis showed two distribution size, one for NPs and another for the agglomerates.

CONCLUSION

The pH-sensitive polymer together with the hydrophilic polymer showed to be suitable as ACNs delivery system. The delayed release profile of ACNs, observed for all formulations, can enhance their poor bioavailability. Nevertheless, ACNs bioavailability in vivo remains to be studied.

摘要

背景

来自巴西莓棕榈(Euterpe oleracea Mart.)的阿萨伊浆果被认为是巴西亚马逊地区最重要的水果。多项研究报告称,阿萨伊浆果的成分之一花青素在药物应用方面具有巨大潜力。然而,与其他类黄酮相比,花青素的生物利用度相对较低。因此,在本研究中,已开发出负载花青素的纳米颗粒以克服其生物利用度差的问题。

方法

采用三因素二级析因设计来评估丙烯酸树脂® L100、聚乙二醇2000(PEG 2000)和聚山梨酯80对花青素包封率(EE)的影响。此外,主要通过扫描电子显微镜(SEM)和动态光散射来评估纳米颗粒的主要参数。

结果

PEG 2000是唯一具有统计学意义(95%置信水平)的单个因素。工艺产率(PY)在67%至92%之间;粒径和形态分析显示出两种分布尺寸,一种是纳米颗粒的尺寸,另一种是团聚体的尺寸。

结论

pH敏感聚合物与亲水性聚合物一起被证明适合作为花青素的递送系统。所有制剂均观察到的花青素缓释特性可提高其较差的生物利用度。然而,花青素在体内的生物利用度仍有待研究。

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