蜂胶和明胶废料的纳米粒子作为新型 L-抗坏血酸递送系统。

Nanoparticles of Waste Material of Propolis and Gelatin as a Novel System for Delivery of L-Ascorbic Acid.

机构信息

Postgraduate Program in Pharmaceutical Sciences, Laboratory of Research and Development of Drug Delivery Systems, Department of Pharmacy, State University of Maringa, Maringa, Parana. Brazil.

Postgraduate Program in Pharmaceutical Sciences, Laboratory of Quality Control and Development of Phytotherapics, Department of Pharmacy, State University of Maringa, Maringa, Parana. Brazil.

出版信息

Curr Drug Deliv. 2017;14(7):1028-1039. doi: 10.2174/1570159X14666160322144315.

DOI:10.2174/1570159X14666160322144315

PMID:27067407

Abstract

BACKGROUND

The waste material from the preparation of propolis extracts is a potential natural compound for application in pharmaceutical and medicine nanostructured products. Ascorbic acid is an excellent antioxidant and an important cofactor of several physiological and biochemical processes.

OBJECTIVE

The aim of this study was to develop and characterize nanoparticles containing L-ascorbic acid prepared with propolis byproduct.

METHOD

Nanoparticle's physicochemical characteristics (surface morphology, particle size, zeta potential, and entrapment efficiency), antioxidant activity, in vitro release profile, and in vitro cytotoxicity were evaluated.

RESULTS

Nanoparticles showed to be spherical, with agglomeration, mean diameter between 110.93 and 480.59 nm, zeta potential near zero and good entrapment efficiency. Antioxidant activity of L-ascorbic acid increased when nanoencapsulated and the drug release was prolonged, controlled mainly by the phenomenon of relaxation of polymer chains and dependent of propolis residue concentration. The application of technology provided a reduction in the level of cytotoxicity of L-ascorbic acid, and the nanoparticles showed a protective effect on macrophages.

摘要

背景

蜂胶提取物制备过程中的废料是一种应用于药物和医药纳米结构产品的潜在天然化合物。抗坏血酸是一种极好的抗氧化剂，也是许多生理和生化过程的重要辅助因子。

目的

本研究旨在开发并表征以蜂胶副产物制备的含 L-抗坏血酸的纳米粒子。

方法

评估了纳米粒子的物理化学特性（表面形态、粒径、Zeta 电位和包封效率）、抗氧化活性、体外释放曲线和体外细胞毒性。

结果

纳米粒子呈球形，存在团聚现象，平均粒径在 110.93 至 480.59nm 之间，Zeta 电位接近零，包封效率良好。L-抗坏血酸的抗氧化活性在纳米封装后增加，药物释放时间延长，主要受聚合物链松弛现象和蜂胶残留浓度的影响。该技术的应用降低了 L-抗坏血酸的细胞毒性水平，纳米粒子对巨噬细胞表现出保护作用。