Nanocarriers from GRAS Zein Proteins to Encapsulate Hydrophobic Actives.
Nanocarriers from GRAS Zein Proteins to Encapsulate Hydrophobic Actives.
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DOI：
10.1021/acs.biomac.6b01440
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发表时间：
2016-10
影响因子：
6.2
通讯作者：
Nikolas T Weissmueller;H. Lu;Amanda Hurley;R. Prud’homme
中科院分区：
文献类型：
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作者：
Nikolas T Weissmueller;H. Lu;Amanda Hurley;R. Prud’homme
限制纳米药物扩展的一个因素是其生产所需的材料和工艺的高成本。我们提出了一种连续的、可扩展的、低成本的纳米封装工艺——Flash nanop沉淀法（FNP），它可以使用玉米蛋白生产具有窄尺寸分布的纳米载体（nc）。玉米蛋白是一种低成本的GRAS蛋白（FDA一般认为是安全的），目前在食品应用中使用，它作为使用FNP的疏水化合物的有效封装剂。四流FNP配置允许封装非常疏水的化合物，这在以前的沉淀过程中是不可能的。我们提出了几种具有高达45 wt %玉米蛋白浓度的药物负荷的模型活性化合物包封到约100 nm的纳米载体中。提出了三个例子：(1)前药物抗氧化剂，维生素e -醋酸酯，(2)抗霍乱群体感应调节剂CAI-1 ((S)-3-羟基三烷醇-4-one；通过调节细胞通讯降低霍乱弧菌毒力的CAI-1)，以及(3)具有一系列疏水性的疏水荧光染料。玉米蛋白和牛奶蛋白之间的特殊相互作用，酪蛋白酸钠，在PBS， LB培养基和pH 2溶液中提供了NCs的稳定性。三种培养基的稳定性和大小变化为玉米蛋白/活性蛋白/酪蛋白NC的组装机制提供了信息。
One factor limiting the expansion of nanomedicines has been the high cost of the materials and processes required for their production. We present a continuous, scalable, low cost nanoencapsulation process, Flash Nanoprecipitation (FNP) that enables the production of nanocarriers (NCs) with a narrow size distribution using zein corn proteins. Zein is a low cost, GRAS protein (having the FDA status of "Generally Regarded as Safe") currently used in food applications, which acts as an effective encapsulant for hydrophobic compounds using FNP. The four-stream FNP configuration allows the encapsulation of very hydrophobic compounds in a way that is not possible with previous precipitation processes. We present the encapsulation of several model active compounds with as high as 45 wt % drug loading with respect to zein concentration into ∼100 nm nanocarriers. Three examples are presented: (1) the pro-drug antioxidant, vitamin E-acetate, (2) an anticholera quorum-sensing modulator CAI-1 ((S)-3-hydroxytridecan-4-one; CAI-1 that reduces Vibrio cholerae virulence by modulating cellular communication), and (3) hydrophobic fluorescent dyes with a range of hydrophobicities. The specific interaction between zein and the milk protein, sodium caseinate, provides stabilization of the NCs in PBS, LB medium, and in pH 2 solutions. The stability and size changes in the three media provide information on the mechanism of assembly of the zein/active/casein NC.