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基于 BSA 的水溶胶纳米粒子的制备及评估——用京尼平交联用于改善难溶性姜黄素的口服生物利用度。

Preparation and evaluation of BSA-based hydrosol nanoparticles cross-linked with genipin for oral administration of poorly water-soluble curcumin.

机构信息

Department of Food Chemistry, Research Institute of Food Science and Technology, 12th km Mashhad-Ghouchan Highway, Mashhad, POB: 91735-147, Iran.

Department of Food Nanotechnology, Research Institute of Food Science and Technology, Mashhad, Iran.

出版信息

Int J Biol Macromol. 2017 Nov;104(Pt A):788-798. doi: 10.1016/j.ijbiomac.2017.06.083. Epub 2017 Jun 21.

DOI:10.1016/j.ijbiomac.2017.06.083
PMID:28647524
Abstract

One of the most interesting functions of albumin is the ability to interact with bioactive compounds. This study describes preparation of protein-based nanoparticles (NPs) for the preparation of solid dispersion of curcumin (CN). Fabrication of hydrosol system of dispersed CN in bovine serum albumin (BSA) was approached, followed by cross-linking with glutaraldehyde (Gta). Response surface methodology (RSM) was used to investigate the influence of input factors (pH, CN content and organic phase ratio (r)), on the particle size and CN entrapment efficiency (EE). Particle size, EE and CN loading efficiency (LE) at optimum condition (pH 7, r 10% and 3.4mg of CN content), were found to be in the range of 153-184.4nm, 72.54%, and 14.508μg/mg, respectively. In the optimum formulation, genipin (Gnp) was used at three different levels (0.1-0.2 and 0.3% w/w of BSA), as a safe, natural cross-linker instead of toxic Gta, to address the limitation of oral delivery purpose. AFM and SEM analysis revealed the spherical and smooth surface of Nps. Ninhydrin (NHD) assay and FT-IR analysis confirmed the cross-linking between BSA and Gnp. In vitro release studies ensure the efficiency of the formulation for sustained release of soluble CN.

摘要

白蛋白的一个最有趣的功能是与生物活性化合物相互作用的能力。本研究描述了用于制备姜黄素(CN)固体分散体的基于蛋白质的纳米粒子(NPs)的制备。制备分散在牛血清白蛋白(BSA)中的 CN 的水溶胶体系,随后用戊二醛(Gta)交联。响应面法(RSM)用于研究输入因素(pH、CN 含量和有机相比例(r))对粒径和 CN 包封效率(EE)的影响。在最佳条件(pH 7、r 10%和 3.4mg CN 含量)下,粒径、EE 和 CN 负载效率(LE)分别在 153-184.4nm、72.54%和 14.508μg/mg 的范围内。在最佳配方中,使用京尼平(Gnp)作为一种安全、天然的交联剂,取代有毒的 Gta,以解决口服递送目的的局限性,其使用水平为 BSA 的 0.1-0.2 和 0.3%(w/w)。AFM 和 SEM 分析显示 NPs 呈球形和光滑表面。茚三酮(NHD)测定和 FT-IR 分析证实了 BSA 和 Gnp 之间的交联。体外释放研究确保了该制剂用于可溶性 CN 持续释放的效率。

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