Division of Pharmaceutical Technology, Faculty of Pharmacy, University of Helsinki, FI-00014, Finland.
Nanoscale. 2012 May 21;4(10):3184-92. doi: 10.1039/c2nr30397c. Epub 2012 Apr 16.
In this study, the self-assembly of hydrophobin class II (HFBII) on the surface of thermally hydrocarbonized porous silicon (THCPSi) nanoparticles was investigated. The HFBII-coating converted the hydrophobic particles into more hydrophilic ones, improved the particles' cell viability in both HT-29 and Caco-2 cell lines compared to uncoated particles, and enhanced the particles' cellular association. The amount of HFBII adsorbed onto the particles was also successfully quantified by both the BCA assay and a HPLC method. Importantly, the permeation of a poorly water-soluble drug, indomethacin, loaded into THCPSi particles across Caco-2 monolayers was not affected by the protein coating. In addition, (125)I-radiolabelled HFBII did not extensively permeate the Caco-2 monolayer and was found to be stably adsorbed onto the THCPSi nanoparticles incubated in pH 7.4, which renders the particles the possibility for further track-imaging applications. The results highlight the potential of HFBII coating for improving wettability, increasing biocompatibility and possible intestinal association of PSi nanoparticulates for drug delivery applications.
本研究考察了亲脂性Ⅱ类（HFBⅡ）在热烃化多孔硅（THCPSi）纳米粒子表面的自组装。与未涂层的粒子相比，HFBⅡ涂层将疏水性粒子转化为亲水性粒子，提高了粒子在 HT-29 和 Caco-2 细胞系中的细胞存活率，并增强了粒子的细胞结合能力。通过 BCA 分析和 HPLC 方法都成功地定量了吸附到粒子上的 HFBⅡ的量。重要的是，负载到 THCPSi 粒子中的疏水性差的药物吲哚美辛的渗透穿过 Caco-2 单层并没有受到蛋白质涂层的影响。此外，（125）I 放射性标记的 HFBⅡ没有广泛渗透到 Caco-2 单层中，并且发现在 pH 7.4 下孵育的 THCPSi 纳米粒子上被稳定吸附，这使得粒子有可能用于进一步的跟踪成像应用。研究结果强调了 HFBⅡ涂层在改善润湿性、提高生物相容性和可能的肠道结合方面的潜力，这对于药物传递应用来说是非常有意义的。
