Department of Analytical Chemistry, School of Sciences, China Pharmaceutical University, Nanjing, Jiangsu, China.
Department of Analytical Chemistry, School of Sciences, China Pharmaceutical University, Nanjing, Jiangsu, China; Key Laboratory of Drug Quality Control and Pharmacovigilance, Pharmaceutical University, Ministry of Education, 639 Longmian Avenue, Nanjing, 211198, Jiangsu Province, China.
Colloids Surf B Biointerfaces. 2018 Oct 1;170:322-329. doi: 10.1016/j.colsurfb.2018.06.042. Epub 2018 Jun 19.
With the intent of enhancing the loading capacity and controlled the release of a low-water soluble drug (quercetin), 6 ar ms (Poly-Ethylene-Glycol)-amine was grafted in the external surface of halloysite nanotubes. The grafted halloysite nanotubes (HNTs-g-PEG) were decorated with carbon quantum dots for additive fluorescents properties. Conjointly, biotin was conjugated to PEG's free amine groups for precise targeting of tumor tissue and higher cellular uptake. The obtained nanoparticles were characterized by the FTIR, TEM, XRD, zeta potential and TGA analysis. The photoluminescence (PL) properties were investigated by firstly, observing under UV-light at 365 nm; then, the fluorescence spectra of modified HNTs at different levels of preparation were obtained and showed a suitable blue fluorescence. Furthermore, the fluorescent properties were demonstrated by the optical image of HNTs-g-PEG-CDs-Biotin obtained from the confocal microscope, which could be interesting for both in vitro and in vivo imaging. Besides, the prepared NPs showed a superior loading capacity of Que (278.36 mg/g) at optimal adsorption conditions comparing to pristine HNTs. The in vitro drug release from these NPs was relatively sustained and pH sensitive. The incubation of the prepared HNTs-g-PEG-CDs-Biotin NPs with HeLa cells showed a low toxicity and a suitable biocompatibility. The MTT assay of the Que-loaded NPs possesses enhanced antitumor activity over the free Que.
为了提高低水溶性药物（槲皮素）的载药量和控制释放，在埃洛石纳米管的外表面接枝了 6 臂聚乙二醇-胺。接枝的埃洛石纳米管（HNTs-g-PEG）用碳量子点进行了修饰，以增加荧光性质。此外，生物素被共轭到 PEG 的游离氨基上，以实现肿瘤组织的精确靶向和更高的细胞摄取。所得纳米粒子通过傅里叶变换红外光谱（FTIR）、透射电子显微镜（TEM）、X 射线衍射（XRD）、Zeta 电位和热重分析（TGA）进行了表征。通过首先在 365nm 的紫外光下观察，研究了光致发光（PL）性质；然后，获得了不同制备水平的修饰 HNTs 的荧光光谱，显示出合适的蓝色荧光。此外，通过共聚焦显微镜获得的 HNTs-g-PEG-CDs-Biotin 的光学图像证明了荧光性质，这对于体外和体内成像都很有趣。此外，与原始 HNTs 相比，在最佳吸附条件下，这些 NPs 对 Que 具有优异的负载能力（278.36mg/g）。这些 NPs 的体外药物释放相对持续且对 pH 敏感。用 HNTs-g-PEG-CDs-Biotin NPs 孵育 HeLa 细胞显示出低毒性和适宜的生物相容性。载 Que 的 NPs 的 MTT 测定显示出比游离 Que 更强的抗肿瘤活性。
