Université de Limoges, Laboratoire PEIRENE, EA 7500, Faculté des Sciences et Techniques, 123 Avenue Albert Thomas, 87060 Limoges, France.
Université de Limoges, Laboratoire PEIRENE EA 7500, Faculté de Pharmacie, 2, rue du Docteur Marcland, 87025 Limoges, France.
Carbohydr Polym. 2019 Jun 1;213:168-175. doi: 10.1016/j.carbpol.2019.02.070. Epub 2019 Feb 20.
Porphyrins are widely used in anticancer photodynamic therapy (PDT). However, low physiological solubility and lack of selectivity towards cancer cells are the main limitations of their clinical use. Nanoparticles are being intensively explored as photosensitizer carriers for PDT to overcome these limitations. The aims of this work are to synthesize core-shell hybrid nanoparticles formed by a silica core and xylan carrying a 5-(4-hydroxyphenyl)-10,15,20-triphenylporphyrin (TPPOH) shell, and evaluate their anticancer activity. To afford drug-controlled incorporation and enhance blood circulation, TPPOH was covalently linked to xylan. Different xylans with degrees of substitution in TPPOH ranging from 0.034 to 1.11, were obtained and characterized. Then, the xylan-TPPOH conjugate (PX) was used to coat the silica nanoparticles (PX SNPs). The obtained nano-objects were characterized and their therapeutic potential for photodynamic therapy evaluated against colorectal cancer cell lines. in vitro analysis showed that PX SNPs were 40-fold and 10-fold more effective against HCT116 cells and HT-29 cells respectively compared to free TPPOH.
卟啉广泛应用于抗癌光动力疗法（PDT）。然而，其在生理上溶解度低且缺乏对癌细胞的选择性，这是其临床应用的主要限制。纳米粒子作为 PDT 的光敏剂载体正在被深入研究，以克服这些限制。本工作的目的是合成由二氧化硅核和携带 5-(4-羟基苯基)-10,15,20-三苯基卟啉（TPPOH）壳的木聚糖形成的核壳混合纳米粒子，并评估它们的抗癌活性。为了实现药物控制的结合并增强血液循环，TPPOH 通过共价键与木聚糖结合。获得了取代度在 TPPOH 为 0.034 到 1.11 之间的不同木聚糖，并对其进行了表征。然后，将木聚糖-TPPOH 缀合物（PX）用于包覆二氧化硅纳米粒子（PX SNPs）。对所得到的纳米物体进行了表征，并评估了它们在针对结肠直肠癌细胞系的光动力疗法中的治疗潜力。体外分析表明，与游离 TPPOH 相比，PX SNPs 对 HCT116 细胞和 HT-29 细胞的有效率分别提高了 40 倍和 10 倍。
