Institute for BioNanotechnology in Medicine, Northwestern University, Chicago, Illinois 60611, USA.
ACS Nano. 2011 Nov 22;5(11):9113-21. doi: 10.1021/nn203343z. Epub 2011 Nov 1.
Self-assembling peptide amphiphile (PA) nanofibers were used to encapsulate camptothecin (CPT), a naturally occurring hydrophobic chemotherapy agent, using a solvent evaporation technique. Encapsulation by PA nanofibers was found to improve the aqueous solubility of the CPT molecule by more than 50-fold. PAs self-assembled into nanofibers in the presence of CPT as demonstrated by transmission electron microscopy. Small-angle X-ray scattering results suggest a slight increase in diameter of the nanofiber to accommodate the hydrophobic cargo. In vitro studies using human breast cancer cells show an enhancement in antitumor activity of the CPT when encapsulated by the PA nanofibers. In addition, using a mouse orthotopic model of human breast cancer, treatment with PA nanofiber-encapsulated CPT inhibited tumor growth. These results highlight the potential of this model PA system to be adapted for delivery of hydrophobic therapies to treat a variety of diseases including cancer.
自组装肽两亲物 (PA) 纳米纤维被用于使用溶剂蒸发技术来包封喜树碱 (CPT),一种天然存在的疏水性化疗药物。PA 纳米纤维的包封被发现将 CPT 分子的水溶解度提高了 50 多倍。正如透射电子显微镜所证明的那样,PA 在存在 CPT 的情况下自组装成纳米纤维。小角 X 射线散射结果表明,纳米纤维的直径略有增加,以容纳疏水性货物。使用人乳腺癌细胞的体外研究表明,当 CPT 被 PA 纳米纤维包封时,其抗肿瘤活性增强。此外,使用人乳腺癌的小鼠原位模型,用 PA 纳米纤维包封的 CPT 治疗抑制了肿瘤生长。这些结果强调了这种模型 PA 系统的潜力,可以适用于传递疏水性治疗药物来治疗包括癌症在内的各种疾病。