Partha Ranga, Mitchell Linsey R, Lyon Jennifer L, Joshi Pratixa P, Conyers Jodie L
Department of Internal Medicine, The University of Texas Health Science Center at Houston, 6431 Fannin Street, Houston, Texas 77030, USA.
ACS Nano. 2008 Sep 23;2(9):1950-8. doi: 10.1021/nn800422k.
We report the preparation and preliminary in vitro studies of nanocarriers termed "buckysomes," which are self-assembled, spherical nanostructures composed of the amphiphilic fullerene AF-1. By inducing AF-1 self-assembly at an elevated temperature of 70 degrees C, dense spherical buckysomes with diameters of 100-200 nm were formed, as observed by electron microscopy and dynamic light scattering. The amphiphilic nature of AF-1 results in the formation of many hydrophobic regions within the buckysomes, making them ideal for embedding hydrophobic molecules to be tested in a drug delivery scheme. After confirming the cellular internalization of buckysomes embedded with the hydrophobic fluorescent dye 1,1'-dioctadecyl-3,3,3',3'-tetramethylindocarbocyanine perchlorate, we embedded paclitaxel, a highly hydrophobic anticancer drug. The in vitro therapeutic efficacy of the paclitaxel-embedded buckysomes toward suppression of MCF-7 breast cancer cell growth was compared to that of Abraxane, a commercially available, nanoparticle-albumin-bound formulation of paclitaxel. Notably, the paclitaxel-embedded buckysomes demonstrated a similar efficacy to that observed with Abraxane in cell viability studies; these results were confirmed microscopically. Moreover, negative control studies of MCF-7 viability using empty buckysomes demonstrated that the buckysomes were not cytotoxic. The results of our studies suggest that buckysomes prepared from self-assembly of AF-1 at 70 degrees C are promising nanomaterials for the delivery of hydrophobic molecules.
我们报告了一种名为“巴基球囊”的纳米载体的制备及其初步体外研究，该纳米载体是由两亲性富勒烯AF-1自组装形成的球形纳米结构。通过在70℃的高温下诱导AF-1自组装，形成了直径为100 - 200nm的致密球形巴基球囊，这通过电子显微镜和动态光散射观察到。AF-1的两亲性导致在巴基球囊内形成许多疏水区域，使其成为在药物递送方案中嵌入待测试疏水分子的理想选择。在用疏水荧光染料1,1'-二辛基-3,3,3',3'-四甲基吲哚碳菁高氯酸盐确认了嵌入巴基球囊的细胞内化后，我们嵌入了紫杉醇，一种高度疏水的抗癌药物。将嵌入紫杉醇的巴基球囊对MCF-7乳腺癌细胞生长抑制的体外治疗效果与Abraxane（一种市售的纳米颗粒白蛋白结合型紫杉醇制剂）进行了比较。值得注意的是，在细胞活力研究中，嵌入紫杉醇的巴基球囊表现出与Abraxane相似的效果；这些结果通过显微镜得到了证实。此外，使用空巴基球囊对MCF-7活力进行的阴性对照研究表明，巴基球囊没有细胞毒性。我们的研究结果表明，由AF-1在70℃自组装制备的巴基球囊是用于递送疏水分子的有前景的纳米材料。
