Unilamellar liposomes with enhanced boron content
Unilamellar liposomes with enhanced boron content
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DOI：
10.1021/bc0501350
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发表时间：
2006-01-01
影响因子：
4.7
通讯作者：
Hawthorne, MF
中科院分区：
文献类型：
--
作者：
Li, TJ;Hamdi, J;Hawthorne, MF
使用新型双链离子型巢碳硼烷脂质 K[nido-7-(C16H33OCH2)(2)CHOCH2-7,8-C2B9H11] (DAC-16) 和胆固醇封装水性缓冲核心，形成了一种新型的富含硼、不含 DSPC 的单层脂质体。由于 DSPC 对于形成稳定的 DAC-16 脂质体不是必需的，因此这些囊泡的硼浓度急剧增加至干脂质中的约 8.8 wt%；这些脂质体具有高达 98% 的双层硼掺入效率。不含 DSPC 的脂质体表现出 40-60 nm 的尺寸分布模式，这在通常与选择性肿瘤摄取相关的范围内。这种尺寸分布在室温下的整个储存过程中保持了几个月。此外，经鉴定，包含 DAC-16、DSPC 和胆固醇的优化脂质体配方在各种温度下储存两个月以上后具有稳定的尺寸分布模式。尽管动物研究表明 DAC-16 脂质体有毒，但这种新型离子型 Nido-Carborane 脂质可以形成高硼含量的脂质体，用于需要输送大量硼的体外应用。
A new type of boron-rich, DSPC-free, unilamellar liposomes was formed using the novel dual-chain, ionic, nido-carborane lipid, K[nido-7-(C16H33OCH2)(2)CHOCH2-7,8-C2B9H11] (DAC-16), and cholesterol for encapsulation of an aqueous buffer core. Since DSPC was not necessary for the formation of stable DAC-16 liposomes, the boron concentration of these vesicles was increased dramatically to approximately 8.8 wt% in the dry lipid; these liposomes had a high bilayer boron incorporation efficiency of 98%. DSPC-free liposomes exhibited a size distribution pattern of 40-60 nm, which was in the range normally associated with selective tumor uptake. This size distribution was maintained throughout storage at room temperature for several months. Additionally, optimized liposome formulations incorporating DAC-16, DSPC, and cholesterol were identified having stable size distribution patterns after storage for more than two months at a variety of temperatures. Although animal studies indicate that DAC-16 liposomes are toxic, this new ionic nido-carborane lipid allows the formation of liposomes of high boron content for in vitro applications that require the delivery of large amounts of boron.