Unilamellar Liposomes with Enhanced Boron Content

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• 作者：Tiejun Li ; Julie Hamdi ; and M. Frederick Hawthorne
• 刊名：Bioconjugate Chemistry
• 出版年：2006
• 出版时间：January 2006
• 年：2006
• 卷：17
• 期：1
• 页码：15 - 20
• 全文大小：97K
• 年卷期：v.17,no.1(January 2006)
• ISSN：1520-4812

文摘

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)₂CHOCH₂-7,8-C₂B₉H₁₁] (DAC-16), and cholesterol for encapsulation ofan aqueous buffer core. Since DSPC was not necessary for the formation of stable DAC-16 liposomes, the boronconcentration of these vesicles was increased dramatically to approximately 8.8 wt % in the dry lipid; theseliposomes had a high bilayer boron incorporation efficiency of 98%. DSPC-free liposomes exhibited a sizedistribution pattern of 40-60 nm, which was in the range normally associated with selective tumor uptake. Thissize distribution was maintained throughout storage at room temperature for several months. Additionally, optimizedliposome formulations incorporating DAC-16, DSPC, and cholesterol were identified having stable size distributionpatterns after storage for more than two months at a variety of temperatures. Although animal studies indicatethat DAC-16 liposomes are toxic, this new ionic nido-carborane lipid allows the formation of liposomes of highboron content for in vitro applications that require the delivery of large amounts of boron.