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2018年第十二届中国药物制剂大会

作者： Atef Mohammed Qasem Ahmed Li-Qing Chen 曹青日 College of Pharmaceutical Scicences Soochow University

Objectives: This study aimed to evaluate the cellular uptake, intra cellular localizatin and polarization effect of p H-sensitive liposome（PSL）-coated single-walled carbon nanohorns（SWCNHs） loading doxorubicin（DOX） and tumor associated macrophages（TAMs） polarization factor IL-21. Methods: DOX was noncovalently conjugated with the oxidized SWCNHs（O-SWCNHs） via π-π stacking interaction to form DOXO-SWCNHs, which was further coated with the PSL loading IL-21 to form IL-21-PSL-DOX-O-SWCNHs. The cellular uptake and intracellular localization of functionalized SWCNHs were performed by using flow cytometry and confocal laser scanning microscope. The polarization of TAMs was evaluated by RT-PCR. The drug loadings of IL-21-PSL-DOX-O-SWCNHs and PSL-DOX-O-SWCNHs were determined. The release of IL-21 and DOX was studied at pH 5.5 and pH 7.4. Results: The cellular uptake and intracellular localization of nanocarriers showed that PSL-DOX-O-SWCNHs could be effectively uptaked by A549 cells, reaching up to 100 % of cellular uptake. The macrophages were expressed as M2 type after irritation by IL-4. PCR results showed that the IL-12 levels significantly increased, while IL-10 levels decreased oppositely after the TAMs were treated with IL-21-PSL-DOX-O-SWCNHs. The drug loadings of IL-21-PSL-DOX-OSWCNHs and PSL-DOX-O-SWCNHs were 1.64% and 24.9%, respectively. The release of IL-21 and DOX from nanocarriers was pH-sensitive, which is beneficial for drug release in the tumor microenvironment. Conclusion: Novel functionalized SWCNHs loading DOX and IL-21（IL-21-PSL-DOX-O-SWCNHs） showed excellent cellular uptake and p H-sensitive release characteristics and could significantly downregulate the expression of M2 macrophage-related factors and up-regulate the expression of M1 macrophagerelated factors.

关键词： single-walled carbon nanohorns doxorubicin pH-sensitive liposome interleukin-21 tumor associated macrophages

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Applications of single-walled carbon nanohorns and Their Toxicities

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复旦学报（自然科学版） 2007年第5期46卷 698-页

作者： Jin Miyawaki Masako Yudasaka Sumio Iijima Japan Science and Technology Agency c/o NEC

1 Results single-walled carbon nanohorn (SWNH) aggregate ,composed of thousands of graphitic tubules (2 -5nmin diameter and 40 -50 nminlength) with a conical"horn-like"cap,has spherical structure with a diam-eter of about 100 nm(Fig.1)[1].The SWNHs contain no metal catalyst ,because they are produced bylaserablation of pure graphite targets .

关键词： single-walled carbon nanohorns applications toxicity in vivo visualization

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