负载光敏剂D-甘露糖修饰胶束的制备及其在靶向光动力治疗中的应用

D-Mannose-Conjugated Micelles Loaded with Photosensitizers for Targeted Photodynamic Therapy

DOI：10.3969/j.issn.1673-1689.2019.10.007

中文关键词: D-甘露糖 主客体识别 载光敏剂胶束 受体介导胞吞 靶向光动力治疗

英文关键词: D-mannose,host-guest recognition,BTA-loaded micelles,receptor-mediated endocytosis,targeted photodynamic therapy

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中文摘要:

本研究合成了D-甘露糖修饰的两亲性β-环糊精（C₃-CD-Man₇）和三臂金刚烷共价键连的BODIPY光敏剂（BTA），并利用β-环糊精（β-CD）与金刚烷（Ad）之间超分子主客体识别作用制备表面D-甘露糖修饰的高负载光敏剂胶束（BTA@C₃-CD-Man₇）。利用透射电镜和动态光散射对BTA@C₃-CD-Man₇胶束形貌、粒径和稳定性进行表征；并采用MTT细胞毒性评价方法考察其对人乳腺癌MDA-MB-231细胞的摄入、光动力治疗效果和光毒性。结果表明BTA@C₃-CD-Man₇粒径均一，在溶液中稳定性良好；甘露糖受体过度表达的乳腺癌细胞MDA-MB-231能够特异性识别并大量摄取BTA@C₃-CD-Man₇，并在665 nm LED灯照射下表现出对MDA-MB-231细胞靶向光动力治疗的效果。

英文摘要:

In this paper，the D-mannose-modified amphiphilic β-cyclodextrin（C₃-CD-Man₇） and a three-arm adamantine-conjugated BODIPY photosensitizer（BTA） are synthesized. Because of the presence of supramolecular host-guest interactions between β-cyclodextrin and adamantane，BTA is loaded into the hydrophobic cavity of micelles self-assembled from C3-CD-Man₇，leading to the formation of BTA-loaded micelles（BTA@C₃-CD-Man₇）. The size，morphology，and stability of BTA@C₃-CD-Man₇are characterized by transmission electron microscopy and dynamic light scattering. The cellular uptake，PDT effect，and phototoxicity of BTA@C₃-CD-Man₇are investigated using the MTT assay. The results show that BTA@C₃-CD-Man₇has uniform size distribution and excellent stability in aqueous solution. More importantly，BTA@C₃-CD-Man₇could be specifically internalized by MDA-MB-231 breast cancer cells that overexpress mannose receptors on cell surfaces. Thus，with 665 nm LED irradiation，the enhanced phototoxicity of BTA@C3-CD-Man7 showed their potential for targeted photodynamic therapy applications.

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