苯基硼酸修饰的硫酸软骨素A基治疗纳米颗粒增强了肿瘤的靶向和穿透能力。,Advanced Functional Materials

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苯基硼酸修饰的硫酸软骨素A基治疗纳米颗粒增强了肿瘤的靶向和穿透能力。
Advanced Functional Materials ( IF 18.5 ) Pub Date : 2015-05-08 , DOI: 10.1002/adfm.201500680
Jae-Young Lee ₁ , Suk-Jae Chung ₁ , Hyun-Jong Cho ₂ , Dae-Duk Kim ₁

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准备了基于苯硼酸功能化的硫酸软骨素A（CSA）-脱氧胆酸（DOCA）的纳米颗粒（NPs），用于靶向和穿透肿瘤。（3-氨基甲基苯基）硼酸（AMPB）通过酰胺键形成与CSA-DOCA共轭物共轭，其成功合成已通过质子核磁共振波谱证实（¹1 H-NMR）。准备了阿霉素（DOX）负载的CSA–DOCA–AMPB NP，它们的平均直径约为200 nm，具有窄的尺寸分布，负的zeta电位和球形形态。与生理pH相比，在酸性pH下从NP释放的DOX增强。与共聚焦激光扫描显微镜和流式细胞术相比，与CSA-DOCA NP相比，CSA-DOCA-AMPB NPs在A549（人肺腺癌）细胞中的细胞摄取有所改善，并渗透到A549多细胞球体中。利用CSA-CD44受体和硼酸-唾液酸的相互作用，通过CSA-DOCA-AMPB NPs体内靶向和穿透肿瘤，通过近红外荧光（NIRF）成像得以揭示。在A549肿瘤异种移植小鼠模型中观察到NP渗透到肿瘤块的核心，并通过三维NIRF成像进行了验证。DOX加载的CSA–DOCA–AMPB NP的多次静脉注射可有效抑制异种移植小鼠模型中A549肿瘤的生长并增加细胞凋亡。这些富含硼酸的NPs有望用于癌症治疗和影像学。

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Phenylboronic Acid‐Decorated Chondroitin Sulfate A‐Based Theranostic Nanoparticles for Enhanced Tumor Targeting and Penetration

Phenylboronic acid‐functionalized chondroitin sulfate A (CSA)–deoxycholic‐acid (DOCA)‐based nanoparticles (NPs) are prepared for tumor targeting and penetration. (3‐Aminomethylphenyl)boronic acid (AMPB) is conjugated to CSA–DOCA conjugate via amide bond formation, and its successful synthesis is confirmed using proton nuclear magnetic resonance spectroscopy (¹H‐NMR). Doxorubicin (DOX)‐loaded CSA–DOCA–AMPB NPs with a mean diameter of ≈200 nm, a narrow size distribution, negative zeta potential, and spherical morphology are prepared. DOX release from NPs is enhanced at acidic pH compared to physiological pH. CSA–DOCA–AMPB NPs exhibit improved cellular uptake in A549 (human lung adenocarcinoma) cells and penetration into A549 multicellular spheroids compared to CSA–DOCA NPs as evidenced by confocal laser scanning microscopy and flow cytometry. In vivo tumor targeting and penetrating by CSA–DOCA–AMPB NPs, based on both CSA–CD44 receptor and boronic acid–sialic acid interactions, is revealed using near‐infrared fluorescence (NIRF) imaging. Penetration of NPs to the core of the tumor mass is observed in an A549 tumor xenografted mouse model and verified by three‐dimensional NIRF imaging. Multiple intravenous injections of DOX‐loaded CSA–DOCA–AMPB NPs efficiently inhibit the growth of A549 tumor in the xenografted mouse model and increase apoptosis. These boronic acid‐rich NPs are promising candidates for cancer therapy and imaging.

更新日期：2015-05-08

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