Versatile Polymeric Microspheres with Tumor Microenvironment Bioreducible Degradation, pH-Activated Surface Charge Reversal, pH-Triggered “off–on” Fluorescence and Drug Release as Theranostic Nanoplatforms,Molecular Pharmaceutics

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Versatile Polymeric Microspheres with Tumor Microenvironment Bioreducible Degradation, pH-Activated Surface Charge Reversal, pH-Triggered “off–on” Fluorescence and Drug Release as Theranostic Nanoplatforms
Molecular Pharmaceutics ( IF 4.5 ) Pub Date : 2018-12-07 00:00:00 , DOI: 10.1021/acs.molpharmaceut.8b00957
Mingliang Pei ₁ , Xu Jia ₁ , Guoping Li ₁ , Peng Liu ₁

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Facile approach has been developed for the versatile polymeric microspheres with tumor microenvironment bioreducible degradation, pH-activated surface charge reversal, pH-triggered “off-on” fluorescence, and drug release via emulsion copolymerization of glycidyl methacrylate (GMA), poly(ethylene glycol) methyl ether methacrylate (PEGMA), and N-rhodamine 6G-ethyl-acrylamide (Rh6GEAm) with N,N-bis(acyloyl)cystamine) (BACy) as disulfide cross-linker and functionalization. The final PGMA-DMMA microspheres showed excellent cytocompatibility, pH-triggered surface charge reversal at pH 5–6, strong fluorescence only in acidic media, and bioreducible degradation with high reductant level, indicating their promising application as theranostic nanoplatforms for precise imaging-guided diagnosis and chemotherapy. The DOX-loaded PGMA-DMMA microspheres with a drug-loading capacity of 18% and particle size of about 150 nm possessed unique pH/reduction dual-responsive controlled release, with a cumulative DOX release of 60.5% within 54 h at the simulated tumor microenvironment but a premature leakage of <8.0% under the simulated physiological condition. Enhanced inhibition efficacy against HepG2 cells was achieved compared to free DOX.

中文翻译：

具有肿瘤微环境生物可还原降解，pH活化的表面电荷逆转，pH触发的“关闭”荧光和药物释放的多功能聚合物微球，作为治疗型纳米平台

已开发出适用于多功能聚合物微球的简便方法，该微球具有肿瘤微环境可生物还原的降解，pH活化的表面电荷逆转，pH触发的“关闭”荧光以及通过甲基丙烯酸缩水甘油酯（GMA），聚乙二醇的乳液共聚释放药物）甲基醚甲基丙烯酸酯（PEGMA），和ñ -Rhodamine 6G乙基丙烯酰胺（Rh6GEAm）与ñ，ñ-双（酰基）胱胺）（BACy）作为二硫键交联剂和官能化。最终的PGMA-DMMA微球表现出优异的细胞相容性，pH激发的pH在5-6时逆转的表面电荷，仅在酸性介质中具有强荧光以及具有高还原水平的可生物还原的降解，表明它们有望作为治疗性纳米平台用于精确的成像指导诊断和化学疗法。载药量为18％，粒径约150 nm的载有DOX的PGMA-DMMA微球具有独特的pH /还原双重响应控制释放，模拟肿瘤在54 h内累积DOX释放为60.5％。微环境，但在模拟的生理条件下过早泄漏小于8.0％。与游离DOX相比，获得了增强的针对HepG2细胞的抑制效力。

更新日期：2018-12-07

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