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JOURNAL OF POLYMER SCIENCE PART A-POLYMER CHEMISTRY · 2013 ·Vol. 51 ·期 9 ·2049-2057 · IF 3.543

Tandem dynamic kinetic resolution and enzymatic polycondensation to synthesize mPEG-functionalized poly(amine-co-ester)-type chiral prodrugs

Xueqi Qian,Zhengyang Jiang,Xianfu Lin,Qi Wu

Amphiphilic poly(amine-co-ester)s, which contain a single effective enantiomer of an asymmetric drug and thus can avoid potentially serious side effects, are difficult to prepare through nonselective chemical routes not only in the process of introducing chiral drugs to the polymer, but also in the synthesis of the polymer's backbone by metal catalysts. A model of racemic mexiletine, an important antiarrhythmic agent, was used to demonstrate the tandem combination of Candida antarctica lipase B (CAL-B)- and Pd/C-catalyzed dynamic kinetic resolution (DKR) and subsequent CAL-B-catalyzed polycondensation, as an efficient protocol to prepare poly(ethylene glycol)-functionalized poly(amine-co-ester)s containing (R)-mexiletine with 99% ee value. Chemoenzymatic DKR and enzymatic polymerization conditions were optimized, and the optical purity of incorporated (R)-mexiletine was confirmed through its hydrolysis from polyester. The copolymers can readily self-assemble into nanometer-scale-sized micelles with well-dispersed spheres, which have a size distribution that can be efficiently adjusted by changing the polymer concentration. © 2013 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem, 2013

研究领域: 生物化学 · 制药工程 · 高分子化学
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CHEMICAL ENGINEERING JOURNAL · 2023 · IF 15.1

Ratiometric upconversion luminescence sensing platform for visual monitoring of antiarrhythmic drug level in serum

Xiaohui Kang,Lanpeng Zhang,Liang Yang,Changlong Jiang

Arrhythmia seriously threatens life and health, it requires long-term use of antiarrhythmic drugs such as mexiletine and needs to monitor the dosage of drugs in the body to ensure efficacy and avoid serious side effects. Here, we designed a sensing platform for real-time visual monitoring of drug efficacy using a ratiometric upconversion probe, which overcomes the fluorescence background interference in the serum, and improves the resolution and accuracy of visual detection. By combining lanthanide-doped upconversion nanoparticles (UCNPs) with readily available organic dyes, an efficient upconversion nanoprobe was constructed under the reaction mechanism of internal filtration effect (IFE) to realize the quantitative detection of mexiletine in serum. Due to the addition of mexiletine, the characteristic emission peak of the probe at 540 nm changes, while the fluorescence intensity at 655 nm is unchanged. Therefore, the visual detection of mexiletine in serum is realized according to the fluorescence intensity changes of I 540 /I 655 . In addition, the designed sensing platform is combined with a smartphone to realize real-time visualization and quantitative monitoring of mexiletine, and the detection limits in fluorescence and colorimetric modes are as low as 55.6 nM and 469.75 nM respectively, consequently resulting in sensitive monitoring the effective dosage of drugs in the serum. The proposed detection platform provides a new sensing strategy for the visual determination of antiarrhythmic drugs and an instant device to warn the treatment process of the disease immediately.

研究领域: 生物医学工程 · 药理学 · 纳米医学
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