用于阿帕鲁胺定量的新型绿色硼碳量子点的设计、表征及生物制药应用;绿色度评估

Design, Characterization and Biopharmaceutical Applications of Novel Green Boron-Carbon Quantum Dots for Quantification of Apalutamide; Greenness Evaluations.

作者信息

Hassan Yasser F, Alzahrani Eman, Abdel-Lateef Mohamed A, Salman Baher I, Ibrahim Adel Ehab

机构信息

Pharmaceutical Analytical Chemistry Department, Faculty of Pharmacy, Al-Azhar University, Assiut branch, Assiut, 71524, Egypt.

Department of Chemistry, College of Science, Taif University, PO Box 11099, Taif, 21944, Saudi Arabia.

出版信息

J Fluoresc. 2024 Jul 8. doi: 10.1007/s10895-024-03802-w.

Abstract

The diagnosis of prostate cancer has been evolving in the current decade, with expected mortality rates of 499,000 death by the year 2030. Apalutamide (APL) has been approved in 2018 as the first drug for the controlling of prostate cancer. APL significant success warrantied its high global sales, which are expected to surpass 58% of segment market sales (together with another drug; enzalutamide). Therefore, new, fast and environmentally friendly analytical methods are required for its determination for the quality control and biological monitoring purposes. The proposed research designs and evaluates the first fluorimetric approach based on novel porous green boron-doped carbon quantum dots (B@CDs) for the determination of APL in biopharmaceutical matrices. The synthetic approach has high quantum yield (31.15%). B@CDs were characterized using several tools, including transmission electron microscopy (TEM), dynamic light scattering (DLS), FTIR and Energy dispersive X-ray spectroscopy (EDX) which proved their improved surface properties with an average nano-diameter of 3.0 nm. The interaction between B@CDs and APL led to enhancement their fluorescence at 441 nm (excitation at 372 nm). The approach was validated for the determination of APL within concentration range of 15.0-700.0 ng mL with quantification limit LOQ 4.37 ng mL and detection limit LOD 1.44 ng mL. The approach was successfully applied for the determination of APL in human plasma and pharmaceutical monitoring of its marketed tablet form. Then, the approach was assessed for its environmental impact using different metrics and proved its ecological greenness.

摘要

在当前十年中,前列腺癌的诊断方法一直在不断发展,预计到2030年死亡率将达到499,000人。阿帕鲁胺(APL)于2018年获批,成为第一种用于控制前列腺癌的药物。APL的显著成功保证了其全球高销售额,预计将超过细分市场销售额的58%(与另一种药物恩杂鲁胺一起)。因此,需要新的、快速且环保的分析方法来进行质量控制和生物监测,以测定APL。本研究提出并评估了基于新型多孔绿色硼掺杂碳量子点(B@CDs)的第一种荧光分析法,用于测定生物制药基质中的APL。合成方法具有高量子产率(31.15%)。使用多种工具对B@CDs进行了表征,包括透射电子显微镜(TEM)、动态光散射(DLS)、傅里叶变换红外光谱(FTIR)和能量色散X射线光谱(EDX),这些都证明了其具有改善的表面性质,平均纳米直径为3.0纳米。B@CDs与APL之间的相互作用导致其在441纳米处的荧光增强(激发波长为372纳米)。该方法在15.0 - 700.0纳克/毫升的浓度范围内对APL的测定进行了验证,定量限LOQ为4.37纳克/毫升,检测限LOD为1.44纳克/毫升。该方法成功应用于人体血浆中APL的测定及其市售片剂形式的药物监测。然后,使用不同指标评估了该方法对环境的影响,证明了其生态绿色性。

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