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地西他滨包载生物素-玉米醇溶蛋白偶联纳米粒的制备、表征及评价

Decitabine enclosed biotin-zein conjugated nanoparticles: synthesis, characterization, and evaluation.

机构信息

Department of Pharmaceutics, National Institute of Pharmaceutical Education & Research (NIPER)-Raebareli, Lucknow, Uttar Pradesh, 226002, India.

Department of Pharmacology & Toxicology, National Institute of Pharmaceutical Education & Research (NIPER)-Raebareli, Lucknow, Uttar Pradesh, 226002, India.

出版信息

Nanomedicine (Lond). 2024;19(21-22):1743-1760. doi: 10.1080/17435889.2024.2374700. Epub 2024 Jul 23.

Abstract

This study focuses on biotinylated nanocarriers designed to encapsulate amphiphilic molecules with self-biodegradable properties for enhanced drug delivery. Biotin-zein conjugated nanoparticles were synthesized and tested in C6 cell lines to evaluate their viability and cellular uptake. Optimization was achieved using a a central composite design. The nanoparticles underwent thermogravimetric analysis, and their pharmacokinetics and biodistribution were also studied. The optimized nanoparticles displayed 96.31% drug encapsulation efficiency, a particle size of 95.29 nm and a zeta potential of -17.7 mV. These nanoparticles showed increased cytotoxicity and improved cellular uptake compared with free drugs. Thermogravimetric analysis revealed that the drug-loaded nanocarriers provided better protection against drug degradation. Pharmacokinetic and biodistribution studies indicated that the formulation had an extended brain residence time, highlighting its effectiveness. The biotin-zein conjugated nanoparticles developed in this study offer a promising nano-vehicle for biodistribution and pharmacokinetic applications. Their high drug encapsulation efficiency, stability and extended brain residence time suggest they are effective for targeted drug delivery and therapeutic uses.

摘要

本研究专注于设计生物素化纳米载体,用于封装具有自降解特性的两亲性分子,以增强药物传递。合成了生物素-玉米醇溶蛋白缀合物纳米颗粒,并在 C6 细胞系中进行了测试,以评估其细胞活力和细胞摄取。使用中心复合设计进行了优化。对纳米颗粒进行了热重分析,并研究了它们的药代动力学和生物分布。优化后的纳米颗粒显示出 96.31%的药物包封效率、95.29nm 的粒径和-17.7mV 的 zeta 电位。与游离药物相比,这些纳米颗粒显示出更高的细胞毒性和改善的细胞摄取。热重分析表明,载药纳米载体能更好地保护药物降解。药代动力学和生物分布研究表明,该制剂具有延长的脑驻留时间,突出了其有效性。本研究开发的生物素-玉米醇溶蛋白缀合纳米颗粒为生物分布和药代动力学应用提供了一种有前途的纳米载体。它们具有高的药物包封效率、稳定性和延长的脑驻留时间,表明它们可有效用于靶向药物递送和治疗用途。

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