静电喷雾微调颗粒尺寸,提高水溶性差药物的口服生物利用度

IF 10.7 1区 医学 Q1 PHARMACOLOGY & PHARMACY Asian Journal of Pharmaceutical Sciences Pub Date : 2024-10-01 DOI:10.1016/j.ajps.2024.100953
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引用次数: 0

摘要

虽然喷雾干燥技术已被广泛用于改善水溶性差药物的生物利用度,但其结果往往表现出粒度分布不理想和粒径过大的问题,从而限制了其有效性。在本研究中,我们介绍了静电喷雾技术,这是一种专为水溶性差的药物量身定制的先进技术,能制造出粒度分布均匀的精细纳米颗粒。以瑞戈非尼(1 克)为模型药物,将聚维酮(5 克)和十二烷基硫酸钠(0.1 克)溶解在 200 毫升乙醇中,分别进行传统喷雾干燥和静电喷雾干燥。与传统喷雾干燥纳米粒子(CSDN)相比,静电喷雾干燥纳米粒子(ESDN)的粒径更小,均匀性更好。研究表明,ESDN 能在更大程度上诱导 HCT-116 细胞凋亡,与 CSDN 相比具有更强的细胞毒性。此外,与 CSDN 相比,ESDN 大大提高了口服生物利用度和抗肿瘤疗效。这些研究结果表明,ESD 在为水溶性差的药物开发增强型给药系统方面具有潜力,能有效解决 CSD 方法的相关局限性。
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Electrostatic spraying for fine-tuning particle dimensions to enhance oral bioavailability of poorly water-soluble drugs
While spray-drying has been widely utilized to improve the bioavailability of poorly water-soluble drugs, the outcomes often exhibit suboptimal particle size distribution and large particle sizes, limiting their effectiveness. In this study, we introduce electrostatic spraying as an advanced technology tailored for poorly water-soluble drugs, enabling the fabrication of nanoparticles with fine and uniform particle size distribution. Regorafenib (1 g), as a model drug, copovidone (5 g), and sodium dodecyl sulfate (0.1 g) were dissolved in 200 ml ethanol and subjected to conventional-spray-dryer and electrostatic spray dryer. The electrostatic spray-dried nanoparticles (ESDN) showed smaller particle sizes with better uniformity compared to conventional spray-dried nanoparticles (CSDN). ESDN demonstrated significantly enhanced solubility and rapid release in water. In vitro studies revealed that ESDN induced apoptosis in HCT-116 cells to a greater extent, exhibiting superior cytotoxicity compared to CSDN. Furthermore, ESDN substantially improved oral bioavailability and antitumor efficacy compared to CSDN. These findings suggest that ESD shows potential in developing enhanced drug delivery systems for poorly water-soluble drugs, effectively addressing the limitations associated with CSD methods.
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来源期刊
Asian Journal of Pharmaceutical Sciences
Asian Journal of Pharmaceutical Sciences Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
18.30
自引率
2.90%
发文量
11
审稿时长
14 days
期刊介绍: The Asian Journal of Pharmaceutical Sciences (AJPS) serves as the official journal of the Asian Federation for Pharmaceutical Sciences (AFPS). Recognized by the Science Citation Index Expanded (SCIE), AJPS offers a platform for the reporting of advancements, production methodologies, technologies, initiatives, and the practical application of scientific knowledge in the field of pharmaceutics. The journal covers a wide range of topics including but not limited to controlled drug release systems, drug targeting, physical pharmacy, pharmacodynamics, pharmacokinetics, pharmacogenomics, biopharmaceutics, drug and prodrug design, pharmaceutical analysis, drug stability, quality control, pharmaceutical engineering, and material sciences.
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