Enhanced Oral Bioavailability and Biodistribution of Voriconazole through Zein-Pectin-Hyaluronic Acid Nanoparticles

IF 8.2 2区材料科学 Q1 MATERIALS SCIENCE, MULTIDISCIPLINARY ACS Applied Materials & Interfaces Pub Date : 2024-12-19 DOI:10.1021/acsami.4c16326

Margani Taise Fin, Camila Diedrich, Christiane Schineider Machado, Letícia Marina da Silva, Ana Paula Santos Tartari, Isabella Camargo Zittlau, Samila Horst Peczek, Rubiana Mara Mainardes

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Abstract

Nanotechnology-based drug delivery systems offer a solution to the pharmacokinetic limitations of voriconazole (VRC), including saturable metabolism and low oral bioavailability. This study developed zein/pectin/hyaluronic acid nanoparticles (ZPHA-VRC NPs) to improve VRC’s pharmacokinetics and biodistribution. The nanoparticles had a spherical morphology with an average diameter of 268 nm, a zeta potential of −48.7 mV, and an encapsulation efficiency of 88%. Stability studies confirmed resistance to pH variations and digestive enzymes in simulated gastric and intestinal fluids. The in vitro release profile showed a controlled release, with 8% of the VRC released in 2 h and 16% over 24 h. Pharmacokinetic studies in rats demonstrated a 2.8-fold increase in the maximum plasma concentration and a 3-fold improvement in bioavailability compared to free VRC. Biodistribution analysis revealed enhanced VRC accumulation in key organs. These results suggest that ZPHA-VRC NPs effectively improve VRC’s therapeutic potential for oral administration.

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玉米胶-透明质酸纳米颗粒增强伏立康唑的口服生物利用度和生物分布

基于纳米技术的给药系统为伏立康唑（VRC）的药代动力学限制提供了解决方案，包括饱和代谢和低口服生物利用度。本研究开发了玉米蛋白/果胶/透明质酸纳米颗粒（ZPHA-VRC NPs），以改善VRC的药代动力学和生物分布。纳米颗粒呈球形，平均直径为268 nm， zeta电位为- 48.7 mV，包封效率为88%。稳定性研究证实了模拟胃液和肠液对pH变化和消化酶的抗性。体外释放谱显示出控释，其中8%的VRC在2小时内释放，16%在24小时内释放。大鼠药代动力学研究表明，与游离VRC相比，最大血浆浓度增加2.8倍，生物利用度提高3倍。生物分布分析显示VRC在关键器官的积累增强。这些结果表明，ZPHA-VRC NPs可有效提高口服VRC的治疗潜力。

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来源期刊

ACS Applied Materials & Interfaces 工程技术-材料科学：综合

CiteScore

16.00

自引率

6.30%

发文量

4978

审稿时长

1.8 months

期刊介绍： ACS Applied Materials & Interfaces is a leading interdisciplinary journal that brings together chemists, engineers, physicists, and biologists to explore the development and utilization of newly-discovered materials and interfacial processes for specific applications. Our journal has experienced remarkable growth since its establishment in 2009, both in terms of the number of articles published and the impact of the research showcased. We are proud to foster a truly global community, with the majority of published articles originating from outside the United States, reflecting the rapid growth of applied research worldwide.