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喹硫平白蛋白纳米粒作为脑内沉积及潜在改善抗精神病活性的有效平台。

Quetiapine Albumin Nanoparticles as an Efficacious Platform for Brain Deposition and Potentially Improved Antipsychotic Activity.

作者信息

Abdel-Bar Hend Mohamed, Tulbah Alaa S, Darwish Hany W, Salama Rania, Naguib Ibrahim A, Yassin Heba A, Abo El-Enin Hadel A

机构信息

Department of Pharmaceutics, Faculty of Pharmacy, University of Sadat City, Sadat City 32897, Egypt.

Institute of Pharmaceutical Science, Faculty of Life Sciences & Medicine, King's College London, London SE1 9NH, UK.

出版信息

Pharmaceutics. 2023 Jun 21;15(7):1785. doi: 10.3390/pharmaceutics15071785.

DOI:10.3390/pharmaceutics15071785
PMID:37513972
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10385742/
Abstract

Quetiapine (QP) is a second-generation short-acting antipsychotic drug extensively metabolized in the liver, producing pharmacologically inactive metabolites and leading to diminished bioavailability. Therefore, this study aimed to develop an intravenous QP albumin nanoparticles (NPs) system for improving QP antipsychotic activity and brain targeting. QP-loaded albumin NPs were prepared by the desolvation method. The fabricated NPs were characterized in terms of particle size, zeta potential, entrapment efficiency (EE%), and in vitro drug release. In vivo pharmacokinetics and biodistribution in rats were studied. In addition, the antipsychotic activity of the optimized platform was also investigated. Human serum albumin (HSA) concentration, pH, and stirring time were modulated to optimize QP albumin NPs with a particle size of 103.54 ± 2.36 nm and a QP EE% of 96.32 ± 3.98%. In addition, the intravenous administration of QP albumin NPs facilitated QP brain targeting with a 4.9-fold increase in targeting efficiency compared to the oral QP solution. The QP albumin NPs improved the QP antipsychotic activity, indicated by suppressing rats' hypermobility and reducing the QP's extrapyramidal side effects. The obtained results proposed that intravenous QP- NPs could improve QP brain targeting and its antipsychotic efficiency.

摘要

喹硫平（QP）是一种第二代短效抗精神病药物，在肝脏中广泛代谢，产生药理活性不高的代谢产物，导致生物利用度降低。因此，本研究旨在开发一种静脉注射用QP白蛋白纳米粒（NPs）系统，以提高QP的抗精神病活性和脑靶向性。采用去溶剂化法制备了载有QP的白蛋白纳米粒。对制备的纳米粒进行了粒径、zeta电位、包封率（EE%）和体外药物释放等方面的表征。研究了大鼠体内的药代动力学和生物分布。此外，还研究了优化平台的抗精神病活性。调节人血清白蛋白（HSA）浓度、pH值和搅拌时间，以优化粒径为103.54±2.36nm、QP EE%为96.32±3.98%的QP白蛋白纳米粒。此外，与口服QP溶液相比，静脉注射QP白蛋白纳米粒促进了QP的脑靶向性，靶向效率提高了4.9倍。QP白蛋白纳米粒提高了QP的抗精神病活性，表现为抑制大鼠的多动并减少QP的锥体外系副作用。所得结果表明，静脉注射QP纳米粒可提高QP的脑靶向性及其抗精神病效率。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efa5/10385742/3c1955042b1a/pharmaceutics-15-01785-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efa5/10385742/6351a66e2c8e/pharmaceutics-15-01785-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efa5/10385742/74880dfcace2/pharmaceutics-15-01785-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efa5/10385742/5cc582407d22/pharmaceutics-15-01785-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efa5/10385742/d41c6fef33ec/pharmaceutics-15-01785-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efa5/10385742/a5182447f5d8/pharmaceutics-15-01785-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efa5/10385742/91c88836e391/pharmaceutics-15-01785-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efa5/10385742/918849f7a781/pharmaceutics-15-01785-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efa5/10385742/fc5fc0957e17/pharmaceutics-15-01785-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efa5/10385742/33848c07e913/pharmaceutics-15-01785-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efa5/10385742/3c1955042b1a/pharmaceutics-15-01785-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efa5/10385742/6351a66e2c8e/pharmaceutics-15-01785-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efa5/10385742/74880dfcace2/pharmaceutics-15-01785-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efa5/10385742/5cc582407d22/pharmaceutics-15-01785-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efa5/10385742/d41c6fef33ec/pharmaceutics-15-01785-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efa5/10385742/a5182447f5d8/pharmaceutics-15-01785-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efa5/10385742/91c88836e391/pharmaceutics-15-01785-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efa5/10385742/918849f7a781/pharmaceutics-15-01785-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efa5/10385742/fc5fc0957e17/pharmaceutics-15-01785-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efa5/10385742/33848c07e913/pharmaceutics-15-01785-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efa5/10385742/3c1955042b1a/pharmaceutics-15-01785-g010.jpg

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