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经美国食品药品监督管理局批准的药物经鼻至脑给药在改善抑郁症和精神疾病管理方面的进展。

Advancement in the Nose-to-Brain Drug delivery of FDA-approved drugs for the better management of Depression and Psychiatric disorders.

作者信息

Upadhyay Rajshekher, Ghosh Pappu, Desavathu Madhuri

机构信息

Department of Pharmacy, School of Chemical Sciences and Pharmacy, Central University of Rajasthan, Kishangarh, Ajmer 305817, Rajasthan, India.

Department of Pharmacy, School of Chemical Sciences and Pharmacy, Central University of Rajasthan, Kishangarh, Ajmer 305817, Rajasthan, India.

出版信息

Int J Pharm. 2024 Dec 25;667(Pt B):124866. doi: 10.1016/j.ijpharm.2024.124866. Epub 2024 Oct 30.

DOI:10.1016/j.ijpharm.2024.124866
PMID:39486490
Abstract

The Prevalence of Depressive and Psychiatric disorders is increasing globally, and despite the availability of numerous FDA-approved drugs, treatment remains challenging. Many conventional antidepressants and antipsychotic formulations face issues such as low solubility, high first-pass metabolism, poor bioavailability, inadequate blood-brain barrier penetration, and systemic side effects. These challenges lead to reduced efficacy, slower onset of action, and decreased patient adherence to treatment. To address these problems, recent studies have explored the nose-to-brain route for drug delivery. This method offers several advantages, including non-invasive drug administration, direct access to the brain, rapid onset of action, reduced systemic exposure and side effects, avoidance of first-pass metabolism, enhanced bioavailability, precision dosing, and improved patient compliance. The formulations used for this approach include lipidic nanoparticles, polymeric nanoparticles, nasal gels, cubosomes, niosomes, polymeric micelles, nanosuspensions, nanoemulsions, nanocapsules, and elastosomes. This review analyzes and summarizes the published work on the nose-to-brain delivery of FDA-approved antidepressants and antipsychotic drugs, with a focus on the preparation, characterization, pharmacokinetics, pharmacodynamics, and toxicity profiling of these nanoformulations.

摘要

全球范围内,抑郁症和精神疾病的患病率正在上升,尽管有许多获得美国食品药品监督管理局(FDA)批准的药物,但治疗仍然具有挑战性。许多传统的抗抑郁药和抗精神病药物制剂面临着诸如溶解度低、首过代谢高、生物利用度差、血脑屏障穿透不足以及全身副作用等问题。这些挑战导致疗效降低、起效缓慢以及患者对治疗的依从性下降。为了解决这些问题,最近的研究探索了药物经鼻入脑的给药途径。这种方法具有多种优势,包括非侵入性给药、直接进入大脑、起效迅速、全身暴露和副作用减少、避免首过代谢、提高生物利用度、精准给药以及改善患者依从性。用于这种方法的制剂包括脂质纳米颗粒、聚合物纳米颗粒、鼻用凝胶、立方液晶、囊泡、聚合物胶束、纳米混悬液、纳米乳剂、纳米胶囊和弹性体。这篇综述分析并总结了已发表的关于FDA批准的抗抑郁药和抗精神病药物经鼻入脑给药的研究工作,重点关注这些纳米制剂的制备、表征、药代动力学、药效学和毒性分析。

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引用本文的文献

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Front Psychiatry. 2025 Jul 15;16:1599038. doi: 10.3389/fpsyt.2025.1599038. eCollection 2025.
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The intersection of circadian rhythms and the blood-brain barrier with drug efficacy and delivery in neurological disorders.昼夜节律与血脑屏障在神经疾病中的药物疗效和递送方面的交叉。
Adv Drug Deliv Rev. 2025 Jul 2;224:115645. doi: 10.1016/j.addr.2025.115645.
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The Nasal-Brain Drug Delivery Route: Mechanisms and Applications to Central Nervous System Diseases.
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MedComm (2020). 2025 Jun 6;6(6):e70213. doi: 10.1002/mco2.70213. eCollection 2025 Jun.