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用于鼻腔/鼻内给药的脂质纳米颗粒

Lipid Nanoparticles for Nasal/Intranasal Drug Delivery.

作者信息

Cunha S, Amaral M H, Lobo J M Sousa, Silva Ana C

机构信息

UCIBIO, ReQuimTe, Laboratory of Pharmaceutical Technology/Centre of Research in Pharmaceutical Sciences, Faculty of Pharmacy, Porto University, Porto, Portugal.

UCIBIO, ReQuimTe, Laboratory of Pharmaceutical Technology/Centre of Research in Pharmaceutical Sciences, Faculty of Pharmacy, Porto University, Porto, Portugal; UFP Energy, Environment and Health Research Unit (FP-ENAS), Universidade Fernando Pessoa, Porto, Portugal.

出版信息

Crit Rev Ther Drug Carrier Syst. 2017;34(3):257-282. doi: 10.1615/CritRevTherDrugCarrierSyst.2017018693.

Abstract

Studies on the development of drug delivery systems have increased because these systems have particular characteristics that allow them to improve therapeutics. Among these, lipid nanoparticles (solid lipid nanoparticles, SLNs; and nanostructured lipid carriers, NLCs) have demonstrated suitability for drug targeting. The nasal administration of drug-loaded lipid nanoparticles showed effectiveness in treating central nervous system (CNS) disorders, particularly neurodegenerative diseases, because the nasal route (also called intranasal route) allows direct nose-to-brain drug delivery by means of lipid nanoparticles. Nonetheless, the feasibility of this application remains an open field for researchers. Drawbacks must be overcome before reaching the clinic (e.g., drug absorption at subtherapeutic levels, rapid mucociliary clearance). The intranasal administration of drugs for systemic absorption is effective for treating other conditions, such as cardiovascular diseases, infections, severe pain, and menopausal syndrome. In the near future, it is expected that patients will benefit from the advantages of lipid nanoparticle-based formulations, via the nasal/intranasal route, which bypasses the blood-brain barrier (BBB), avoiding first-pass metabolism and gastrointestinal degradation. This review discusses the use of SLNs and NLCs for nasal drug administration. A brief description of the nasal route and the features of SLNs and NLCs is initially provided.

摘要

由于药物递送系统具有能够改善治疗效果的特殊特性,对其开发的研究有所增加。其中,脂质纳米粒(固体脂质纳米粒,SLNs;以及纳米结构脂质载体,NLCs)已显示出适用于药物靶向。载药脂质纳米粒的鼻腔给药在治疗中枢神经系统(CNS)疾病,特别是神经退行性疾病方面显示出有效性,因为鼻腔途径(也称为鼻内途径)允许通过脂质纳米粒实现直接的鼻脑药物递送。尽管如此,这种应用的可行性对研究人员来说仍是一个有待开拓的领域。在进入临床之前必须克服一些缺点(例如,亚治疗水平的药物吸收、快速的黏液纤毛清除)。用于全身吸收的药物鼻腔给药对治疗其他病症有效,如心血管疾病、感染、剧痛和更年期综合征。在不久的将来,预计患者将通过鼻腔/鼻内途径从基于脂质纳米粒的制剂的优势中受益,该途径绕过血脑屏障(BBB),避免首过代谢和胃肠道降解。本综述讨论了SLNs和NLCs在鼻腔给药中的应用。最初简要介绍了鼻腔途径以及SLNs和NLCs的特性。

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