Intranasal delivery of nanostructured lipid carriers, solid lipid nanoparticles and nanoemulsions: A current overview of in vivo studies.
Intranasal delivery of nanostructured lipid carriers, solid lipid nanoparticles and nanoemulsions: A current overview of in vivo studies.
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DOI：
10.1016/j.apsb.2021.02.012
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发表时间：
2021-04
期刊：
影响因子：
--
通讯作者：
Silva AC
中科院分区：
文献类型：
--
作者：
Costa CP;Moreira JN;Sousa Lobo JM;Silva AC
由于需要药物通过血脑屏障（BBB）到达大脑，中枢神经系统（CNS）疾病的治疗具有挑战性。在已经研究的各种策略中，利用鼻内途径将药物从鼻子直接输送到大脑已经显示出有希望的结果。此外，将药物包封在基于脂质的纳米载体中，如固体脂质纳米颗粒（sln）、纳米结构脂质载体（nlc）或纳米乳（NEs），可以通过增加生物利用度和位点特异性递送来改善鼻到脑的运输。本综述提供了基于脂质的纳米载体（sln， NLCs和NEs）用于鼻到脑输送的体内研究的最新进展。根据过去两年的文献，我们提出了药物经鼻给药后到达大脑的不同机制。报告了药代动力学和药效学研究的结果，并对体内研究中使用的不同动物的鼻腔解剖结构之间的差异进行了批判性分析。虽然药物从鼻子转运到大脑的确切机制尚不完全清楚，其在人类中的有效性也不清楚，但似乎鼻内途径与使用NLCs， sln或NEs一起有利于药物靶向到大脑。这些系统已被证明比其他非封装药物的途径或配方更有效，因此它们有望在未来几年内获得监管机构的批准。大鼠和家兔经鼻给药纳米结构脂质载体（NLC）、固体脂质纳米颗粒（SLN）和纳米乳剂导致脑内药物浓度高于血液，证明了鼻至脑给药的有效性。
The management of the central nervous system (CNS) disorders is challenging, due to the need of drugs to cross the blood‒brain barrier (BBB) and reach the brain. Among the various strategies that have been studied to circumvent this challenge, the use of the intranasal route to transport drugs from the nose directly to the brain has been showing promising results. In addition, the encapsulation of the drugs in lipid-based nanocarriers, such as solid lipid nanoparticles (SLNs), nanostructured lipid carriers (NLCs) or nanoemulsions (NEs), can improve nose-to-brain transport by increasing the bioavailability and site-specific delivery. This review provides the state-of-the-art of in vivo studies with lipid-based nanocarriers (SLNs, NLCs and NEs) for nose-to-brain delivery. Based on the literature available from the past two years, we present an insight into the different mechanisms that drugs can follow to reach the brain after intranasal administration. The results of pharmacokinetic and pharmacodynamics studies are reported and a critical analysis of the differences between the anatomy of the nasal cavity of the different animal species used in in vivo studies is carried out. Although the exact mechanism of drug transport from the nose to the brain is not fully understood and its effectiveness in humans is unclear, it appears that the intranasal route together with the use of NLCs, SLNs or NEs is advantageous for targeting drugs to the brain. These systems have been shown to be more effective for nose-to-brain delivery than other routes or formulations with non-encapsulated drugs, so they are expected to be approved by regulatory authorities in the coming years. Intranasal delivery of nanostructured lipid carriers (NLC), solid lipid nanoparticles (SLN) and nanoemulsions in rats and rabbits resulted in higher drug concentration in the brain, compared to blood, proving the effectiveness of nose-to-brain delivery.
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影响因子：
5.8
作者：
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