Journal
ACTA PHARMACEUTICA SINICA B
Volume 11, Issue 4, Pages 925-940Publisher
INST MATERIA MEDICA, CHINESE ACAD MEDICAL SCIENCES
DOI: 10.1016/j.apsb.2021.02.012
Keywords
Nose-to-brain delivery; Intranasal administration; Nanostructured lipid carriers; NLC; Solid lipid nanoparticles; SLN; Nanoemulsions; In vivo studies; Pharmacokinetic; Pharmacodynamics
Categories
Funding
- Fundaca o para a Ciencia e a Tecnologia (FCT) (Portugal) [SFRH/136177/2018]
- Applied Molecular Biosciences Unit-UCIBIO - FCT [UIDP/04378/2020, UIDB/04378/2020]
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The management of CNS disorders is challenging due to the need for drugs to cross the BBB and reach the brain. Using the intranasal route combined with lipid-based nanocarriers has shown promising results in targeting drugs to the brain. Although the exact mechanism remains unclear, these systems are more effective than other routes and are expected to be approved by regulatory authorities in the future.
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. (C) 2021 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V.
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