Abstract
Nose-to-brain drug delivery has recently attracted enormous attention as an alternative to other delivery routes, including the most popular oral one. Due to the unique anatomical features of the nasal cavity, drugs administered intranasally can be delivered directly to the central nervous system. The most important advantage of this approach is the ability to avoid the blood–brain barrier surrounding the brain and blocking the entry of exogenous substances to the central nervous system. Moreover, selective brain targeting could possibly avoid peripheral side effects of pharmacotherapy. The challenges associated with nose-to-brain drug delivery are mostly due to the small volume of the nasal cavity and insufficient drug absorption from nasal mucosa. These issues could be minimized by using a properly designed drug carrier. Microemulsions as potential drug delivery systems offer good solubilizing properties and the ability to enhance drug permeation through biological membranes. The aim of this review is to summarize the current status of the research focused on microemulsion-based systems for nose-to-brain delivery with special attention to the most extensively investigated neurological and psychiatric conditions, such as neurodegenerative diseases, epilepsy, and schizophrenia.
Highlights
Efficient delivery of active pharmaceutical ingredients (APIs) to the brain is crucial for successful therapy of numerous neurological and psychiatric disorders
Florence et al [146] published the results of a study aiming at the formulation of an intranasal, mucoadhesive oil-water (O/W) microemulsion for nose-to-brain delivery of clobazam, an anticonvulsant benzodiazepine drug used for the treatment of different epilepsy types and applied in some psychiatric disorders manifesting with anxiety
Capmul® MCM EP, Labrasol®, Transcutol® P, water, chitosan in vitro: Franz cells, cellulose acetate membrane in vivo: male Sprague-Dawley rats, blood and brain concentration, gamma scintigraphy visualization addition of chitosan contributed to higher brain concentration of the drug rivastigmine hydrogen tartrate
Summary
Efficient delivery of active pharmaceutical ingredients (APIs) to the brain is crucial for successful therapy of numerous neurological and psychiatric disorders. The most important feature determining its properties is the presence of tight junctions in the paracellular space between adjacent cells These structures consisting of several specific transmembrane proteins, like claudin, occludin, and junction adhesion molecules [2], are essential for limiting the permeability of the BBB to hydrophilic molecules including drugs. Approach tide-based active ingredients can be transformed into their elements cationic form, has Another the involves applying inactive display better to penetrate across the ability to interact with negatively charged prodrugs, structural which elements of the BBBability [22]. Nano-Recently, one of the most non-invasive methods forRecently, drug delivery particulate systems [29,30]extensively in order toinvestigated improve their ability to cross the BBB. Microemulsions can be considered as promising vehicles for different therapeutic agents delivered in this way; they are not free from drawbacks and the summarized research show some questions that have not been properly addressed yet
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