Special Issue "Nose to Brain Delivery"
A special issue of Pharmaceutics (ISSN 1999-4923).
Deadline for manuscript submissions: 31 August 2018
The blood-brain barrier (BBB) separates the central nervous system (CNS) from general circulation. Drugs targeting the brain represent a remarkable problem, owing to BBB, which does not allow most drugs to pass through it. The use of a nose-to-brain delivery route is an important and noninvasive method of drug delivery to solve this problem and bypass the BBB. Different strategies have been developed to enhance nose-to-brain drug delivery. In fact, it is well-known that an intranasal direct anatomical connection between the nasal cavity and the CNS exists, which suggests the development of nasal formulations for brain targeting of drugs. The design and preparation of nasal formulations involve the development of polymeric pharmaceutical platforms able to interact with nasal mucosa: Bioadhesion and penetration enhancement through nasal mucosa layers are the first and most important characteristics that these systems must have. The development of new nasal systems represents a great challenge in the field of controlled drug targeting and delivery.
This Special Issue has the aim of highlighting current progress in the use of the nasal route for brain targeting.
Prof. Paolo Giunchedi
Prof. Elisabetta Gavini
Prof. Maria Cristina Bonferoni
Manuscript Submission Information
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- Nasal route
- Brain targeting
- Transmucosal delivery
- Penetration enhancers
The below list represents only planned manuscripts. Some of these manuscripts have not been received by the Editorial Office yet. Papers submitted to MDPI journals are subject to peer-review.
Tentative Title: Nose to brain delivery of antiviral drugs: a way to overcome their active efflux?
Author: Alessandro Dalpiaz
Abstarct: The review will focus the dramatic difficulties of antiviral drugs to penetrate in the brain from the bloodstream, being substrates of active efflux transporters. These transporters, located in the physiological barriers between blood and CNS, are able to recognize their substrates and to actively efflux them into the bloodstream. The review will describe the types of active transporters known to efflux the antiviral drugs. Moreover, potential inhibitors of these active transporters will be also considered, evidencing however that their possible co-administration causes in general serious unwanted effects. The nasal administration of antiviral drugs will be therefore proposed in order to overcome the problems above described. The antiviral drugs and the nasal formulations adopted will be described, evidencing their efficacy for the brain targeting. Finally, new prodrugs based on bile acids able to elude, without inhibiting, the active efflux transporters will be described and proposed as potential anti HIV agents able to efficaciously penetrate into macrophages of central nervous system, one of most important HIV Sanctuaries of the body, following nasal administration.
Tentative Title: Versatile mucohadesive niosomes: a deep physico-chemical characterization
Author: Maria Carafa
Abstract: The aim of this study is to prepare suitable chitosan-glutamate(CG) coated non-ionic surfactant vesicles for intranasal delivery. Different vesicles were prepared using several non-ionic surfactants, cholesterol and chitosan glutamate. The interaction between CG coated niosomes and different mucin concentrations was studied to obtain vesicles with mucoadhesive properties. The size, ζ-potential and pH of the nanocarriers were controlled during the study to be suited for nasal delivery. Furthermore, fluorimetric analysis was carried out to investigate fluidity, microviscosity, polarity of vesicle bilayer and turbidity of CGcoated niosome suspensions. The physical-chemical stability of niosome suspensions were tested at two different storage temperatures, 4ºC and room temperature, following the size and ζ-potential. Additionally, stability studies in artificial biological fluids were carried out. Morphology studies using Atomic Force Microscopy (AFM) was employed for niosomes, CG coated-niosomes and CG coated-niosomes with mucin.
Tentative Title: Surface-modified nanoparticles for nose-to-brain delivery: from bioadhesion to targeting
Author: F. Sonvico, A. Clementino, F. Buttini, S. Guterres, A. Raffin
Abstract: In the field of nasal delivery, one of the most fascinating applications is the delivery of drugs directly to the central nervous system avoiding the blood brain barrier. This approach would provide a series of benefits, such as the reduction of doses and the localization of potent drugs reducing their systemic side effects. Recently, clinical trials have been explored the nasal administration of insulin for the treatment of Alzheimer’s disease, with promising results. The use of nanomedicines could provide further options for making nose-to-brain delivery reality. In particular, apart from the selection of devices able for the deposition of the formulation in the upper part of the nose, the surface modification of these nanomedicines appears to constitute the key to optimize the delivery of drugs from the nasal cavity to the brain. In this review, the use of surface electrostatic charges, mucoadhesive polymers, such as polysaccharides, as well as targeting moieties directed towards specific proteins on the surface of olfactory cells in the design of nanomedicines for nasal administration would be described and critically evaluated for nose-to-brain delivery.
Tentative Title: Nose to Brain Delivery of Polymeric Nanoparticles for Epilepsy Disease: an overview
Authors: Teresa Musumeci1, Angela Bonaccorso and Giovanni Puglisi
Abstract: Epilepsy is the 4th most common neurological problem affecting world population, which can be considered a spectrum disorder because of its several causes, seizure types, its ability to vary in severity and impact from person to person, and its range of co-existing conditions. The approaches to drug therapy of epilepsy are directed at the control of symptoms by chronic administrations of antiepileptic drugs. The AED are administered orally or intravenously but alternative routes of administration are needed to overcome the limits. Intranasal administration represents an attractive route because it is possible to reach the brain bypassing blood brain barrier and the drug avoids first pass metabolism. It is possible to obtain an increase in patient compliance for the easy and non-invasive way of administration. This route shows some drawbacks such as mucociliar clearance and the small volume that could be administrated, in fact only drugs that are efficacy at low doses can be considered. The drug also needs excellent aqueous solubility or must be able to be formulated using solubilizing agents. The use of nanomedicine formulations able to encapsulate active molecules represents a good strategy in order to overcome several limitations of this route and of conventional drug. The aim of this review is to describe the innovative application of nanomedicine for epilepsy treatment using nose to brain delivery.