Mucoadhesion as a strategy to enhance the direct nose-to-brain drug delivery

Patil, Mrunal U.

doi:10.1016/b978-0-12-822522-6.00007-2

Cited by 6 publications

(3 citation statements)

References 249 publications

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“…It can be achieved by the sol–gel transition of the formulation in contact with the nasal mucosa and is also promoted by the use of mucoadhesive agents. These agents interact with mucins in the mucus layer, decreasing mucociliary clearance and improving formulation mucosal affinity [ 91 ].…”

Section: Resultsmentioning

confidence: 99%

Chitosan-Based Thermogelling System for Nose-to-Brain Donepezil Delivery: Optimising Formulation Properties and Nasal Deposition Profile

et al. 2023

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Donepezil nasal delivery strategies are being continuously investigated for advancing therapy in Alzheimer’s disease. The aim of this study was to develop a chitosan-based, donepezil-loaded thermogelling formulation tailored to meet all the requirements for efficient nose-to-brain delivery. A statistical design of the experiments was implemented for the optimisation of the formulation and/or administration parameters, with regard to formulation viscosity, gelling and spray properties, as well as its targeted nasal deposition within the 3D-printed nasal cavity model. The optimised formulation was further characterised in terms of stability, in vitro release, in vitro biocompatibility and permeability (using Calu-3 cells), ex vivo mucoadhesion (using porcine nasal mucosa), and in vivo irritability (using slug mucosal irritation assay). The applied research design resulted in the development of a sprayable donepezil delivery platform characterised by instant gelation at 34 °C and olfactory deposition reaching a remarkably high 71.8% of the applied dose. The optimised formulation showed prolonged drug release (t1/2 about 90 min), mucoadhesive behaviour, and reversible permeation enhancement, with a 20-fold increase in adhesion and a 1.5-fold increase in the apparent permeability coefficient in relation to the corresponding donepezil solution. The slug mucosal irritation assay demonstrated an acceptable irritability profile, indicating its potential for safe nasal delivery. It can be concluded that the developed thermogelling formulation showed great promise as an efficient donepezil brain-targeted delivery system. Furthermore, the formulation is worth investigating in vivo for final feasibility confirmation.

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Section: Resultsmentioning

confidence: 99%

Chitosan-Based Thermogelling System for Nose-to-Brain Donepezil Delivery: Optimising Formulation Properties and Nasal Deposition Profile

et al. 2023

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“…Mucoadhesion is the phenomenon defined by the sustainable adhesive attraction between a mucosal surface and a second biological or synthetic (most often polymeric) substrate. The utilization of mucoadhesive excipients is an integral part of the design of mucosal dosage forms since they ensure a prolonged retention, intimate contact with the mucosa, and resilience of the emerging film to gravity and unfavorable physiological processes at the site of application (such as the nasal mucociliary clearance and the great oscillatory stress in the oral cavity) [ 13 , 204 ]. Mucoadhesive properties are inherent for many polymeric materials of natural and semisynthetic origin that possess the ability to interact with the mucus mucins, the mucus milieu, and/or the mucosal epithelia in their hydrated state.…”

Section: The Nasal and Oromucosal Drug Deliverymentioning

confidence: 99%

“…Although mucoadhesive polymers and viscosity enhancers are known to oppose the natural clearance mechanisms in the nasal cavity, quite often, the principles of their action contradict the provision of other desired qualities. The sustainability (mechanical strength) of a mucosally applied film, for example, increases in the presence of poor water-soluble polymers (with greater hydrophobicity or high degree of cross-linking), whereas such polymers indeed lower the mucoadhesive capacity [ 204 ]. The higher concentration of mucoadhesive polymers and the greater viscosity and yield stress of the formulation normally favor endurable retention and stability of the mucoadhesive layer but violate sprayability and spreadability [ 218 , 219 ].…”

Section: The Nasal and Oromucosal Drug Deliverymentioning

confidence: 99%

Advances in the Prophylaxis of Respiratory Infections by the Nasal and the Oromucosal Route: Relevance to the Fight with the SARS-CoV-2 Pandemic

et al. 2022

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In this time of COVID-19 pandemic, the strategies for prevention of the infection are a primary concern. Looking more globally on the subject and acknowledging the high degree of misuse of protective face masks from the population, we focused this review on alternative pharmaceutical developments eligible for self-defense against respiratory infections. In particular, the attention herein is directed to the nasal and oromucosal formulations intended to boost the local immunity, neutralize or mechanically “trap” the pathogens at the site of entry (nose or mouth). The current work presents a critical review of the contemporary methods of immune- and chemoprophylaxis and their suitability and applicability in topical mucosal dosage forms for SARS-CoV-2 prophylaxis.

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