NOSE-TO-BRAIN DRUG DELIVERY OF NANOFORMULATIONS: PREPARATION AND IN VITRO EVALUATION

Year 2023, Volume: 27 Issue: Current Research Topıcs In Pharmacy: Drug Delivery, 13 - 16, 28.06.2025

Işık Çelikkol Özge Eşim Canan Hasçiçek

Abstract

Central nervous system (CNS)-related diseases constitute 6.3% of all diseases globally. Because of the increased prevalence of CNS-diseases, the requirement for novel strategies for delivering therapeutics across the blood-brain barrier (BBB) has arisen [1]. The management of CNS diseases is challenging. BBB is the main obstacle preventing traditional therapeutics from reaching the CNS. Researchers have developed strategies that can deliver therapeutics to the CNS, such as (1) bypassing BBB by using other administration routes, (2) transient disrupting BBB by physical or biochemical approaches, (3) enabling penetration into BBB by administration of endogenous transporters and receptors, (4) inhibition of efflux transporters, (5) using drug carriers [2]. Nose-to-brain route has been considered a viable alternative to deliver therapeutics to the brain. Intranasal delivery to the CNS has some advantages including noninvasiveness, minimized systemic exposure, rapid transport from the nasal mucosa to the brain and prompt efficiency, elimination of the first-pass effect, lower side effects [3]. Although it has many advantages, mucociliary clearance, and limited absorption from the nasal epithelium are also disadvantages [4]. Due to the disadvantages of intranasal administration, various approaches are needed to increase drug penetration. Nanotechnology-based drug delivery systems including nanoparticles, in situ gels and liposomes have been designed to make use of the superiorities nanocarriers, such as extended retention at the nasal mucosa, nanoranged size, and ability to open the tight junctions [2, 3]. In this study, migraine, a chronic neurological disease, was chosen as a model, and dexketoprofen trometamol (DXT) loaded chitosan- and chitosan/alginate nanoparticles were developed and characterized for treatment of migraine. Chitosan has been chosen as an ideal polymer for targeting the brain via intranasal therapy due to its capacity to generate inter-/intramolecular bonding and polycationic surface as a result of its amino groups. The developed nanoparticle formulations were formulated into a chitosan-based hydrogel formulation and the mucoadhesive properties of the formulations were investigated.

Keywords

Chitosan , dexketoprofen trometamol , nanoparticle , nose-to-brain

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