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Papers of the Week

Papers: 2 Apr 2022 - 8 Apr 2022


2022 Apr 01

Curr Drug Deliv

Exploring nose to brain nano delivery for effective management of migraine.


Tanna V, Sawarkar SP, Ravikumar P
Curr Drug Deliv. 2022 Apr 01.
PMID: 35366772.


Migraine is a disabling disease, characterized by severe throbbing headache. Patients demand quick relief from this pain. The presence of blood brain barrier does not permit the drug to penetrate the brain effectively. Administration of conventional anti-migraine medications via oral route leads to erratic absorption of drugs. Delayed gastric emptying is also responsible for ineffective absorption of drug. Migraine induced nausea and vomiting, further limits patient compliance to oral medication. Other limitations associated with oral route include extensive first pass metabolism, slow onset of action, inability to cross blood brain barrier and requirement of large amount of dose/dosage and frequent administration. The anti-migraine drugs used in migraine like triptans are therapeutically effective but have low bioavaialability on oral administration. Also, these drugs are associated with several cardiovascular complications. The oral dose of most antimigraine drugs oral tritpans, Ergot amine, NSAIDs and CGRP antagonist is quite high because of their poor bioavailability. As a result of these drugs are associated with several side effects. This aspects necessitates the need of developing a dosage form that can deliver drug directly brain thereby reducing the dose. Use of invasive techniques to deliver these therapeutics to the brain do exist, however, they are painful, require expert assistance and are not cost-effective approach for migraine treatment. These limitations demand development of a novel non-invasive approach that is safe, efficacious and has high patient compliance. As, reported it is possible to target the brain tissue by administering the drug intranasally using olfactory and the trigeminal pathway. This route is non-invasive, avoids first-pass metabolism, eliminates nausea and vomiting, helps reduce dose, and thus helps achieve increase patient compliance. Some factors like solubility, lipophilicity of the drug, mucociliary clearance, enzymatic degradation hinder the bioavailability of the drug by nasal route. Therefore, there is a grave need to develop novel nasal formulations with prolonged nasal residence time, which can modulate pharmacokinetics for adequate therapeutic response, and render efficient yet robust brain targeting. It is necessary to consider these challenges in developing efficient intranasal dosage form. This review gives a brief overview of all the novel carriers reported for improving the treatment of migraine. Nanocarrier based delivery systems like in-situ gels, micro emulsion, nanoemulsion, nanoparticles, vesicular systems, micelles, and microspheres used in nose to brain delivery of migraine therapeutics are also discussed in the article.