Cited by 482Advanced Drug Delivery SystemsBarrier Structure and Function StudiesInhalation and Respiratory Drug Delivery

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Direct nose to brain drug delivery via integrated nerve pathways bypassing the blood–brain barrier: an excellent platform for brain targeting

Pardeshi, Chandrakantsing Vijaysing, Belgamwar, Veena Shailendra·2013·Expert Opinion on Drug Delivery

DOI 10.1517/17425247.2013.790887

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Abstract

INTRODUCTION: The blood-brain barrier (BBB) represents a stringent barrier for delivery of neurotherapeutics in vivo. An attempt to overcome this barrier is represented by the direct transport of drugs from the nose to the brain along the olfactory and trigeminal nerve pathways. These nerve pathways initiate in the nasal cavity at olfactory neuroepithelium and terminate in the brain. An enormous range of neurotherapeutics, both macromolecules and low molecular weight drugs, can be delivered to the central nervous system (CNS) via this route. AREAS COVERED: Present review highlights the literature on the anatomy-physiology of the nasal cavity, pathways and mechanisms of neurotherapeutic transport across nasal epithelium and their biofate and various strategies to enhance direct nose to brain drug delivery. The authors also emphasize a variety of drug molecules and carrier systems delivered via this route for treating CNS disorders. Patents related to direct nose to brain drug delivery systems have also been listed. EXPERT OPINION: Direct nose to brain drug delivery system is a practical, safe, non-invasive and convenient form of formulation strategy and could be viewed as an excellent alternative approach to conventional dosage forms. Existence of a direct transport route from the nasal cavity to the brain, bypassing the BBB, would offer an exciting mode of delivering neurotherapeutic agents.

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Intranasal insulin delivery and therapy1Abbreviations: α-CD, α-cyclodextrin; β-CD, β-cyclodextrin; γ-CD, γ-cyclodextrin; AUC, area under the plasma/serum concentration versus time curve; Cmax, maximum or peak plasma/serum concentration; Cmin, minimum plasma/serum concentration; DDPC, didecanoyl-L-α-phosphatidylcholine; DM-β-CD, dimethyl-β-cyclodextrin; EDTA, ethylenediaminetetraacetic acid; FITC, fluorescein isothiocyanate; HLB, hydrophile–lipophile balance; hGH, human growth hormone; HP-β-CD, hydroxy-propyl-β-cyclodextrin; HPC, hydroxypropylcellulose; HSA, human serum albumin; Hyaff 11, hyaluronic acid ester; IDDM, insulin-dependent diabetes mellitus; Ig, immunoglobulin; Laureth-9, polyoxyethylene-9-lauryl ether; LPC, lysophosphatidylcholine; LPG, lysophosphatidylglycerol; MCC, microcrystalline cellulose; MTR, mucociliary transport rate; NIDDM, non-insulin-dependent diabetes mellitus; PC, phosphatidylcholine; RAMEB, randomly methylated β-cyclodextrin; SDC, sodium deoxycholate; SGC, sodium glycocholate; STDHF, sodium taurodihydrofusidate; 99mTc, 99mtechnetium; TER, transepithelial resistance.1
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Background
Overcoming barriers to patient adherence: the case for developing innovative drug delivery systems
Baryakova, T. H., Pogostin, B. H., Langer, R., & McHugh, K. J. (2023) · Nature Reviews Drug Discovery · doi:10.1038/s41573-023-00670-0 · Cited by 566
Tailoring Formulations for Intranasal Nose-to-Brain Delivery: A Review on Architecture, Physico-Chemical Characteristics and Mucociliary Clearance of the Nasal Olfactory Mucosa
Gänger, S., & Schindowski, K. (2018) · Pharmaceutics · doi:10.3390/pharmaceutics10030116 · Cited by 447
“Another great impact for safe and efficient N2B targeting is the reproducibility of drug administration in the olfactory region [115].”
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Authors: Pardeshi, C. V., & Belgamwar, V. S.
ORCID: Pardeshi, Chandrakantsing Vijaysing
Belgamwar, Veena Shailendra
Venue: Expert Opinion on Drug Delivery
Publisher: Informa UK Limited
Published: 2013-04-16
Volume: 10
Issue: 7
Pages: 957-972
ISSN: 1742-5247 (ISSN-L)
1744-7593
DOI: 10.1517/17425247.2013.790887
OpenAlex: W2162752807
Cited by: 482
References: 92
Citations by year: 2026: 44 · 2025: 41 · 2024: 50 · 2023: 48 · 2022: 39 · 2021: 65 · 2020: 43 · 2019: 50 · 2018: 36 · 2017: 20 · 2016: 13 · 2015: 14 · 2014: 12 · 2013: 6
FWCI: 1.89
Type: journal article
Language: en
Open access: closed
Locations: Expert Opinion on Drug Delivery (publishedVersion)
PubMed (publishedVersion)
Topics: Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
Life Sciences › Neuroscience › Neurology › Barrier Structure and Function Studies
Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Inhalation and Respiratory Drug Delivery
Keywords: nose-to-brain delivery, blood-brain barrier bypass, intranasal drug delivery, olfactory epithelium, nasal epithelium, neurotherapeutics, brain drug delivery, drug carriers, patents
MeSH terms: Administration, Intranasal, Biological Transport, Blood-Brain Barrier, Brain, Pharmaceutical Preparations, Humans, Nasal Mucosa, Olfactory Pathways, Trigeminal Nerve, Drug Delivery Systems

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Direct nose to brain drug delivery via integrated nerve pathways bypassing the blood–brain barrier: an excellent platform for brain targeting

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