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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Comparison of the sedative effects of medetomidine administered intranasally, by atomization or drops, and intramuscular injection in dogs
Jafarbeglou, M., & Marjani, M. (2019) · Veterinary Anaesthesia and Analgesia · doi:10.1016/j.vaa.2019.05.003 · Cited by 13
Nose-to-brain drug delivery: Regulatory aspects, clinical trials, patents, and future perspectives
Pandey, A. P., Nikam, A. N., Basavraj, S., Mutalik, S. P., Gopalan, D., Kulkarni, S., Padya, B. S., Fernandes, G. J., & Mutalik, S. (2021) · Elsevier eBooks · doi:10.1016/b978-0-12-822522-6.00023-0 · Cited by 13
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“Two distinct pathways for molecules to pass through the olfactory receptor neurons: transcellular, and paracellular (Pardeshi and Belgamwar 2013) are given in Table 4 The transcellular pathway involves the passive diffusion of lipophilic drugs across sustentacular cells, fluid-phase endocytosis, or…”
Evolution of Alzheimer’s Disease Therapeutics: From Conventional Drugs to Medicinal Plants, Immunotherapy, Microbiotherapy and Nanotherapy
Ortiz-Islas, E., Montes, P., Rodríguez-Pérez, C. E., Ruiz-Sánchez, E., Sánchez-Barbosa, T., Pichardo-Rojas, D., Zavala‐Tecuapetla, C., Carvajal, K., & Campos‐Peña, V. (2025) · Pharmaceutics · doi:10.3390/pharmaceutics17010128 · Cited by 14
Intranasal Delivery of Paclitaxel-Loaded Ligand Conjugated Polymeric Nanoparticles for Targeted Brain Delivery
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Particles Containing Cells as a Strategy to Promote Remyelination in Patients With Multiple Sclerosis
Matías‐Guiu, J., Matías‐Guiu, J. A., Montero‐Escribano, P., Barcia, J. A., Canales-Aguirre, A. A., Mateos‐Díaz, J. C., & Gómez‐Pinedo, U. (2020) · Frontiers in Neurology · doi:10.3389/fneur.2020.00638 · Cited by 12
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RETRACTED: Transferrin-Conjugated Chitosan Nanoparticles for Direct Nose-to-Brain Delivery of Ziprasidone: Pharmacokinetic and Pharmacodynamic Evaluation
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Retracted
Nanocarrier Mediated Intranasal Drug Delivery Systems for the Management of Parkinsonism: A Review
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“…on frequent administration of the drug, presence of tight junctions, low permeability of molecules larger than 1000 dalton, and enzymatic degradation of proteins or peptide molecules (Costantino et al. 2007; Jadhav et al. 2007; Wu et al. 2008; Bahadur and Pathak 2012; Pardeshi and Belgamwar 2013).”
Background
Development of nanostructured environmentally responsive system containing hydroxypropyl methylcellulose for nose-to-brain administration of meloxicam
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Sachan, N., Bahadur, S., & Sharma, P. K. (2019) · Drug Delivery Letters · doi:10.2174/2210303109666190508083142 · Cited by 12
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BackgroundInfluential
Recent advances in the development of asenapine formulations
Suresh, A., Narayan, R., & Nayak, U. (2020) · Expert Opinion on Drug Delivery · doi:10.1080/17425247.2020.1792439 · Cited by 11
Role of peroxisome proliferator‐activated receptors in stroke prevention and therapy—The best is yet to come?
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“Pioglitazone injected intracerebroventricularly to mice decreased IL-6 expression at 24 hr after MCAO, which was accompanied by reduced infarction volume and improved neurological sequelae (Patzer et al., 2008).”
Background
Natural Glycan Derived Biomaterials for Inflammation Targeted Drug Delivery
Niu, Y., Xue, Q., & Fu, Y. S. (2021) · Macromolecular Bioscience · doi:10.1002/mabi.202100162 · Cited by 11
Quantitative and qualitative analysis of direct nose-to-brain drug delivery
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Self-citation
An Ex vivo Investigation on Drug Permeability of Sheep Nasal Epithelial Tissue Membranes from the Respiratory and Olfactory Regions
Haasbroek‐Pheiffer, A., Viljoen, A. M., Steenekamp, J. H., Chen, W., & Hamman, J. H. (2022) · Current Drug Delivery · doi:10.2174/1567201820666221214105836 · Cited by 10
Revolutionizing Parkinson’s treatment: Harnessing the potential of intranasal nanoemulsions for targeted therapy
Sharma, G., Wadhwa, K., Kumar, S., Singh, G., & Pahwa, R. (2025) · Drug Delivery and Translational Research · doi:10.1007/s13346-024-01770-z · Cited by 11
Sedation Characteristics of Intranasal Alfaxalone in Adult Yucatan Swine
Hampton, C. E., Takawira, C., Ross, J., & Liu, C. (2021) · Journal of the American Association for Laboratory Animal Science · doi:10.30802/aalas-jaalas-20-000099 · Cited by 10
Functionalized Nanoparticles in Drug Delivery: Strategies to Enhance Direct Nose-to-Brain Drug Delivery via Integrated Nerve Pathways
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FORMULATION AND OPTIMIZATION OF RITONAVIR NASAL NANOSUSPENSION FOR BRAIN TARGETING
Mulam, T. R., Kshirsagar, S. J., & Kakad, S. P. (2021) · INDIAN DRUGS · doi:10.53879/id.58.04.11888 · Cited by 10
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Background
Technological Strategies Applied to Pharmaceutical Systems for Intranasal Administration of Drugs Intended for Neurological Treatments: A Review
Botan, M. V. G., da Silva, J. B., & Bruschi, M. L. (2024) · AAPS PharmSciTech · doi:10.1208/s12249-024-02974-9 · Cited by 9
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Influential
Self-Assembled systems for Nose-to-Brain delivery of Temozolamide (TMZ) in brain tumor therapy
Bhagat, N., Nalawala, Z., Patel, J., Das, D., Baldha, R., Sarolia, J., & Rathod, S. (2025) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2025.125540 · Cited by 9
Paclitaxel-Ang-2-functionalized bionic mesoporous selenium nanoparticles for targeted therapy of glioma
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“It is reported that drugs absorbed by nasal mucosa can be easily transported to the brain, 32 and intranasal route is the alternative route to parenteral administration.”
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Self-citation
Niosomes-Based Drug Delivery in Targeting the Brain Tumors Via Nasal Delivery
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“Generally, agents with a molecular weight up to 1000 Da without absorption enhancer appears to have good bioavailability [29].”
BackgroundInfluential

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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