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Is oral lipid-based delivery for drug targeting to the brain feasible?

Brookes, Alice; Ji, Liuhang; Bradshaw, Tracey D.; Stocks, Michael; Gray, David; Butler, James; Gershkovich, Pavel

Is oral lipid-based delivery for drug targeting to the brain feasible? Thumbnail


Alice Brookes

Liuhang Ji

Tracey D. Bradshaw

Professor of Medicinal Chemistry and Drug Discovery

Professor of Applied Lipid Science

James Butler


This review outlines the feasibility of oral lipid-based targeted delivery of drugs to the brain, including permeation of the central nervous system's (CNS) protective blood–brain barrier (BBB). The structure of the BBB and disruption caused by varying disease states highlights the need for disease-specific approaches to alter permeation. Disruption during disease state, and the effects of certain molecules on the barrier, demonstrate the possibility of exploiting such BBB disruption for drug delivery. Many administration methods can be used to target the brain, but oral administration is considered ideal for chronic, long-term illnesses. Several lipids that have been shown to facilitate drug delivery into the brain after systemic administration, but could also be delivered orally, are discussed, including oleic acid, triolein, alkylglycerol, and conjugates of linoleic and myristic acids. Current data reveal the potential for the use of such lipids as part of oral formulations for delivery to the brain by reaching sufficient plasma levels after administration to increase the permeability of the BBB. However, gaps in the literature remain regarding the concentrations and form of most lipids required to produce the desired effects. The use of lipids via oral delivery for brain targeting has not been investigated thoroughly enough to determine with certainty if similar permeability-enhancing effects would be observed as for parenteral administration. In conclusion, further research to fill research gaps is needed, but the limited evidence suggests that oral lipid-based drug delivery for brain targeting is potentially feasible.

Journal Article Type Article
Acceptance Date Feb 5, 2022
Online Publication Date Feb 17, 2022
Publication Date Mar 1, 2022
Deposit Date May 19, 2022
Publicly Available Date May 19, 2022
Journal European Journal of Pharmaceutics and Biopharmaceutics
Print ISSN 0939-6411
Electronic ISSN 1873-3441
Publisher Elsevier BV
Peer Reviewed Peer Reviewed
Volume 172
Pages 112-122
Keywords Pharmaceutical Science; General Medicine; Biotechnology
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