Journal
AAPS PHARMSCITECH
Volume 22, Issue 4, Pages -Publisher
SPRINGER
DOI: 10.1208/s12249-021-01999-8
Keywords
borneol; natural permeation enhancer; BBB; mucosal delivery; transdermal delivery
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Borneol is a natural compound that has been used in Traditional Chinese Medicine for over 1000 years. It has been studied extensively as a permeation enhancer across various physiological barriers, including the blood-brain barrier, mucosal barriers, and transdermal barriers, due to its ability to alter membrane properties and modulate transport proteins.
Incorporation of permeation enhancers is one of the most widely employed approaches for delivering drugs across biological membranes. Permeation enhancers aid in delivering drugs across various physiological barriers such as brain capillary endothelium, stratum corneum, corneal epithelium, and mucosal membranes that pose resistance to the entry of a majority of drugs. Borneol is a natural, plant-derived, lipophilic, volatile, bicyclic monoterpenoid belonging to the class of camphene. It has been used under the names Bing Pian or Long Nao in Traditional Chinese Medicine for more than 1000 years. Borneol has been incorporated predominantly as an adjuvant in the traditional Chinese formulations of centrally acting drugs to improve drug delivery to the brain. This background knowledge and anecdotal evidence have led to extensive research in establishing borneol as a permeation enhancer across the blood-brain barrier. Alteration in cell membrane lipid structures and modulation of multiple ATP binding cassette transporters as well as tight junction proteins are the major contributing factors to blood-brain barrier opening functions of borneol. Owing to these mechanisms of altering membrane properties, borneol has also shown promising potential to improve drug delivery across other physiological barriers as well. The current review focuses on the role of borneol as a permeation enhancer across the blood-brain barrier, mucosal barriers including nasal and gastrointestinal linings, transdermal, transcorneal, and blood optic nerve barrier.
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