Borneol
Also known as: endo-(1R)-1,7,7-trimethyl-bicyclo[2.2.1]heptan-2-ol, endo-(1S)-1,7,7-trimethyl-bicyclo[2.2.1]heptan-2-ol, camphene derivative, natural monoterpenoid, Borneol
Overview
Borneol is a natural bicyclic monoterpenoid found in the essential oils of various plants, including *Dipterocarpus aromatica*, *Cinnamomum camphora*, and *Blumea balsamifera*. It is also available as synthetic racemic mixtures. This lipophilic and volatile compound is primarily recognized for its pharmacological effects, notably neuroprotection in ischemic stroke, analgesic properties, and its significant ability to facilitate drug delivery across the blood-brain barrier (BBB). Its unique characteristic lies in its capacity to modulate BBB permeability, which makes it a valuable agent for enhancing the delivery of central nervous system (CNS) drugs. While preclinical evidence for its neuroprotective and BBB-modulating effects is robust, human clinical trials, particularly for systemic applications, are still limited, with emerging data supporting its topical analgesic use.
Benefits
Borneol offers several evidence-based benefits, primarily in neuroprotection, enhanced CNS drug delivery, and analgesia. A meta-analysis of animal studies demonstrated that borneol significantly improves cerebral blood flow and reduces nerve injury in ischemic stroke models, indicating strong neuroprotective potential. For CNS drug delivery, a systematic review and meta-analysis of 58 preclinical studies (1137 animals) found that borneol significantly increased CNS drug concentrations in 45 out of 47 studies by increasing BBB permeability, suggesting its utility in improving the efficacy of brain-targeted therapies. In terms of analgesia, a randomized, double-blind, placebo-controlled clinical trial (n=122) showed that topical borneol significantly reduced pain compared to placebo. While most data are from animal models, the clinical trial for analgesia provides promising human evidence. Borneol may also contribute to vasodilation and neurotransmitter modulation, further supporting its neuroprotective and analgesic effects. Preclinical effect sizes are significant, and clinical analgesia effects were statistically significant, though larger human trials are needed for confirmation.
How it works
Borneol exerts its effects primarily by modulating the blood-brain barrier (BBB) permeability. It achieves this by inhibiting efflux transporters, such as P-glycoprotein, and loosening tight junction proteins, which are critical components of the BBB. This action allows for increased penetration of drugs into the central nervous system (CNS). Additionally, borneol is believed to increase vasodilatory neurotransmitters and inhibit ion channel active transport, contributing to improved cerebral blood flow. In the context of analgesia, it interacts with pain pathways, though the exact molecular targets are still under investigation. Its lipophilic nature facilitates its absorption and ability to cross biological membranes, including the BBB, where it is subsequently metabolized to camphor.
Side effects
The overall safety profile of borneol appears favorable, particularly at studied doses, with preclinical studies indicating reversible changes in the blood-brain barrier (BBB) without increasing peripheral drug toxicity. However, comprehensive human safety data are limited. In a randomized controlled clinical trial for topical analgesia, borneol was well-tolerated, with no major adverse events reported. Common side effects (>5%) are not well-characterized due to limited clinical data, and uncommon (1-5%) or rare (<1%) side effects are not reported in available literature. A significant consideration is its potential to alter the pharmacokinetics of other central nervous system (CNS) drugs by modulating BBB permeability; therefore, caution is advised when co-administering borneol with CNS-active medications. Contraindications are not yet established, but caution is warranted in individuals with pre-existing compromised BBB or CNS disorders until more data become available. Safety data for special populations, such as pregnant women, children, and the elderly, are currently lacking, necessitating further research.
Dosage
Standardized dosage guidelines for borneol are not yet established, as most research has been conducted in animal models, which utilize varied doses. For topical analgesia, a clinical trial used a specific formulation, but exact dosage details are not widely specified. Optimal dosage ranges and maximum safe doses for systemic use in humans remain undefined and require dedicated clinical dose-finding studies. The timing of administration is crucial, especially when borneol is used to enhance CNS drug delivery, as its effects on BBB permeability appear to be rapid. For co-administered drugs, timing relative to borneol administration is critical to maximize CNS penetration. Topical formulations have shown efficacy for pain relief, while oral or other routes have been explored in preclinical CNS studies. Its lipophilicity aids absorption, and the purity and specific isomer form of borneol can influence its bioavailability and pharmacokinetic profile. No specific cofactors are identified as necessary for its efficacy.
FAQs
Is borneol safe for human use?
Preliminary clinical data suggest topical borneol is safe and well-tolerated. However, more extensive research is needed to fully establish its systemic safety profile for human use.
Can borneol enhance drug delivery to the brain?
Yes, preclinical studies show borneol significantly increases blood-brain barrier permeability, leading to enhanced concentrations of drugs in the central nervous system.
How quickly does borneol act?
Effects on the blood-brain barrier and analgesic properties have been observed to occur relatively rapidly, within hours, in both animal and clinical studies.
Is borneol effective for stroke?
Preclinical evidence supports borneol's neuroprotective effects in ischemic stroke models, but its clinical efficacy in human stroke patients has not yet been established.
Are there risks of increased toxicity due to BBB modulation?
Preclinical studies indicate that borneol induces reversible blood-brain barrier changes without increasing peripheral toxicity, but human data on this aspect are limited.
Research Sources
- https://pmc.ncbi.nlm.nih.gov/articles/PMC6225363/ – This systematic review and meta-analysis of 58 preclinical studies (1137 animals) investigated borneol's effect on CNS drug delivery. It found that borneol significantly improved CNS drug concentrations and BBB permeability by inhibiting efflux proteins and modulating tight junctions. The study concluded that borneol has a favorable safety profile with reversible BBB changes, though it noted the heterogeneity of preclinical study designs.
- https://www.frontiersin.org/journals/pharmacology/articles/10.3389/fphar.2021.606682/full – This meta-analysis of animal experiments explored borneol's intervention in ischemic stroke. It demonstrated statistically significant neuroprotective effects, including improved cerebral blood flow and reduced nerve injury. The analysis used robust statistical methods, but acknowledged that the findings from animal models may not directly translate to humans.
- https://www.embopress.org/doi/10.15252/emmm.201607300 – This randomized, double-blind, placebo-controlled clinical trial (n=122) evaluated topical borneol for analgesia. The study found that topical borneol significantly reduced pain compared to placebo, indicating its potential as an analgesic. While well-designed, the study was limited to topical application and a single indication, suggesting the need for larger trials to confirm broader efficacy and safety.
Supplements Containing Borneol
Resinall E Tabs
Health Concerns
Resinall K
Health Concerns
Dreamy + Collagen Boost Ginger Honey Tea
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Even + Collagen Boost Lime Mint
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Well +Collagen Boost
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Even +Collagen Boost
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Well Dreamy +Collagen Boost
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Dreamy + Collagen Boost Ginger Honey Tea
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Even + Collagen Boost Lime Mint
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Well + Collagen Boost Meyer Lemon Tea
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HANBOLI Nasal Stick
HANBOLI