Tier 4 — mechanistic

Comparative pharmacokinetics and safety assessment of transdermal berberine and dihydroberberine

Buchanan B, Meng Q, Poulin MM, Zuccolo J, Azike CG, Gabriele J, Baranowski DC
PloS one 2018 13:e0194979

Bibliography

PubMed
PMID 29579096
PubMed Central
PMC5868852
DOI
10.1371/journal.pone.0194979
Funding
Partially supported by Innovation PEI, the Atlantic Canada Opportunities Agency and the National Research Council of Canada; Delivra provided author salary support.
Competing interests
Authors were or had been Delivra employees; the company had a pending patent on topical berberine and dihydroberberine formulations.

Study snapshot

DesignPreclinical acute and repeated-dose pharmacokinetic study
ModelSprague-Dawley rats
Sample19 male rats in the acute study; 40 male rats in the repeated-dose study; no human participants
InterventionProprietary transdermal berberine or dihydroberberine formulations versus oral berberine
DurationAcute sampling and 14-day exposure
EndpointsSerum berberine exposure and pharmacokinetic timing; Berberine metabolite concentrations; Repeated-dose exposure and selected tolerability measures

What the study showed, in plain terms

After a single dose in rats, topical berberine and especially topical dihydroberberine increased measured berberine exposure relative to oral berberine. At day 14, the dihydroberberine formulation retained higher circulating exposure, while topical berberine performed less well. These were proprietary formulations, not human consumer-patch trials.

Key findings

After a single dose in rats, topical berberine and especially topical dihydroberberine increased measured berberine exposure relative to oral berberine. At day 14, the dihydroberberine formulation retained higher circulating exposure, while topical berberine performed less well. These were proprietary formulations, not human consumer-patch trials.

What this study can and cannot tell us

Animal pharmacokinetics does not validate consumer adhesive patches, human delivered dose, weight loss or long-term safety. Authors were employees of a company with a pending formulation patent.

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