Stabilized sulforaphane for clinical use: Phytochemical delivery efficiency.
Level 4 - case-series / case-control
Uncontrolled human pharmacokinetic and tolerability pilot combined with preclinical animal and in vitro assays
PubMed 27935214 · doi:10.1002/mnfr.201600766
What was done
Researchers evaluated the stability, bioavailability, and bioactivity of two stabilized sulforaphane (SF) preparations—an α-cyclodextrin inclusion complex (SF-αCD) and a commercial SF-rich supplement. Testing included in vitro cytoprotective phase 2 response assays in cultured cells, in vivo topical cytoprotective enzyme induction in SKH1 mice, and an oral pharmacokinetic and tolerability pilot in 10 human volunteers.
What was found
In cultured cells, both stabilized formulations demonstrated potency comparable to pure SF for inducing cytoprotective responses while offering greater stability. In the human pilot (n = 10), oral SF-αCD reached peak serum concentrations (AUC peak) at 2 hours, though 6 of 10 participants reported mild stomach upset. In mice, topical application of SF-αCD failed to upregulate skin cytoprotective enzymes, whereas pure SF succeeded. The abstract provided no specific numerical concentrations, bioavailability percentages, or statistical values.
Why it matters
Stabilization of sulforaphane with cyclodextrin facilitates oral delivery and cellular bioactivity without degradation, but gastrointestinal intolerance in humans and lack of topical efficacy in mice highlight formulation-specific delivery limitations.
Limits
The human evaluation was an uncontrolled, single-arm pharmacokinetic pilot with a very small sample size (n = 10) and provided no exact numerical pharmacokinetic parameters or confidence intervals in the abstract. Topical delivery was ineffective in the animal model, and a high proportion of human participants (60%) experienced gastrointestinal discomfort.
Cited by
- supports A synthetic stabilized form of sulforaphane developed by a UK company produced adverse side effects in laboratory experiments.