Modulation of drug efflux by aloe materials: an in vitro investigation across rat intestinal tissue
Abstract
Background: Clinically, significant herb-drug interactions have been previously documented and
can be pharmacodynamic and/or pharmacokinetic in nature. Pharmacokinetic interactions have
been attributed to induction or inhibition of either metabolic enzymes or efflux transporters.
Objective: The effect of gel and whole leaf materials from 3 different aloe species namely Aloe
ferox, Aloe marlothii, and Aloe vera as well as polysaccharides precipitated from the A. vera
materials on the bi-directional transport of cimetidine across rat intestinal tissue was investigated.
Materials and Methods: Cimetidine transport studies were performed across excised rat intestinal
tissue mounted in Sweetana-Grass diffusion chambers in both the apical-to-basolateral and
basolateral-to-apical directions. Results: While A. vera gel and whole leaf materials did not inhibit
the efflux of cimetidine, the polysaccharides precipitated from them did show a reduction of
cimetidine efflux. On the other hand, both A. ferox and A. marlothii gel and whole leaf materials
exhibited an inhibition effect on cimetidine efflux. Conclusions: This study identified a modulation
effect of efflux transporters by certain aloe materials. This may cause herb-drug pharmacokinetic
interactions when drugs that are substrates for these efflux transporters are taken simultaneously
with aloe materials. On the other hand, these aloe materials may be used for drug absorption
enhancement for drugs with low bioavailability due to extensive efflux.
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- Faculty of Health Sciences [2385]