Synergistic mechanisms of constituents in herbal extracts during intestinal absorption: Focus on natural occurring nanoparticles

Zhao Q. · Pharmaceutics · 2020 · 149 citations

Why are purified herbal medicines often surprisingly less effective than the messy whole extracts? Nature's secret might just lie in microscopic, naturally occurring nanoparticles.

The traditional strategy of systematically isolating active ingredients in herbal medicine has hit a curious roadblock: purer extracts often show significantly weaker pharmacological effects. Why? Because purification strips away their natural intestinal absorption power. When taken orally, various coexisting plant metabolites—both primary and secondary—team up to help active compounds cross the intestinal barrier.

These clever coexisting constituents boost performance through multiple tactics. They improve solubility, block first-pass breakdown by enzymes and transporters, enhance cell membrane permeability, and gently open the tight junctions between intestinal cells.

Even more fascinating, some of these companions actively transform the physical form of bioactive compounds by creating natural nanoparticles. This comprehensive review highlights that herbal extracts are not just single compounds, but sophisticated mixtures of active ingredients and built-in pharmacokinetic synergists, paving the way for fresh strategies in herbal drug development.

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