Role of herbal bioactives as a potential bioavailability enhancer for Active Pharmaceutical Ingredients

Fitoterapia. 2014 Sep;97:1-14. doi: 10.1016/j.fitote.2014.05.005. Epub 2014 May 23.


The current review emphasizes on the herbal bioenhancers which themselves do not possess inherent pharmacological activity of their own but when co-administered with Active Pharmaceutical Ingredients (API), enhances their bioavailability and efficacy. Herbal bioenhancers play a crucial role in enhancing the bioavailability and bioefficacy of different classes of drugs, such as antihypertensives, anticancer, antiviral, antitubercular and antifungal drugs at low doses. This paper highlights various natural compounds that can be utilized as an efficient bioenhancer. Several herbal compounds including piperine, quercetin, genistein, naringin, sinomenine, curcumin, and glycyrrhizin have demonstrated capability to improve the pharmacokinetic parameters of several potent API. This article also focuses on various United States patents on herbal bioenhancers, which has proved to be beneficial in improving oral absorption of nutraceuticals like vitamins, minerals, amino acids and certain herbal compounds. The present paper also describes proposed mechanism of action, which mainly includes absorption process, drug metabolism, and action on drug target. The herbal bioenhancers are easily available, safe, free from side effects, minimizes drug toxicity, shortens the duration of treatment, lowers the drug resistance problems and minimizes the cost of treatment. Inspite of the fact that herbal bioenhancers provide an innovative concept for enhancing the bioavailability of several potent drugs, there are numerous bioenhancers of herbal origin that are yet to be explored in several vital areas. These bioenhancers must also be implied to enhance the bioavailability and bioefficacy through routes other than the oral route of drug delivery. There is a vast array of unexploited plants which can be investigated for their drug bioenhancing potency. The toxicity profiles of these herbal bioenhancers must not be overlooked. Researches must be carried out to solve these issues and to deliver a safe and effective dose of drugs to attain desired pharmacological response.

Keywords: Active Pharmaceutical Ingredient; Bioavailability; Bioefficacy; Bioenhancer; Pharmacokinetic parameters.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Adjuvants, Pharmaceutic / pharmacology
  • Adjuvants, Pharmaceutic / therapeutic use*
  • Alkaloids / pharmacology
  • Alkaloids / therapeutic use
  • Benzodioxoles / pharmacology
  • Benzodioxoles / therapeutic use
  • Biological Availability
  • Carum
  • Cuminum
  • Curcumin / pharmacology
  • Curcumin / therapeutic use
  • Ergolines / pharmacology
  • Ergolines / therapeutic use
  • Flavanones / pharmacology
  • Flavanones / therapeutic use
  • Genistein / pharmacology
  • Genistein / therapeutic use
  • Ginger
  • Glycyrrhizic Acid / pharmacology
  • Glycyrrhizic Acid / therapeutic use
  • Humans
  • Morphinans / pharmacology
  • Morphinans / therapeutic use
  • Piperidines / pharmacology
  • Piperidines / therapeutic use
  • Plant Extracts / pharmacology
  • Plant Extracts / therapeutic use*
  • Polyunsaturated Alkamides / pharmacology
  • Polyunsaturated Alkamides / therapeutic use
  • Quercetin / pharmacology
  • Quercetin / therapeutic use


  • Adjuvants, Pharmaceutic
  • Alkaloids
  • Benzodioxoles
  • Ergolines
  • Flavanones
  • Morphinans
  • Piperidines
  • Plant Extracts
  • Polyunsaturated Alkamides
  • sinomenine
  • Glycyrrhizic Acid
  • Quercetin
  • Genistein
  • Curcumin
  • naringin
  • lysergol
  • piperine