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Review

Drug Bioavailability Enhancing Agents of Natural Origin (Bioenhancers) that Modulate Drug Membrane Permeation and Pre-Systemic Metabolism

Centre of Excellence for Pharmaceutical Sciences (Pharmacen™), North-West University, Potchefstroom 2520, South Africa
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Received: 11 December 2018 / Revised: 23 December 2018 / Accepted: 24 December 2018 / Published: 16 January 2019
(This article belongs to the Special Issue Transmucosal Absorption Enhancers in the Drug Delivery Field)
Many new chemical entities are discovered with high therapeutic potential, however, many of these compounds exhibit unfavorable pharmacokinetic properties due to poor solubility and/or poor membrane permeation characteristics. The latter is mainly due to the lipid-like barrier imposed by epithelial mucosal layers, which have to be crossed by drug molecules in order to exert a therapeutic effect. Another barrier is the pre-systemic metabolic degradation of drug molecules, mainly by cytochrome P450 enzymes located in the intestinal enterocytes and liver hepatocytes. Although the nasal, buccal and pulmonary routes of administration avoid the first-pass effect, they are still dependent on absorption of drug molecules across the mucosal surfaces to achieve systemic drug delivery. Bioenhancers (drug absorption enhancers of natural origin) have been identified that can increase the quantity of unchanged drug that appears in the systemic blood circulation by means of modulating membrane permeation and/or pre-systemic metabolism. The aim of this paper is to provide an overview of natural bioenhancers and their main mechanisms of action for the nasal, buccal, pulmonary and oral routes of drug administration. Poorly bioavailable drugs such as large, hydrophilic therapeutics are often administered by injections. Bioenhancers may potentially be used to benefit patients by making systemic delivery of these poorly bioavailable drugs possible via alternative routes of administration (i.e., oral, nasal, buccal or pulmonary routes of administration) and may also reduce dosages of small molecular drugs and thereby reduce treatment costs. View Full-Text
Keywords: bioenhancer; cytochrome P450; drug absorption enhancer; efflux; metabolism; P-glycoprotein; pharmacokinetic interaction; tight junction bioenhancer; cytochrome P450; drug absorption enhancer; efflux; metabolism; P-glycoprotein; pharmacokinetic interaction; tight junction
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MDPI and ACS Style

Peterson, B.; Weyers, M.; Steenekamp, J.H.; Steyn, J.D.; Gouws, C.; Hamman, J.H. Drug Bioavailability Enhancing Agents of Natural Origin (Bioenhancers) that Modulate Drug Membrane Permeation and Pre-Systemic Metabolism. Pharmaceutics 2019, 11, 33. https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics11010033

AMA Style

Peterson B, Weyers M, Steenekamp JH, Steyn JD, Gouws C, Hamman JH. Drug Bioavailability Enhancing Agents of Natural Origin (Bioenhancers) that Modulate Drug Membrane Permeation and Pre-Systemic Metabolism. Pharmaceutics. 2019; 11(1):33. https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics11010033

Chicago/Turabian Style

Peterson, Bianca, Morné Weyers, Jan H. Steenekamp, Johan D. Steyn, Chrisna Gouws, and Josias H. Hamman 2019. "Drug Bioavailability Enhancing Agents of Natural Origin (Bioenhancers) that Modulate Drug Membrane Permeation and Pre-Systemic Metabolism" Pharmaceutics 11, no. 1: 33. https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics11010033

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