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dc.contributor.authorPeterson, Bianca
dc.contributor.authorWeyers, Morné
dc.contributor.authorSteenekamp, Jan H.
dc.contributor.authorSteyn, Johan D.
dc.contributor.authorGouws, Chrisna
dc.contributor.authorHamman, Josias H.
dc.date.accessioned2019-04-02T10:46:29Z
dc.date.available2019-04-02T10:46:29Z
dc.date.issued2019
dc.identifier.citationPeterson, B. et al. 2019. Drug bioavailability enhancing agents of natural origin (bioenhancers) that modulate drug membrane permeation and pre-systemic metabolism. Pharmaceutics, 11(1): Article no 33. [https://doi.org/10.3390/pharmaceutics11010033]en_US
dc.identifier.issn1999-4923
dc.identifier.urihttp://hdl.handle.net/10394/32101
dc.identifier.urihttps://www.mdpi.com/1999-4923/11/1/33/pdf
dc.identifier.urihttps://doi.org/10.3390/pharmaceutics11010033
dc.description.abstractMany 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 costsen_US
dc.language.isoenen_US
dc.publisherMDPIen_US
dc.subjectBioenhanceren_US
dc.subjectCytochrome P450en_US
dc.subjectDrug absorption enhanceren_US
dc.subjectEfflux; metabolismen_US
dc.subjectP-glycoproteinen_US
dc.subjectPharmacokinetic interactionen_US
dc.subjectTight junctionen_US
dc.titleDrug bioavailability enhancing agents of natural origin (bioenhancers) that modulate drug membrane permeation and pre-systemic metabolismen_US
dc.typeArticleen_US
dc.contributor.researchID10081097 - Hamman, Josias Hendrik
dc.contributor.researchID12450960 - Gouws, Chrisna
dc.contributor.researchID12297305 - Steyn, Johan Dewald
dc.contributor.researchID10096078 - Steenekamp, Jan Harm
dc.contributor.researchID20265832 - Peterson, Bianca
dc.contributor.researchID21653100 - Weyers, Morné


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