Effects of Excipients in Oral Drug Absorption
A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Physical Pharmacy and Formulation".
Deadline for manuscript submissions: closed (31 October 2021) | Viewed by 7317
Special Issue Editors
Interests: PBPK; biowaivers; pharmacokinetics; dissolution; absorption; drug solubility
Special Issues, Collections and Topics in MDPI journals
Interests: oral absorption; intestinal permeability methods; in vitro–in vivo correlations; PK modelling
Special Issues, Collections and Topics in MDPI journals
Interests: biopharmaceutics; biowaivers; oral absorption; dissolution; PBBM
Special Issue Information
Dear Colleagues,
Excipients have been considered in the past as inactive and inert substances, but over the years numerous studies have contradicted this belief. Excipients may affect oral bioavailability of a drug product through their effects on drug release, membrane permeability, gastrointestinal (GI) physiology (motility and volumes) and drug first pass metabolism. The relevance and clinical impact of excipient effects differ according to the properties of the drug and formulation – while excipient changes for BCS Class 1 drugs are generally considered to be lower risk, additional mechanistic insight is needed to assess the potential impact of an excipient for other BCS classes. The observed effects of excipients in the oral absorption process have been characterized in the past, mainly in vitro (i.e., in dissolution studies, in vitro cell culture methods, or in situ animal studies). Nevertheless, the development and validation of all these in vitro and preclinical models is still ongoing and a clear predictive link to the clinical performance of drug products (i.e., their impact on Cmax or AUC), is still missing. Furthermore, some of the clinical BE study failures which are widely cited as examples of excipient effects lack mechanistic insight into how the excipient could perpetrate the effect observed. On the other hand, the mentioned in vitro and preclinical methods cover only partially some of the proposed mechanisms, and excipient effects in humans continue to be explored using modern techniques, e.g., exploration of effects on motility and water fluxes using human intubation studies coupled with image methodologies (as MRI) and computational fluid dynamic models. The aim of this Special Issue is to cover the latest insights in excipient effects on oral absorption from a mechanistic perspective, including the new in vitro predictive models and the computational and database approaches to get risk-based assessment tools to help in formulation selection.
Prof. Dr. Isabel Gonzalez-Alvarez
Prof. Dr. Marival Bermejo
Dr. Talia Flanagan
Guest Editors
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Keywords
- excipient effect
- oral dosage forms
- solubilization
- drug carriers
- oral bioavailability
- biowaiver risks
- gastrointestinal Image methods
- in vivo predictive dissolution IPD
- permeability enhancers
- GI motility
