Frontispiece: Glyceride-Mimetic Prodrugs Incorporating Self-Immolative Spacers Promote Lymphatic Transport, Avoid First-Pass Metabolism, and Enhance Oral Bioavailability
نویسندگان
چکیده
منابع مشابه
Oral bioavailability and first-pass effects.
Existing experimental strategies for the in vivo evaluation of factors affecting oral bioavailability have been reviewed. Based on concepts that have evolved, an integrated set of strategies emerges that appears capable of providing estimates of the individual contributions attributable to absorption, losses in the gut lumen, and first-pass elimination in the gut wall and the liver. The only as...
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Polycations are explored as carriers to deliver therapeutic nucleic acids. Polycations are conventionally pharmacological inert with the sole function of delivering therapeutic cargo. This study reports synthesis of a self-immolative polycation (DSS-BEN) based on a polyamine analogue drug N(1),N(11)-bisethylnorspermine (BENSpm). The polycation was designed to function dually as a gene delivery ...
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β-Lapachone has drawn increasing attention as an anti-inflammatory and anti-cancer drug. However, its oral bioavailability has not been yet assessed, which might be useful to develop efficient dosage forms possibly required for non-clinical and clinical studies and future market. The aim of the present study was thus to investigate pharmacokinetic properties of β-lapachone as well as its first-...
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Oral bioavailability of some drugs is substantially lower in cynomolgus monkeys than in various other species, including humans. In the present study, midazolam was used as a model drug to investigate the reason for the lower bioavailability in these monkeys. The bioavailability of midazolam after oral administration was minimal in monkeys and rats, being only 2.1 and 1.1%, respectively. In mon...
متن کاملComparison of alkyl ester versus triglyceride mimetic lipid prodrug strategies to target a model immunomodulator to the lymphatic system
SUMMARY The current study aims to use an oral lipophilic prodrug approach to promote the delivery of a model immunomodulator, mycophenolic acid (MPA) to the lymphatic system to facilitate enhanced uptake into lymphocytes. The project builds on recent studies demonstrating that targeted drug delivery to lymphocytes in the lymphatics may enhance immunomodulatory effects [1,2]. Two types of lipoph...
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ژورنال
عنوان ژورنال: Angewandte Chemie International Edition
سال: 2016
ISSN: 1433-7851
DOI: 10.1002/anie.201684461