Lipid-based formulations for oral administration

Opportunities for bioavailability enhancement and lipoprotein targeting of lipophilic drugs

Research output: Chapter in Book/Report/Conference proceedingChapter (Book)Researchpeer-review

Abstract

The identification of increasingly complex intracellular drug targets, escalating requirements in terms of drug potency and the use of combinatorial chemistry libraries and in vitro receptor-based activity assays, has led to a trend toward the identification of increasingly lipophilic lead molecules. The clinical usefulness of highly lipophilic, poorly water-soluble drugs, however, is often limited by their low and variable oral bioavailability, and although co-administration with lipids, lipidic excipients, or fatty meals may improve the bioavailability of lipophilic drugs, the mechanistic aspects of this enhancement are incompletely understood.
Original languageEnglish
Title of host publicationDrug Targeting Technology
Subtitle of host publicationPhysical Chemical Biological Methods
EditorsHans Schreier
Place of PublicationBoca Raton FL USA
PublisherCRC Press
Chapter4
Pages85-130
Number of pages46
Volume115
ISBN (Electronic)9780203908563
ISBN (Print)9780824705800
DOIs
Publication statusPublished - 2001

Publication series

NameDrugs and the pharmaceutical sciences: A Series of Textbooks and Monographs
PublisherCRC Press
Volume115

Cite this

Porter, C. J. H., & Charman, W. N. (2001). Lipid-based formulations for oral administration: Opportunities for bioavailability enhancement and lipoprotein targeting of lipophilic drugs. In H. Schreier (Ed.), Drug Targeting Technology: Physical Chemical Biological Methods (Vol. 115, pp. 85-130). (Drugs and the pharmaceutical sciences: A Series of Textbooks and Monographs; Vol. 115). Boca Raton FL USA: CRC Press. https://doi.org/10.1081/RRS-100107429
Porter, Christopher J.H. ; Charman, William N. / Lipid-based formulations for oral administration : Opportunities for bioavailability enhancement and lipoprotein targeting of lipophilic drugs. Drug Targeting Technology: Physical Chemical Biological Methods. editor / Hans Schreier. Vol. 115 Boca Raton FL USA : CRC Press, 2001. pp. 85-130 (Drugs and the pharmaceutical sciences: A Series of Textbooks and Monographs).
@inbook{3ce423112351488e9c363ed54568f233,
title = "Lipid-based formulations for oral administration: Opportunities for bioavailability enhancement and lipoprotein targeting of lipophilic drugs",
abstract = "The identification of increasingly complex intracellular drug targets, escalating requirements in terms of drug potency and the use of combinatorial chemistry libraries and in vitro receptor-based activity assays, has led to a trend toward the identification of increasingly lipophilic lead molecules. The clinical usefulness of highly lipophilic, poorly water-soluble drugs, however, is often limited by their low and variable oral bioavailability, and although co-administration with lipids, lipidic excipients, or fatty meals may improve the bioavailability of lipophilic drugs, the mechanistic aspects of this enhancement are incompletely understood.",
author = "Porter, {Christopher J.H.} and Charman, {William N.}",
year = "2001",
doi = "10.1081/RRS-100107429",
language = "English",
isbn = "9780824705800",
volume = "115",
series = "Drugs and the pharmaceutical sciences: A Series of Textbooks and Monographs",
publisher = "CRC Press",
pages = "85--130",
editor = "Hans Schreier",
booktitle = "Drug Targeting Technology",
address = "Australia",

}

Porter, CJH & Charman, WN 2001, Lipid-based formulations for oral administration: Opportunities for bioavailability enhancement and lipoprotein targeting of lipophilic drugs. in H Schreier (ed.), Drug Targeting Technology: Physical Chemical Biological Methods. vol. 115, Drugs and the pharmaceutical sciences: A Series of Textbooks and Monographs, vol. 115, CRC Press, Boca Raton FL USA, pp. 85-130. https://doi.org/10.1081/RRS-100107429

Lipid-based formulations for oral administration : Opportunities for bioavailability enhancement and lipoprotein targeting of lipophilic drugs. / Porter, Christopher J.H.; Charman, William N.

Drug Targeting Technology: Physical Chemical Biological Methods. ed. / Hans Schreier. Vol. 115 Boca Raton FL USA : CRC Press, 2001. p. 85-130 (Drugs and the pharmaceutical sciences: A Series of Textbooks and Monographs; Vol. 115).

Research output: Chapter in Book/Report/Conference proceedingChapter (Book)Researchpeer-review

TY - CHAP

T1 - Lipid-based formulations for oral administration

T2 - Opportunities for bioavailability enhancement and lipoprotein targeting of lipophilic drugs

AU - Porter, Christopher J.H.

AU - Charman, William N.

PY - 2001

Y1 - 2001

N2 - The identification of increasingly complex intracellular drug targets, escalating requirements in terms of drug potency and the use of combinatorial chemistry libraries and in vitro receptor-based activity assays, has led to a trend toward the identification of increasingly lipophilic lead molecules. The clinical usefulness of highly lipophilic, poorly water-soluble drugs, however, is often limited by their low and variable oral bioavailability, and although co-administration with lipids, lipidic excipients, or fatty meals may improve the bioavailability of lipophilic drugs, the mechanistic aspects of this enhancement are incompletely understood.

AB - The identification of increasingly complex intracellular drug targets, escalating requirements in terms of drug potency and the use of combinatorial chemistry libraries and in vitro receptor-based activity assays, has led to a trend toward the identification of increasingly lipophilic lead molecules. The clinical usefulness of highly lipophilic, poorly water-soluble drugs, however, is often limited by their low and variable oral bioavailability, and although co-administration with lipids, lipidic excipients, or fatty meals may improve the bioavailability of lipophilic drugs, the mechanistic aspects of this enhancement are incompletely understood.

UR - http://www.scopus.com/inward/record.url?scp=85051149330&partnerID=8YFLogxK

U2 - 10.1081/RRS-100107429

DO - 10.1081/RRS-100107429

M3 - Chapter (Book)

SN - 9780824705800

VL - 115

T3 - Drugs and the pharmaceutical sciences: A Series of Textbooks and Monographs

SP - 85

EP - 130

BT - Drug Targeting Technology

A2 - Schreier, Hans

PB - CRC Press

CY - Boca Raton FL USA

ER -

Porter CJH, Charman WN. Lipid-based formulations for oral administration: Opportunities for bioavailability enhancement and lipoprotein targeting of lipophilic drugs. In Schreier H, editor, Drug Targeting Technology: Physical Chemical Biological Methods. Vol. 115. Boca Raton FL USA: CRC Press. 2001. p. 85-130. (Drugs and the pharmaceutical sciences: A Series of Textbooks and Monographs). https://doi.org/10.1081/RRS-100107429