Strategies to improve oral drug bioavailability
- 10 May 2005
- journal article
- review article
- Published by Taylor & Francis Ltd in Expert Opinion on Drug Delivery
- Vol. 2 (3), 419-433
- https://doi.org/10.1517/17425247.2.3.419
Abstract
Efforts to improve oral drug bioavailability have grown in parallel with the pharmaceutical industry. As the number and chemical diversity of drugs has increased, new strategies have been required to develop orally active therapeutics. The past two decades have been characterised by an increased understanding of the causes of low bioavailability and a great deal of innovation in oral drug delivery technologies, marked by an unprecedented growth of the drug delivery industry. The advent of biotechnology and consequent proliferation of biopharmaceuticals have brought new challenges to the drug delivery field. In spite of the difficulties associated with developing oral forms of this type of therapeutics, significant progress has been made in the past few years, with some oral proteins, peptides and other macromolecules currently advancing through clinical trials. This article reviews the approaches that have been successfully applied to improve oral drug bioavailability, primarily, prodrug strategies, lead optimisation through medicinal chemistry and formulation design. Specific strategies to improve the oral bioavailability of biopharmaceuticals are also discussed.Keywords
This publication has 98 references indexed in Scilit:
- β‐Cyclodextrin Reduces Bioavailability of Orally Administered [3H]Benzo[a]pyrene in the RatJournal of Pharmaceutical Sciences, 2005
- Presystemic metabolism and intestinal absorption of antipsoriatic fumaric acid estersBiopharmaceutics & Drug Disposition, 2003
- Activity–Bioavailability balance in Oral Drug Development for a Selected Group of 6‐FluoroquinolonesJournal of Pharmaceutical Sciences, 2002
- Development of oral heparin therapy for prophylaxis and treatment of deep venous thrombosisCardiovascular Surgery, 2001
- Transport mechanisms of a glycoside, p-nitrophenyl-β-d-glucopyranoside, across rat small intestinal brush-border membranesBiochimica et Biophysica Acta (BBA) - Biomembranes, 1998
- Vitamin B12 Mediated Oral Delivery Systems for Granulocyte-Colony Stimulating Factor and ErythropoietinBioconjugate Chemistry, 1995
- Bile acid derived HMG-CoA reductase inhibitorsBiochimica et Biophysica Acta (BBA) - Molecular Basis of Disease, 1994
- 6,7,8,9-Tetrahydro-N,N-di-n-propyl-3H-benzindol-8-amines. Derivatives as Potent and Orally Active Serotonin 5-HT1A Receptor AgonistsJournal of Medicinal Chemistry, 1994
- Synthesis and Biological Activity of Bile Acid-Derived HMG-CoA Reductase Inhibitors. The Role of 21-Methyl in Recognition of HMG-CoA Reductase and the Ileal Bile Acid Transport SystemJournal of Medicinal Chemistry, 1994
- New Approaches for the Preparation of Hydrophobic Heparin DerivativesJournal of Pharmaceutical Sciences, 1994