Chan LMS, Lowes S, Hirst BH: The ABCs of drug transport in intestine and liver: efflux proteins limiting absorption and bioavailability. Eur J Pharm Sci 2004, 21:25–51.
PubMed
Article
CAS
Google Scholar
Walgren RA, Karnaky KJ, Lindenmayer GE, et al.: Efflux of dietary flavanoid quercetin 4’-beta-glucoside across human intestinal Caco-2 cell monolayers by apical multidrug resistance-associated protein-2a. J Pharmacol Exp Ther 2000, 294:830–836.
PubMed
CAS
Google Scholar
Watkins PB: Drug metabolism by cytochromes P450 in the liver and small bowel. Gastrointest Pharmacol 1992, 21:511–526.
CAS
Google Scholar
Thummel KE, Wilkinson GR: In vitro and in vivo drug interactions involving human CYP34A. Annu Rev Pharmacol Toxicol 1998, 38:389–430.
PubMed
Article
CAS
Google Scholar
Keppler D, Cui Y, König J, et al.: Export pumps for anionic conjugates encoded by MRP genes. Adv Enzyme Regul 1999, 39:787–791.
Google Scholar
Mouly S, Paine MR: P-glycoprotein increases from proximal to distal regions of human small intestine. Pharm Res 2003, 20:1595–1599.
PubMed
Article
CAS
Google Scholar
Adachi Y, Suzuki H, Sugiyama Y: Quantitative evaluation of the function of small intestinal P-glycoprotein: comparative studies between in situ and in vitro. Pharm Res 2003, 20:1163–1169.
PubMed
Article
CAS
Google Scholar
Li Q, Sai Y, Kato Y, et al.: Influence of drugs and nutrients on transporter gene expression levels in Caco-2 and LS180 intestinal epithelial cell lines. Pharm Res 2003, 20:1119–1124.
PubMed
Article
CAS
Google Scholar
Kim RB, Wandel C, Leake B, et al.: Interrelationship between substrates and inhibitors of human CYP3A and P-glycoprotein. Pharm Res 1999, 16:408–414.
PubMed
Article
CAS
Google Scholar
Troutman MD, Thakker DR: Efflux ratio cannot assess P-glycoprotein-mediated attenuation of absorptive transport: asymmetric effect of P-glycoprotein on absorptive and secretory transport across Caco-2 cell monolayers. Pharm Res 2003, 20:1200–1209. This paper presents data showing that Pgp-mediated efflux during absorptive and secretory transport was asymmetric for all compounds tested. The authors conclude that the use of efflux ratios can be misleading in predicting the extent to which Pgp attenuates the absorption of substrates from the intestinal lumen.
PubMed
Article
CAS
Google Scholar
Chiu Y-Y, Hagahi K, Neudeck BL, et al.: Human jejunal permeability of cyclosporin A: influence of surfactants on P-glycoprotein efflux in Caco-2 cells. Pharm Res 2003, 20:749–756.
PubMed
Article
CAS
Google Scholar
Esfand R, Tomalia DA: Poly(amidoamine)(PAMAM) dendrimers: from biomimicry to drug delivery and biomedical applications. Drug Discov Today 2001, 6:427–436.
PubMed
Article
CAS
Google Scholar
El-Sayed M, Rhodes CA, Ginski M, et al.: Transport mechanism(s) of poly(amidoamine) dendrimers across Caco-2 cell monolayers. Int J Pharm 2003, 265:151–157.
PubMed
Article
CAS
Google Scholar
D’Emanuele A, Jevprasesphant R, Penny J, et al.: The use of dendrimer-propranolol prodrug to bypass efflux transporters and enhance oral bioavailability. J Control Release 2004, 95:447–453.
PubMed
Article
CAS
Google Scholar
Deferme S, Tack J, Lammert F, et al.: P-glycoprotein attenuating effect of human intestinal fluid. Pharm Res 2003, 20:900–903. This paper is important because it presents data on the impact of human intestinal fluid on Pgp-mediated efflux under in vitro conditions using the Caco-2 monolayer test system. Results from this commonly used cell line suggest that use of traditional buffer salts only may overestimate the transporting effects of Pgp compared with effects in vivo.
PubMed
Article
CAS
Google Scholar
Steffansen B, Nielsen CU, Brodin B, et al.: Intestinal solute carriers: an overview of trends and strategies for improving oral drug absorption. Eur J Pharmaceut Sci 2004, 21:3–16.
Article
CAS
Google Scholar
Herrera-Ruiz D, Wang Q, Cook TS, et al.: Spatial expression patterns of peptide transporters in human and rat gastro intestinal tract, Caco-2 in vitro cell culture model, and multiple human tissues. AAPS Pharm Sci 2001, 3:(article 9), http://www.aapspharmsci.org.
Okamura M, Terada T, Katsura T, et al.: Inhibitory effect of zinc on PEPT1-mediated transport of glycylsarcosine and b-lactam antibiotics in human intestinal cell line Caco-2. Pharm Res 2003, 20:1389–1393.
PubMed
Article
CAS
Google Scholar
Thomsen AE, Friedrichsen GM, Sørensen AH, et al.: Prodrugs of purine and pyrimidine analogues for the intestinal di/tripeptide transporter PepT1: affinity for hPepT1 in Caco-2 cells, drug release in aqueous media and in vitro metabolism. J Control Release 2003, 86:279–292. This paper presents data on several key measurements of a prodrugbased delivery system designed to enhance the oral bioavailability of the drugs such as acyclovir. One of the prodrugs tested showed high affinity for the intestinal transporter PEPT1 and characteristics desired (stability in the upper intestine and as the prodrug is transported through the epithelium and the ability to regenerate the parent drug in blood).
PubMed
Article
CAS
Google Scholar
Amidon GL, Lennernäs H, Shah VP, et al.: A theoretical basis for a biopharmaceutical drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res 1995, 12:413–420.
PubMed
Article
CAS
Google Scholar
Rinaki E, Valsami G, Macheras P: Quantitative biopharmaceutics classification system: the central role of dose/solubility ratio. Pharm Res 2003, 20:1917–1925.
PubMed
Article
CAS
Google Scholar
Yazdanian M, Briggs K, Jankovsky C, et al.: The ‘high solubility’ definition of the current FDA guidance on biopharmaceutical classification system may be too strict for acidic drugs. Pharm Res 2004, 21:293–299.
PubMed
Article
CAS
Google Scholar
Hilgers AR, Smith DP, Biermacher JJ, et al.: Predicting oral absorption of drugs: a case study with a novel class of antimicrobial agents. Pharm Res 2003, 20:1149–1155.
PubMed
Article
CAS
Google Scholar
Turner JV, Maddalena DJ, Agotonovic-Kustrin S: Bioavailability prediction based on molecular structure for a diverse series of drugs. Pharm Res 2004, 21:68–82. This report presents a predictive model using neural networks and theoretical descriptors. The model worked well when compared with data from the literature representing 137 compounds.
PubMed
Article
CAS
Google Scholar
Willmann S, Schmitt Q, Keldenich J, et al.: A physiologic model for simulating gastrointestinal flow and drug absorption in rats. Pharm Res 2003, 20:1766–1771.
PubMed
Article
CAS
Google Scholar
Sahoo SK, Labhasetwar V: Nanotech approaches to drug delivery and imaging. Drug Discov Today 2003, 8:1112–1120.
PubMed
Article
CAS
Google Scholar
Tao SL, Desai TA: Microfabricated drug delivery systems: from particles to pores. Adv Drug Del Rev 2003, 55:315–328.
Article
CAS
Google Scholar
Wilding IR, Prior DV: Remote controlled capsules in human drug absorption (HAD) studies. Crit Rev Ther Drug Carrier Syst 2003, 20:405–431.
Article
CAS
Google Scholar
Orive G, Hern’andez RM, Gasc’on AR, et al.: Drug delivery in biotechnology: present and future. Curr Opin Biotech 2003, 14:659–664.
PubMed
Article
CAS
Google Scholar
Arb’os P, Campanero MA, Arangoa MA, et al.: Nanoparticles with specific bioadhesive properties to circumvent the presystemic degradation of fluorinated pyrimidines. J Control Release 2004, 96:55–65.
Article
CAS
Google Scholar
Pandey R, Zahoor A, Sharma S, et al.: Nanoparticle encapsulated antitubercular drugs as a potential oral drug delivery system against murine tuberculosis. Tuberculosis 2003, 83:373–378.
PubMed
Article
Google Scholar
García-Fuentes M, Torres D, Alonso MJ: Design of lipid nanoparticles for the oral delivery of hydrophilic macromolecules. Colloids Surf B Biointerfaces 2002, 27:159–168.
Article
Google Scholar
Gabor F, Stangel M, Wirth M: Lectin-mediated bioadhesion: binding characteristics of plant lectins on the enterocyte-like cell lines Caco-2, HT-29, and HCT-8. J Control Release 1998, 55:131–142.
PubMed
Article
CAS
Google Scholar
Lambkin I, Pinilla C, Hamashin C, et al.: Toward targeted oral vaccine delivery systems: Selection of lectin mimetics from combinatorial libraries. Pharm Res 2003, 20:1258–1266.
PubMed
Article
CAS
Google Scholar
Irrache JM, Durrer D, Duchene D, et al.: Bioadhesion of lectinlatex conjugates to rat intestinal mucosa. Pharm Res 1996, 13:1716–1719.
Article
Google Scholar
Tao SL, Lubeley MW, Desai TA: Bioadhesive poly(methyl methacrylate) microdevices for controlled drug delivery. J Control Release 2003, 88:215–228. This paper describes the process by which MF particles are prepared using traditional micromachining processes, the chemistry of binding lectins to one side of the particles, and their binding characteristics to Caco-2 monolayers.
PubMed
Article
CAS
Google Scholar
Ahmed A, Bonner C, Desai TA: Bioadhesive microdevices with multiple reservoirs: a new platform for oral drug delivery. J Control Release 2002, 81:291–306.
PubMed
Article
CAS
Google Scholar
Heller R, Gilbert R, Jaroszeski MJ: Clinical applications of electrochemotherapy. Adv Drug Deliv Rev 1999, 35:119–129.
PubMed
Article
CAS
Google Scholar
Gharty-Tagoi EB, Morgan JS, Ahmed K, et al.: Electroporationmediated delivery of molecules to model intestinal epithelia. Int J Pharm 2004, 270:127–138.
Article
Google Scholar
Cor’a LA, Am’erico MF, Oliveira B, et al.: Disintegration of magnetic tablets in human stomach evaluated by alternate current biosusceptometry. Eur J Pharm Biopharm 2003, 56:413–420.
Article
CAS
Google Scholar