Evaluation of nano- and microparticle uptake by the gastrointestinal tract.

Numerous papers over the last two decades have demonstrated that particle uptake by the gastrointestinal tract is a reality. In addition, polymeric nano- and microparticles have proved to be useful delivery systems to enhance oral bioavailability of poorly absorbed drugs or to induce mucosal immune response. However, despite the amount of data available, no set criteria are available for the design of a good particulate carrier for oral delivery of peptides or antigens. This is partly due to the publication of conflicting and confusing data. The source of discrepancy is actually multiparametric (e.g., methodology, mode of evaluation, animal species) and is still not fully understood. The purpose of this review is to discuss the advantages and the limitations of the methodologies and the models used to evaluate gastrointestinal uptake of nano- and microparticles.

[1]  M. Deleers,et al.  A new nanocapsule formulation with hydrophilic core : Application to the oral administration of salmon calcitonin in rats , 1996 .

[2]  A. R. Thomson,et al.  Uptake of Small Resin Particles (1–5µ Diameter) by the Alimentary Canal of the Calf , 1960, Nature.

[3]  J. Steinkamp,et al.  Phagocytosis: flow cytometric quantitation with fluorescent microspheres. , 1982, Science.

[4]  A. Florence,et al.  Nanoparticle Uptake by the Rat Gastrointestinal Mucosa: Quantitation and Particle Size Dependency , 1990, The Journal of pharmacy and pharmacology.

[5]  A. Pockley,et al.  A rapid microplate-based fluorometric assay for phagocytosis. , 1993, Immunological investigations.

[6]  J. Benoit,et al.  Fate of [14C]poly(DL-lactide-co-glycolide) nanoparticles after intravenous and oral administration to mice , 1994 .

[7]  P. Edman,et al.  Microspheres as a nasal delivery system for peptide drugs , 1992 .

[8]  N Hussain,et al.  Factors affecting the oral uptake and translocation of polystyrene nanoparticles: histological and analytical evidence. , 1995, Journal of drug targeting.

[9]  D. Cremaschi,et al.  Selective transport of microparticles across Peyer's patch follicle‐associated M cells from mice and rats , 1995, Experimental physiology.

[10]  C. Ashworth,et al.  A study of particulate intestinal absorption and hepatocellular uptake. Use of polystyrene latex particles. , 1961, Experimental cell research.

[11]  S. Davis,et al.  The importance of gastrointestinal uptake of particles in the design of oral delivery systems , 1995 .

[12]  M. Donowitz,et al.  Elevated intraluminal pressure alters rabbit small intestinal transport in vivo. , 1982, The American journal of physiology.

[13]  R. Simmons,et al.  Evidence for the phagocytic transport of intestinal particles in dogs and rats , 1988, Infection and immunity.

[14]  M. Aprahamian,et al.  Transmucosal passage of polyalkylcyanoacrylate nanocapsules as a new drug carrier in the small intestine , 1987, Biology of the cell.

[15]  Hugh N. Nellans,et al.  B) Mechanisms of peptide and protein absorption , 1991 .

[16]  Clive G. Wilson,et al.  A γ-scintigraphic evaluation of microparticulate ophthalmic delivery systems: liposomes and nanoparticles , 1987 .

[17]  P. Smith,et al.  Methods for evaluating intestinal permeability and metabolism in vitro. , 1996, Pharmaceutical biotechnology.

[18]  Donald E. Chickering,et al.  Biologically erodable microspheres as potential oral drug delivery systems , 1997, Nature.

[19]  Tucker Sp,et al.  Migration of polarized epithelial cells through permeable membrane substrates of defined pore size. , 1992 .

[20]  K. Ulbrich,et al.  Tumour tropism and anti-cancer efficacy of polymer-based doxorubicin prodrugs in the treatment of subcutaneous murine B16F10 melanoma. , 1994, British Journal of Cancer.

[21]  J. Pappo,et al.  Monoclonal antibody-directed targeting of fluorescent polystyrene microspheres to Peyer's patch M cells. , 1991, Immunology.

[22]  J. Steinkamp,et al.  In vitro and in vivo measurement of phagocytosis by flow cytometry. , 1986, Methods in enzymology.

[23]  H. Cottier,et al.  Uptake by enterocytes and subsequent translocation to internal organs, eg, the thymus, of Percoll microspheres administered per os to suckling mice. , 1983, Journal of the Reticuloendothelial Society.

[24]  I. Toth,et al.  Co-polymerised peptide particles (CPP) I: synthesis, characterisation and in vitro studies on a novel oral nanoparticulate delivery system , 1996 .

[25]  P. James,et al.  M cell numbers increase after transfer of SPF mice to a normal animal house environment. , 1987, The American journal of pathology.

[26]  K. Carr,et al.  Gastrointestinal uptake and translocation of microparticles in the streptozotocin-diabetic rat. , 1996, Journal of anatomy.

[27]  G W Halbert,et al.  The Uptake and Translocation of Latex Nanospheres and Microspheres after Oral Administration to Rats , 1989, The Journal of pharmacy and pharmacology.

[28]  F. Poelma,et al.  Evaluation of a chronically isolated internal loop in the rat for the study of drug absorption kinetics. , 1987, Journal of pharmaceutical sciences.

[29]  R Weltzin,et al.  Role of the glycocalyx in regulating access of microparticles to apical plasma membranes of intestinal epithelial cells: implications for microbial attachment and oral vaccine targeting , 1996, The Journal of experimental medicine.

[30]  R. Berg,et al.  BACTERIAL TRANSLOCATION ACROSS ENTEROCYTES: RESULTS OF A STUDY OF BACTERIAL‐ENTEROCYTE INTERACTIONS UTILIZING Caco‐2 CELLS , 1994, Shock.

[31]  J S Cornes,et al.  Number, size, and distribution of Peyer's patches in the human small intestine , 1965, Gut.

[32]  J. Kopeček,et al.  HPMA copolymer-anticancer drug-OV-TL16 antibody conjugates. 1. influence of the method of synthesis on the binding affinity to OVCAR-3 ovarian carcinoma cells in vitro. , 1996, Journal of drug targeting.

[33]  H. Junginger,et al.  Intestinal transit of bioadhesive microspheres in an in situ loop in the rat—A comparative study with copolymers and blends based on poly(acrylic acid) , 1990 .

[34]  V. Lenaerts,et al.  Tissue concentration of nanoencapsulated radio-labelled cyclosporin following peroral delivery in mice or ophthalmic application in rabbits , 1996 .

[35]  B. Hirst,et al.  Comparison of poly(DL-lactide-co-glycolide) and polystyrene microsphere targeting to intestinal M cells. , 1993, Journal of drug targeting.

[36]  S. Davis,et al.  The preparation and characterization ofpoly(lactide-co-glycolide) microparticles: III. Microparticle/polymer degradation rates and the in vitro release of a model protein , 1994 .

[37]  S. Davis,et al.  Microparticulate absorption from the rat intestine , 1994 .

[38]  W. Rubas,et al.  A human colonic cell line sharing similarities with enterocytes as a model to examine oral absorption: advantages and limitations of the Caco-2 model. , 1997, Critical reviews in therapeutic drug carrier systems.

[39]  N. McHale,et al.  The effect of anesthetics on lymphatic contractility. , 1989, Microvascular research.

[40]  A. Dayan,et al.  Translocation of particulates across the gut wall--a quantitative approach. , 1995, Journal of drug targeting.

[41]  J. Seifert,et al.  The influence of age and particle number on absorption of polystyrene particles from the rat gut. , 1996, Journal of anatomy.

[42]  K. Luthman,et al.  Caco-2 monolayers in experimental and theoretical predictions of drug transport , 1996 .

[43]  J. Kreuter,et al.  Distribution and elimination of polymethyl methacrylate nanoparticles after peroral administration to rats. , 1984, Journal of pharmaceutical sciences.

[44]  A T Florence,et al.  Comparative, quantitative study of lymphoid and non-lymphoid uptake of 60 nm polystyrene particles. , 1994, Journal of drug targeting.

[45]  David J Brayden,et al.  Binding and uptake of biodegradable poly-DL-lactide micro- and nanoparticles in intestinal epithelia. , 1998, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

[46]  B. Hirst,et al.  Targeting to intestinal M cells. , 1996, Journal of anatomy.

[47]  J. Benoit,et al.  Intestinal absorption of PLAGA microspheres in the rat. , 1996, Journal of anatomy.

[48]  T. Kissel,et al.  Poly(acrylic acid) microparticles widen the intercellular spaces of Caco-2 cell monolayers : An examination by confocal laser scanning microscopy , 1996 .

[49]  J. Kreuter,et al.  Improved peroral delivery of avarol with polybutylcyanoacrylate nanoparticles , 1994 .

[50]  M. E. Lefevre,et al.  Intestinal barrier to large particulates in mice. , 1980, Journal of toxicology and environmental health.

[51]  I. Wilding,et al.  The role of γ-scintigraphy in oral drug delivery , 1991 .

[52]  M. E. Lefevre,et al.  Intestinal absorption of particulate matter. , 1977, Life sciences.

[53]  J. Pawley,et al.  Handbook of Biological Confocal Microscopy , 1990, Springer US.

[54]  P. Artursson,et al.  Starch microspheres enhance insulin absorption across epithelial cells by affecting the integrity of tight junctions , 1992 .

[55]  M. E. Lefevre,et al.  Intestinal Uptake of Fluorescent Microspheres in Young and Aged Mice 1 , 1989, Proceedings of the Society for Experimental Biology and Medicine. Society for Experimental Biology and Medicine.

[56]  S. Davis,et al.  The quantitation of the absorption of microparticles into the intestinal lymph of Wistar rats , 1994 .

[57]  M. Hashida,et al.  Biliary excretion of polystyrene microspheres with covalently linked FITC fluorescence after oral and parenteral administration to male Wistar rats. , 1996, Journal of drug targeting.

[58]  J. Pappo,et al.  Uptake and translocation of fluorescent latex particles by rabbit Peyer's patch follicle epithelium: a quantitative model for M cell uptake. , 1989, Clinical and experimental immunology.

[59]  J. Seifert,et al.  Rapid insorption of small particles in the gut. , 1990, The American journal of gastroenterology.

[60]  Thomas R. Tice,et al.  Controlled vaccine release in the gut-associated lymphoid tissues. I. Orally administered biodegradable microspheres target the peyer's patches , 1990 .

[61]  D. Cremaschi,et al.  Confocal analysis of fluorescent bead uptake by mouse Peyer's patch follicle‐associated M cells , 1992, Experimental physiology.

[62]  R. Kinne,et al.  In vitro permeability of PBCA nanoparticles through porcine small intestine. , 1993, Journal of drug targeting.

[63]  D. Lewis,et al.  The transport of microspheres from the gastro‐intestinal tract to inflammatory air pouches in the rat , 1989, The Journal of pharmacy and pharmacology.

[64]  P. Couvreur,et al.  Slow Delivery of the Selective Cholecystokinin Agonist pBC 264 into the Rat Nucleus Accumbens Using Microspheres , 1996, Journal of neurochemistry.

[65]  J. Fell Targeting of drugs and delivery systems to specific sites in the gastrointestinal tract. , 1996, Journal of anatomy.

[66]  J. Labský,et al.  Fate of 14C-terpolymer (methylmethacrylate-14C, 2-hydroxyethylmethacrylate, butylacrylate) nanoparticles after peroral administration to rats. , 1989, Die Pharmazie.

[67]  J. Kraehenbuhl,et al.  Conversion by Peyer's patch lymphocytes of human enterocytes into M cells that transport bacteria. , 1997, Science.

[68]  D. Lewis,et al.  The Transfer of Polystyrene Microspheres from the Gastrointestinal Tract to the Circulation after Oral Administration in the Rat , 1995, The Journal of pharmacy and pharmacology.

[69]  P. James,et al.  Salmonella-induced M-cell formation in germ-free mouse Peyer's patch tissue. , 1991, The American journal of pathology.

[70]  J. Vanderhoff,et al.  Accumulation of Latex in Peyer's Patches and Its Subsequent Appearance in Villi and Mesenteric Lymph Nodes 1 2 , 1978, Proceedings of the Society for Experimental Biology and Medicine. Society for Experimental Biology and Medicine.