High doses of intravenous protamine cause generalized vascular permeability changes in brain and other organs, and concomitant hypoproteinemia. The present investigations test the hypothesis that protamine has a dual action of both binding serum proteins and of undergoing absorptive-mediated transcytosis through microvascular endothelial barriers. Binding of albumin to protamine was demonstrated using equilibrium dialysis, and protamine was shown to selectively augment the uptake of albumin, but not sucrose, in isolated bovine or human brain capillaries. In contrast, the anionic macromolecule, dextran sulfate, resulted in an increased capillary uptake of both albumin and sucrose in vitro. The selective effects of protamine on albumin transport were also documented in vivo using an external organ technique; the intravenous injection of 1.5 mg/kg protamine resulted in a marked and selective influx of albumin into brain, heart, kidney, lung, and liver, and the increased albumin transport exceeded the increased sucrose uptake in some organs by an order of magnitude. The transcytosis of protamine through the cerebral microvascular barrier was documented with an internal carotid artery perfusion technique. In summary, these studies provide evidence for protamine-mediated vectorial transport of albumin through microvascular barriers in brain and other organs.
W M Pardridge, J L Buciak, Y S Kang, R J Boado
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A Historical Review of Brain Drug Delivery
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Nanoparticle designs for delivery of nucleic acid therapeutics as brain cancer therapies
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Advanced Drug Delivery Reviews | 2021 |
Biotherapeutic effect of cell-penetrating peptides against microbial agents: a review
IZ Sadiq, A Muhammad, SB Mada, B Ibrahim, UA Umar |
Tissue Barriers | 2021 |
Biotherapeutic effect of cell-penetrating peptides against microbial agents: a review.
Sadiq IZ, Muhammad A, Mada SB, Ibrahim B, Umar UA |
Tissue Barriers | 2021 |
Nanoparticle designs for delivery of nucleic acid therapeutics as brain cancer therapies.
Karlsson J, Luly KM, Tzeng SY, Green JJ |
Advanced Drug Delivery Reviews | 2021 |
Brain Delivery of Nanomedicines: Trojan Horse Liposomes for Plasmid DNA Gene Therapy of the Brain
Pardridge WM |
2020 | |
Brain Delivery of Nanomedicines: Trojan Horse Liposomes for Plasmid DNA Gene Therapy of the Brain
WM Pardridge |
2020 | |
Engineered nanoparticles for systemic siRNA delivery to malignant brain tumours
J Karlsson, Y Rui, KL Kozielski, AL Placone, O Choi, SY Tzeng, J Kim, JJ Keyes, MI Bogorad, K Gabrielson, H Guerrero-Cazares, A Quiñones-Hinojosa, PC Searson, JJ Green |
Nanoscale | 2019 |
Polymeric siRNA gene delivery – transfection efficiency versus cytotoxicity
A Kargaard, JP Sluijter, B Klumperman |
Journal of Controlled Release | 2019 |
Elimination of substances from the brain parenchyma: efflux via perivascular pathways and via the blood–brain barrier
SB Hladky, MA Barrand |
Fluids and barriers of the CNS | 2018 |
Multi-targeting peptides for gene carriers with high transfection efficiency
J Zhao, Q Li, X Hao, X Ren, J Guo, Y Feng, C Shi |
Journal of Materials Chemistry B | 2017 |
Cationic and amphipathic cell-penetrating peptides (CPPs): Their structures and in vivo studies in drug delivery
JL Zaro, WC Shen |
Frontiers of Chemical Science and Engineering | 2015 |
Handbook of Biologically Active Peptides
DM Pollock |
Handbook of Biologically Active Peptides | 2013 |
Effective Intravenous Therapy for Neurodegenerative Disease With a Therapeutic Enzyme and a Peptide That Mediates Delivery to the Brain
Y Meng, I Sohar, DE Sleat, JR Richardson, KR Reuhl, RB Jenkins, G Sarkar, P Lobel |
Molecular Therapy | 2013 |
Drug delivery strategies for the treatment of malignant gliomas
D Allhenn, MA Boushehri, A Lamprecht |
International Journal of Pharmaceutics | 2012 |
CNS delivery via adsorptive transcytosis
F Hervé, N Ghinea, JM Scherrmann |
The AAPS Journal | 2008 |
Permeation of Growth Hormone across the Blood-Brain Barrier
W Pan, Y Yu, CM Cain, F Nyberg, PO Couraud, AJ Kastin |
Endocrinology | 2005 |
Mechanisms involved in the blood–brain barrier increased permeability induced by Phoneutria nigriventer spider venom in rats
LP le Sueur, CB Collares-Buzato, MA da Cruz-Höfling |
Brain Research | 2004 |
Peptide Transport and Delivery into the Central Nervous System
L Prokai, K Prokai-Tatrai |
2003 | |
Role of Hypolipidemic Drug Clofibrate in Altering Iron Regulatory Proteins IRP1 and IRP2 Activities and Hepatic Iron Metabolism in Rats Fed a Low-Iron Diet
HL Huang, NS Shaw |
Toxicology and Applied Pharmacology | 2002 |
ISOLATION AND MOLECULAR CHARACTERIZATION OF BRAIN MICROVASCULAR ENDOTHELIAL CELLS FROM HUMAN BRAIN TUMORS
RE Unger, JB Oltrogge, HV Briesen, B Engelhardt, U Woelki, W Schlote, R Lorenz, H Bratzke, CJ Kirkpatrick |
In Vitro Cellular & Developmental Biology - Animal | 2002 |
ISOLATION AND MOLECULAR CHARACTERIZATION OF BRAIN MICROVASCULAR ENDOTHELIAL CELLS FROM HUMAN BRAIN TUMORS
RE Unger, JB Oltrogge, HV Briesen, B Engelhardt, U Woelki, W Schlote, R Lorenz, H Bratzke, CJ Kirkpatrick |
In vitro cellular & developmental biology. Animal | 2002 |
Pharmacokinetics and Delivery of Tat and Tat-Protein Conjugates to Tissues in Vivo
HJ Lee, WM Pardridge |
Bioconjugate Chemistry | 2001 |
Interactions of ?-Amyloids with the Blood?Brain Barrier
WA Banks, AJ Kastin, LM Maness, MF Banks, M Shayo, RO McLAY |
Annals of the New York Academy of Sciences | 1997 |
Vascular permeability in the peripheral autonomic and somatic nervous systems: Controversial aspects and comparisons with the blood-brain barrier
JA Kiernan |
Microscopy Research and Technique | 1996 |
Antibody delivery through the blood-brain barrier
U Bickel |
Advanced Drug Delivery Reviews | 1995 |
Vector-mediated peptide drug delivery to the brain
WM Pardridge |
Advanced Drug Delivery Reviews | 1995 |
Fine-structural investigation of rat brain microvascular endothelial cells: Tight junctions and vesicular structures in freshly isolated and cultured preparations
NJ Lane, PA Revest, S Whytock, NJ Abbott |
Journal of Neurocytology | 1995 |
In vitro cytotoxicity of macromolecules in different cell culture systems
S Choksakulnimitr, S Masuda, H Tokuda, Y Takakura, M Hashida |
Journal of Controlled Release | 1995 |
Immunocytochemical studies of protamine-induced blood-brain barrier opening to endogenous albumin
AW Vorbrodt, DH Dobrogowska, M Ueno, AS Lossinsky |
Acta Neuropathologica | 1995 |
New approaches to drug delivery through the blood-brain barrier
WM Pardridge |
Trends in Biotechnology | 1994 |
Transport of human recombinant brain-derived neurotrophic factor (BDNF) through the rat blood-brain barrier in vivo using vector-mediated peptide drug delivery
W M Pardridge, Y S Kang, J L Buciak |
Pharmaceutical Research | 1994 |