scholarly journals Bis-azaaromatic quaternary ammonium salts as ligands for the blood–brain barrier choline transporter

2010 ◽  
Vol 20 (11) ◽  
pp. 3208-3210 ◽  
Author(s):  
Guangrong Zheng ◽  
Zhenfa Zhang ◽  
Paul R. Lockman ◽  
Werner J. Geldenhuys ◽  
David D. Allen ◽  
...  
Keyword(s):  
Blood Brain Barrier ◽  
Quaternary Ammonium ◽  
Quaternary Ammonium Salts ◽  
Ammonium Salts ◽  
Brain Barrier ◽  
Choline Transporter ◽  
Blood Brain

3D-QSAR study of bis-azaaromatic quaternary ammonium analogs at the blood–brain barrier choline transporter

2005 ◽  
Vol 13 (13) ◽  
pp. 4253-4261 ◽  
Author(s):  
Werner J. Geldenhuys ◽  
Paul R. Lockman ◽  
Tiffany H. Nguyen ◽  
Cornelis J. Van der Schyf ◽  
Peter A. Crooks ◽  
...  
Keyword(s):  
Blood Brain Barrier ◽  
Quaternary Ammonium ◽  
3D Qsar ◽  
Brain Barrier ◽  
Qsar Study ◽  
Choline Transporter ◽  
Blood Brain

Gemini quaternary ammonium-incorporated biodegradable multiblock polyurethane micelles for brain drug delivery

RSC Advances ◽  
2015 ◽  
Vol 5 (8) ◽  
pp. 6160-6171 ◽  
Author(s):  
Rui-Chao Liang ◽  
Fang Fang ◽  
Yan-Chao Wang ◽  
Ni-Jia Song ◽  
Jie-Hua Li ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Blood Brain Barrier ◽  
Quaternary Ammonium ◽  
Drug Accumulation ◽  
Brain Barrier ◽  
Brain Drug Delivery ◽  
Blood Brain

Gemini quaternary ammonium (GQA) incorporated biodegradable multiblock polyurethane (BMPUs) micelles could transport drug across blood–brain barrier and improve brain drug accumulation.

Inhibition of choline uptake byN-cyclohexylcholine, a high affinity ligand for the choline transporter at the blood–brain barrier

2005 ◽  
Vol 13 (4) ◽  
pp. 259-266 ◽  
Author(s):  
Werner J. Geldenhuys ◽  
Paul R. Lockman ◽  
Ashok E. Philip ◽  
James H. Mcafee ◽  
Bryan L. Miller ◽  
...  
Keyword(s):  
Blood Brain Barrier ◽  
Brain Barrier ◽  
Choline Uptake ◽  
Choline Transporter ◽  
High Affinity ◽  
Affinity Ligand ◽  
Blood Brain ◽  
High Affinity Ligand

scholarly journals Predictive screening model for potential vector-mediated transport of cationic substrates at the blood–brain barrier choline transporter

2010 ◽  
Vol 20 (3) ◽  
pp. 870-877 ◽  
Author(s):  
Werner J. Geldenhuys ◽  
Vamshi K. Manda ◽  
Rajendar K. Mittapalli ◽  
Cornelis J. Van der Schyf ◽  
Peter A. Crooks ◽  
...  
Keyword(s):  
Blood Brain Barrier ◽  
Brain Barrier ◽  
Potential Vector ◽  
Choline Transporter ◽  
Screening Model ◽  
Blood Brain

scholarly journals Nanoparticles Based on Quaternary Ammonium Chitosan-methyl-β-cyclodextrin Conjugate for the Neuropeptide Dalargin Delivery to the Central Nervous System: An In Vitro Study

Pharmaceutics ◽  
2020 ◽  
Vol 13 (1) ◽  
pp. 5
Author(s):  
Chiara Migone ◽  
Letizia Mattii ◽  
Martina Giannasi ◽  
Stefania Moscato ◽  
Andrea Cesari ◽  
...  
Keyword(s):  
Blood Brain Barrier ◽  
Quaternary Ammonium ◽  
Oral Absorption ◽  
In Vitro Study ◽  
Brain Barrier ◽  
Mucosal Barrier ◽  
Blood Brain ◽  
The Brain

Peptide oral administration is a hard goal to reach, especially if the brain is the target site. The purpose of the present study was to set up a vehicle apt to promote oral absorption of the neuropeptide dalargin (DAL), allowing it to cross the intestinal mucosal barrier, resist enzymatic degradation, and transport drugs to the brain after crossing the blood–brain barrier. Therefore, a chitosan quaternary ammonium derivative was synthesized and conjugated with methyl-β-cyclodextrin to prepare DAL-medicated nanoparticles (DAL-NP). DAL-NP particle size was 227.7 nm, zeta potential +8.60 mV, encapsulation efficiency 89%. DAL-NP protected DAL from degradation by chymotrypsin or pancreatin and tripled DAL degradation time compared to non-encapsulated DAL. Use of DAL-NP was safe for either Caco-2 or bEnd.3 cells, with the latter selected as a blood–brain barrier model. DAL-NP could also cross either the Caco-2 or bEnd.3 monolayer by the transepithelial route. The results suggest a potential DAL-NP ability to transport to the brain a DAL dose fraction administered orally, although in vivo experiments will be needed to confirm the present data obtained in vitro.

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