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- Greenwood, John, et al.
(författare)
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Current research into brain barriers and the delivery of therapeutics for neurological diseases : a report on CNS barrier congress London, UK, 2017
- 2017
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Ingår i: Fluids and Barriers of the CNS. - : Springer Science and Business Media LLC. - 2045-8118. ; 14
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Forskningsöversikt (refereegranskat)abstract
- This is a report on the CNS barrier congress held in London, UK, March 22-23rd 2017 and sponsored by Kisaco Research Ltd. The two 1-day sessions were chaired by John Greenwood and Margareta Hammarlund-Udenaes, respectively, and each session ended with a discussion led by the chair. Speakers consisted of invited academic researchers studying the brain barriers in relation to neurological diseases and industry researchers studying new methods to deliver therapeutics to treat neurological diseases. We include here brief reports from the speakers.
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| 2. |
- Hu, Yang, et al.
(författare)
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The Impact of Liposomal Formulations on the Release and Brain Delivery of Methotrexate : An In Vivo Microdialysis Study
- 2017
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Ingår i: Journal of Pharmaceutical Sciences. - : Elsevier BV. - 0022-3549 .- 1520-6017. ; 106:9, s. 2606-2613
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Tidskriftsartikel (refereegranskat)abstract
- The impact of liposomal formulations on the in vivo release and brain delivery of methotrexate (MTX) was quantitatively assessed in rats. Two PEGylated liposomal MTX formulations based on hydrogenated soy phosphatidylcholine (HSPC) or egg-yolk phosphatidylcholine (EYPC) were prepared. The drug release and uptake into the brain after intravenous administration of both formulations were compared with unformulated MTX by determining the released, unbound MTX in brain and plasma using microdialysis. Total MTX concentrations in plasma were determined using regular blood sampling. The administration of both high-and low-dose EYPC liposomes resulted in 10 times higher extent of MTX release in plasma compared to that obtained from HSPC liposomes (p < 0.05). MTX itself possessed limited brain uptake with steady-state unbound brain-to-plasma concentration ratio (K-p,K-uu) of 0.10 +/- 0.06. Encapsulation in HSPC liposomes did not affect MTX brain uptake (K-p,K-uu 0.11 +/- 0.05). In contrast, EYPC liposomes significantly improved MTX brain delivery with a 3-fold increase of Kp, uu (0.28 +/- 0.14 and 0.32 +/- 0.13 for high-and low-dose EYPC liposomal MTX, respectively, p < 0.05). These results provide unique quantitative evidence that liposomal formulations based on different phospholipids can result in very different brain delivery of MTX.
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