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The Impact of Lipos...
The Impact of Liposomal Formulations on the Release and Brain Delivery of Methotrexate : An In Vivo Microdialysis Study
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- Hu, Yang (författare)
- Uppsala universitet,Institutionen för farmaceutisk biovetenskap,Science for Life Laboratory, SciLifeLab,Translationell PKPD
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- Rip, Jaap (författare)
- Eyesiu Med BV, JH Oortweg 19, NL-2333 Leiden, Netherlands.
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- Gaillard, Pieter J. (författare)
- Eyesiu Med BV, JH Oortweg 19, NL-2333 Leiden, Netherlands.;2 BBB Med BV, JH Oortweg 19, NL-2333 Leiden, Netherlands.
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- de lange, Elizabeth C. M. (författare)
- Leiden Univ, Leiden Acad Ctr Drug Res, Div Pharmacol, Cluster Syst Pharmacol, Leiden, Netherlands.
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- Hammarlund-Udenaes, Margareta (författare)
- Uppsala universitet,Institutionen för farmaceutisk biovetenskap,Science for Life Laboratory, SciLifeLab,Translationell PKPD
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(creator_code:org_t)
- Elsevier BV, 2017
- 2017
- Engelska.
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Ingår i: Journal of Pharmaceutical Sciences. - : Elsevier BV. - 0022-3549 .- 1520-6017. ; 106:9, s. 2606-2613
- Relaterad länk:
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http://jpharmsci.org...
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Ämnesord
Stäng
- 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.
Ämnesord
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Farmaceutiska vetenskaper (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Pharmaceutical Sciences (hsv//eng)
Nyckelord
- liposome
- nanocarrier
- blood-brain barrier
- brain delivery
- in vivo release
- microdialysis
- methotrexate
Publikations- och innehållstyp
- ref (ämneskategori)
- art (ämneskategori)
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