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Immobilized liposom...
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Beigi, FaridehUppsala universitet,Institutionen för naturvetenskaplig biokemi
(författare)
Immobilized liposome and biomembrane partitioning chromatography of drugs for prediction of drug transport
- Artikel/kapitelEngelska1998
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LIBRIS-ID:oai:DiVA.org:uu-89998
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https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-89998URI
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https://doi.org/10.1016/S0378-5173(97)00398-0DOI
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Språk:engelska
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Sammanfattning på:engelska
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Ämneskategori:art swepub-publicationtype
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Drug partitioning into lipid bilayers was studied by chromatography on liposomes and biomembranes immobilized in gel beads by freeze–thawing. The drug retention volume was expressed as a capacity factor, Ks, normalized with respect to the amount of immobilized phospholipid. Log Ks values for positively charged drugs on brain phosphatidylserine (PS)/egg phosphatidylcholine (PC) liposomes decreased as the ionic strength was increased, increased as the PS:PC ratio or the pH was increased and varied linearly with the temperature. Log Ks values for beta-blockers, phenothiazines and benzodiazepines on egg phospholipid (EPL) liposomes correlated well with corresponding values on red cell membrane lipid liposomes (r2=0.96), and on human red cell membrane vesicles containing transmembrane proteins (r2=0.96). A fair correlation was observed between the values on EPL liposomes and those on native membranes of adsorbed red cells (r2=0.86). Compared to the data obtained with liposomes, the retentions of hydrophilic drugs became larger and the range of log Ks values more narrow on the vesicles and the membranes, which expose hydrophilic protein surfaces and oligosaccharides. Lower correlations were observed between drug retention on EPL liposomes and egg PC liposomes; and between retention on liposomes (or vesicles) and immobilized artificial membrane (IAM) monolayers of PC analogues. Absorption of orally administered drugs in humans (literature data) was nearly complete for drugs of log Ks values in the interval 1.2–2.5 on vesicles. Both vesicles and liposomes can thus be used for chromatographic analysis of drug–membrane interaction and prediction of drug absorption.
Biuppslag (personer, institutioner, konferenser, titlar ...)
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Gottschalk, IngoUppsala universitet,Institutionen för naturvetenskaplig biokemi
(författare)
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Lagerquist Hägglund, ChristineUppsala universitet,Institutionen för naturvetenskaplig biokemi
(författare)
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Haneskog, LarsUppsala universitet,Institutionen för naturvetenskaplig biokemi
(författare)
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Brekkan, EggertUppsala universitet,Institutionen för naturvetenskaplig biokemi
(författare)
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Zhang, Yanxiao
(författare)
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Österberg, Thomas
(författare)
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Lundahl, PerUppsala universitet,Institutionen för naturvetenskaplig biokemi
(författare)
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Uppsala universitetInstitutionen för naturvetenskaplig biokemi
(creator_code:org_t)
Sammanhörande titlar
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Ingår i:International Journal of Pharmaceutics164:1-2, s. 129-1370378-51731873-3476
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