Drug interaction and location in liposomes: correlation with polar surface areas

El Maghraby, G.M.M., Williams, A.C. ORCID: https://orcid.org/0000-0003-3654-7916 and Barry, B.W. (2005) Drug interaction and location in liposomes: correlation with polar surface areas. International Journal of Pharmaceutics, 292 (1-2). pp. 179-185. ISSN 0378-5173 doi: 10.1016/j.ijpharm.2004.11.037

Abstract/Summary

An important step in liposome characterization is to determine the location of a drug within the liposome. This work thus investigated the interaction of dipalmitoylphosphatidylcholine liposomes with drugs of varied water solubility, polar surface area (PSA) and partition coefficient using high sensitivity differential scanning calorimetry. Lipophilic estradiol (ES) interacted strongest with the acyl chains of the lipid membrane, followed by the somewhat polar 5-fluorouracil (5-FU). Strongly hydrophilic mannitol (MAN) showed no evidence of interaction but water soluble polymers inulin (IN) and an antisense oligonucleotide (OLG), which have very high PSAs, interacted with the lipid head groups. Accordingly, the drugs could be classified as: hydrophilic ones situated in the aqueous core and which may interact with the head groups; those located at the water-bilayer interface with some degree of penetration into the lipid bilayer; those lipophilic drugs constrained within the bilayer. (c) 2004 Elsevier B.V. All rights reserved.

Item Type	Article
URI	https://reading-clone.eprints-hosting.org/id/eprint/13754
Item Type	Article
Refereed	Yes
Divisions	Life Sciences > School of Chemistry, Food and Pharmacy > School of Pharmacy
Uncontrolled Keywords	liposomes, high sensitivity differential scanning calorimetry, polar, surface areas, drug-liposome interaction., DIFFERENTIAL SCANNING CALORIMETRY, THERMOTROPIC PHASE-BEHAVIOR, MOLECULAR-INTERACTIONS, PENETRATION ENHANCERS, HOMOLOGOUS SERIES, CHAIN-LENGTH, TRANSITION, ABSORPTION, DIPALMITOYLPHOSPHATIDYLCHOLINE, PERMEABILITY
Download/View statistics	View download statistics for this item