dc.contributor.author | Flaten, Gøril Eide | |
dc.contributor.author | Chang, Ting-Tung | |
dc.contributor.author | Phillips, William T. | |
dc.contributor.author | Brandl, Martin | |
dc.contributor.author | Bao, Ande | |
dc.contributor.author | Goins, Beth | |
dc.date.accessioned | 2016-03-16T14:01:28Z | |
dc.date.available | 2016-03-16T14:01:28Z | |
dc.date.issued | 2012-12-05 | |
dc.description.abstract | Context: Camptothecin (CPT) represents a potent anticancer drug. Its therapeutic use however is
impaired by both drug solubility, hydrolysis and protein interactions in vivo. Use of liposomes as
drug formulation approach could overcome some of these challenges.
<p>Objective: The objective of this study was to perform a mechanistic study of the incorporation
and retention of the lipophilic parent CPT-compound in different liposome formulations using
radiolabeled CPT and thus be able to identify promising CPT delivery systems. In this context
we also wanted to establish an appropriate mouse tumor model, in vivo scintigraphic imaging
and biodistribution methodology for testing the most promising formulation.
<p>Materials and methods: CPT retention in various liposome formulations following incubation in
buffer and serum was determined. The HT-29 mouse tumor model, 111In-labeled liposomes as
well as 3H-labeled CPT were used to investigate the biodistribution of liposomes and drug.
<p>Results and discussion: The ability of different liposome formulations to retain CPT in buffer
was influenced by the lipid concentration and the drug:lipid ratio rather than lipid composition.
The tested formulations were cleared from the blood in the following order:CPT-solutionCPTliposomes
111In-labeled liposomes, and liposomes mainly accumulated in liver.
<p>Conclusion: Lipid composition did not influence CPT retention to the same extent as earlier
observed in incorporation studies. The set up for the biodistribution study works well and is
suited for future in vivo studies on CPT liposomes. The biodistribution study showed that
liposomes circulated longer than free drug, but premature release of drug from liposomes
occurred. Further studies to develop formulations with higher retention potential and prolonged
circulation are desired. | en_US |
dc.description | Accepted manuscript version. Published version available at <a href=http://dx.doi.org/10.3109/08982104.2012.742537>http://dx.doi.org/10.3109/08982104.2012.742537</a> | en_US |
dc.identifier.citation | Journal of liposome research 2013, 23(1):70-81 | en_US |
dc.identifier.cristinID | FRIDAID 1033180 | |
dc.identifier.doi | 10.3109/08982104.2012.742537 | |
dc.identifier.issn | 0898-2104 | |
dc.identifier.uri | https://hdl.handle.net/10037/8984 | |
dc.identifier.urn | URN:NBN:no-uit_munin_8539 | |
dc.language.iso | eng | en_US |
dc.publisher | Taylor & Francis | en_US |
dc.rights.accessRights | openAccess | |
dc.subject | VDP::Medisinske Fag: 700 | en_US |
dc.subject | VDP::Medical disciplines: 700 | en_US |
dc.title | Liposomal formulations of poorly soluble camptothecin: drug retention and biodistribution | en_US |
dc.type | Journal article | en_US |
dc.type | Tidsskriftartikkel | en_US |
dc.type | Peer reviewed | en_US |