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Influence of drug-to-lipid ratio on drug release properties and liposome integrity in liposomal doxorubicin formulations
Uppsala University, Disciplinary Domain of Science and Technology, Chemistry, Department of Physical and Analytical Chemistry, Physical Chemistry.
Uppsala University, Disciplinary Domain of Science and Technology, Chemistry, Department of Physical and Analytical Chemistry, Physical Chemistry.
2008 (English)In: Journal of liposome research, ISSN 0898-2104, E-ISSN 1532-2394, Vol. 18, no 2, 145-157 p.Article in journal (Refereed) Published
Abstract [en]

Recent studies have shown that the release properties of vincristine encapsulated in large unilamellar vesicles (LUV) can be regulated by varying the drug-to-lipid (D/L) ratio. In this work it is shown that the drug-to-lipid ratio technique for regulating drug release also applies to doxorubicin encapsulated in LUV. In particular it is shown that the half-times (T1/2) for doxorubicin release from distearoylphosphatidylcholine (DSPC)/cholesterol LUV in vitro can be increased more than six-fold by increasing the D/L ratio from 0.05 (wt/wt) to 0.39 (wt/wt). This behavior is consistent with the behavior expected for drugs that ppt. following accumulation into liposomes. It is shown that the release properties of ciprofloxacin-a drug that does not ppt. following accumulation into LUV-are not affected by the D/L ratio. It is also shown that the cryst. intravesicular doxorubicin ppts. obsd. as the D/L ratio is raised from 0.05 to 0.46 adopt increasingly unusual morphologies. Linear crystals are obsd. at lower D/L values, however triangular and rectangular variations are obsd. as the D/L ratio is increased, and induce considerable distortion in vesicle morphol. It is noted that trapping efficiency following uptake of external doxorubicin into LUV is reduced from nearly 100% at a D/L ratio of 0.05 (wt/wt) to less than 70% at an (initial) D/L ratio of 0.8 (wt/wt). It is suggested that this arises, at least in part, from membrane-disrupting effects of internal drug crystals as they increase in size.

Place, publisher, year, edition, pages
2008. Vol. 18, no 2, 145-157 p.
Keyword [en]
liposomes, drug precipitation, liposoml doxorubicin, drug loading
National Category
Chemical Sciences
Identifiers
URN: urn:nbn:se:uu:diva-17541DOI: 10.1080/08982100802129372ISI: 000257020500004PubMedID: 18569449OAI: oai:DiVA.org:uu-17541DiVA: diva2:45312
Available from: 2008-07-03 Created: 2008-07-03 Last updated: 2017-12-08Bibliographically approved

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Edwards, KatarinaKarlsson, Göran

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