In vitro kinetic of drug release and pulmonary retention of microencapsulated antibiotic in liposomal formulations in relation to the lipid composition

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DOIResolve DOI: http://doi.org/10.3109/02652049709051137
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TypeArticle
Journal titleJournal of Microencapsulation
Volume14
Issue3
Pages335348; # of pages: 14
SubjectPulmonary; drug release; liposome; antibiotic; microencapsulated
AbstractIn previous in-vivo studies, we demonstrated that liposomal entrapment of tobramycin resulted in an increased availability of the antibiotic in the lungs without increasing bactericidal efficacy (Omri et al. 1994). With the aim of developing liposomal formulations allowing more efficient liposome-bacteria interactions, we studied the influence of lipid composition on both drug release and pulmonary retention of encapsulated tobramycin. The phase transition temperatures of nine liposome-tobramycin formulations consisting of two synthetic phospholipids (distearoyl phosphatidylcholine (DPSC) or dipalmitoyl phosphatidylcholine (DPPC) with dimyristoyl phosphatidyl-glycerol (DMPG) or dimyristoyl phosphatidylcholine (DMPC)) were determined by differential scanning calorimetry. Liposomes, varying in terms of membrane fluidity and charge were submitted to in-vitro and in-vivo kinetic studies while retention and release of tobramycin were measured by high-performance liquid chromato-graphy (HPLC). Five less fluid liposome formulations showed absence or very low tobramycin release in in-vitro tests and long term pulmonary retention of tobramycin. Four fluid liposome formulations showed in in vitro tests modulated tobramycin release while pulmonary retention of tobramycin was dependent of the presence of charged phospholipids. Administration of charged fluid liposomes in mice showed a low level of tobramycin in the kidneys; non-charged fluid liposomes exhibited a relatively high level of tobramycin retention in the kidneys.
Publication date
LanguageEnglish
AffiliationNRC Biotechnology Research Institute; National Research Council Canada
Peer reviewedNo
NRC number34566
NPARC number3539885
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Record identifierb3edd3d1-3261-4316-b68d-71a235abe8c6
Record created2009-03-01
Record modified2016-05-09
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