Formulation of glycerolipidic prodrugs into PEGylated liposomes for brain delivery.

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DOIResolve DOI: http://doi.org/10.1016/S1773-2247(09)50008-1
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TypeArticle
Journal titleJournal of drug delivery science and technology
Volume19
Issue1
Pages6166; # of pages: 6
SubjectHIV; brain; blood brain barrier; PEGylated liposomes; glycerolipidic prodrugs
AbstractAlthough numerous drugs are used to treat HIV infection with increasing efficacy, the patient's brain is often infected by the virus and acts as a sanctuary where drugs cannot penetrate due to their low passage through the blood brain barrier. Therefore, the design of new medicine able to reach the brain is extemely challenging. An approach based on prodrug synthesis and encapsulation into PEGylated nanocarriers was proposed and applied to didanosine, a nucleosidic analogue used to treat HIV-1 associated dementia. In this study, appropriate formulations of PEGylated liposomes were designed to incorporate two glycerolipidic prodrugs of didanosine. Preparation methods based on Bangham's or emulsion/evaporation techniques formulations exhibited particle size under 300 nm with high incorporation of prodrugs as shown by light scattering, optical microscopy experiments and differential scanning calorimetry. Finally the uptake of fluorescently labeled PEGylated formulations by rat brain immortalized endothelial cells modeling the BBB was evidence by confocal laser scanning microscopy. All the results suggest that the encapsulation of didanosine prodrugs into PEGylated liposomes is a promising approach in the goal increasing didanosine concentration in the brain and treating HIV-1-associated dementia.
Publication date
LanguageEnglish
AffiliationNational Research Council Canada; NRC Institute for Biological Sciences
Peer reviewedNo
NRC numberBOURGEOIS2009
NPARC number9387394
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Record identifierd17b58cc-8930-46a6-b962-c38e62f5b625
Record created2009-07-10
Record modified2016-05-09
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