NDLI: Pharmacokinetics of lipid-drug conjugates loaded into liposomes

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Pharmacokinetics of lipid-drug conjugates loaded into liposomes

Content Provider	Scilit
Author	Signorell, Rea D. Luciani, Paola Brambilla, Davide Leroux, Jean-Christophe
Copyright Year	2018
Description	Journal: European Journal of Pharmaceutics and Biopharmaceutics Drugs that are neither lipophilic nor suitable for encapsulation via remote loading procedures are generally characterized by low entrapment efficiencies and poor retention in liposomes. One approach to circumvent this problem consists in covalently linking a lipid to the drug molecule in order to permit its insertion into the vesicle membrane. The nature of the conjugated lipid and linker, as well as the composition of the liposomal bilayer were found to have a profound impact on the pharmacokinetic properties and biodistribution of the encapsulated drugs as well as on their biological activity. This contribution reviews the past and recent developments on liposomal lipid-drug conjugates, and discusses important issues related to their stability and in vivo performance. It also provides an overview of the data that were generated during the clinical assessment of these formulations. The marketing authorization of the immunomodulating compound mifamurtide in several countries as well as the promising results obtained with the lipid prodrug of mitomycin C suggest that carefully designed liposomal formulations of lipid-drug conjugates is a valid strategy to improve a drug’s pharmacokinetic profile and with that its therapeutic index and/or efficacy.
Related Links	https://www.research-collection.ethz.ch/bitstream/20.500.11850/268595/2/Signorell_etal_Review_2018.pdf
Ending Page	199
Page Count	12
Starting Page	188
ISSN	09396411
DOI	10.1016/j.ejpb.2018.04.003
Journal	European Journal of Pharmaceutics and Biopharmaceutics
Volume Number	128
Language	English
Publisher	Elsevier BV
Publisher Date	2018-07-01
Access Restriction	Open
Subject Keyword	Journal: European Journal of Pharmaceutics and Biopharmaceutics Pharmacology and Pharmacy Lipid-drug Conjugates
Content Type	Text
Resource Type	Article
Subject	Medicine Biotechnology Pharmaceutical Science

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