TY - JOUR
T1 - The prospects of lipidic prodrugs
T2 - An old approach with emerging an future
AU - Dahan, Arik
AU - Markovic, Milica
AU - Aponick, Aaron
AU - Zimmermann, Ellen M.
AU - Ben-Shabat, Shimon
N1 - Funding Information:
This work was funded through the US‐Israel Binational Science Foundation (BSF) grant number 2015365. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed. No writing assistance was utilized in the production of this manuscript.
Funding Information:
This work was funded through the US Israel Binational Science Foundation (BSF) grant number 2015365. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.
Publisher Copyright:
© 2019 © 2019 Newlands Press.
PY - 2019/1/1
Y1 - 2019/1/1
N2 - Nowadays, prodrugs are no longer used as a last resort, rather, they are intentionally designed at the early stages of drug development. Lipidic prodrug strategy, where a drug moiety is covalently bound to a lipid carrier, was initially proposed half a century ago, yet, this approach still remains to be explored. Lipidic prodrugs can join physiological lipid metabolic pathways, and hence provide drug targeting via lymphatic transport or site-specific drug release, improve drugs' pharmacokinetic profile, overcome obstacles originating from biological barriers and bypass hepatic first-pass metabolism. Physiological pathways of lipid processing, uses of different lipidic prodrugs and their clinical benefits are overviewed. Overall, lipidic prodrugs present a promising approach for overcoming different obstacles and fulfilling various unmet needs in drug delivery/targeting.
AB - Nowadays, prodrugs are no longer used as a last resort, rather, they are intentionally designed at the early stages of drug development. Lipidic prodrug strategy, where a drug moiety is covalently bound to a lipid carrier, was initially proposed half a century ago, yet, this approach still remains to be explored. Lipidic prodrugs can join physiological lipid metabolic pathways, and hence provide drug targeting via lymphatic transport or site-specific drug release, improve drugs' pharmacokinetic profile, overcome obstacles originating from biological barriers and bypass hepatic first-pass metabolism. Physiological pathways of lipid processing, uses of different lipidic prodrugs and their clinical benefits are overviewed. Overall, lipidic prodrugs present a promising approach for overcoming different obstacles and fulfilling various unmet needs in drug delivery/targeting.
KW - biopharmaceutics
KW - cholesterol
KW - drug delivery
KW - fatty acid
KW - lipid
KW - lymphatic drug transport
KW - phospholipid
KW - prodrug
KW - triglyceride
UR - http://www.scopus.com/inward/record.url?scp=85073594958&partnerID=8YFLogxK
U2 - 10.4155/fmc-2019-0155
DO - 10.4155/fmc-2019-0155
M3 - Review article
AN - SCOPUS:85073594958
SN - 1756-8919
VL - 11
SP - 2563
EP - 2571
JO - Future Medicinal Chemistry
JF - Future Medicinal Chemistry
IS - 19
ER -