title: Biolabile peptidyl delivery systems toward sequential drug release.
abstract: Compact carriers for peptidyl delivery systems (PDSs) loaded with various drugs were synthesized using a simple and convenient solid phase organic synthesis strategy, including semi-orthogonal functional group protection schemes. Each attachment point of the compact carrier can thus be bound to an anticancer agent through a biodegradable covalent link. Chemo- and biostability experiments of a model peptidyl platform loaded with three different drugs revealed pH and liver homogenate (metabolic) dependent sequential release behavior. The versatility of this approach will serve to expedite the preparation of PDS libraries. This approach may prove useful for applications suitable for personalized medicine where multiple drug delivery is required in a sequential and controlled fashion.
authors.affiliation: Department of Biological Chemistry, Ariel University, Ariel 40700, Israel.
authors.forename: Elena
authors.initials: E
authors.lastname: Ragozin
authors.affiliation: Department of Biological Chemistry, Ariel University, Ariel 40700, Israel.|Department of Chemistry, Bar-Ilan University, Ramat Gan 52900, Israel.
authors.forename: Boris
authors.initials: B
authors.lastname: Redko
authors.affiliation: Department of Molecular Biology, Ariel University, Ariel 40700, Israel.
authors.forename: Elena
authors.initials: E
authors.lastname: Tuchinsky
authors.affiliation: Department of Biological Chemistry, Ariel University, Ariel 40700, Israel.|Department of Chemistry, Bar-Ilan University, Ramat Gan 52900, Israel.
authors.forename: Alex
authors.initials: A
authors.lastname: Rozovsky
authors.affiliation: Department of Chemistry, Bar-Ilan University, Ramat Gan 52900, Israel.
authors.forename: Amnon
authors.initials: A
authors.lastname: Albeck
authors.affiliation: Department of Biological Chemistry, Ariel University, Ariel 40700, Israel.
authors.forename: Flavio
authors.initials: F
authors.lastname: Grynszpan
authors.affiliation: Department of Biological Chemistry, Ariel University, Ariel 40700, Israel.
authors.forename: Gary
authors.initials: G
authors.lastname: Gellerman
mesh_terms: D002460:Cell Line; D002851:Chromatography, High Pressure Liquid; D016503:Drug Delivery Systems; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D010455:Peptides / Q000008:administration & dosage*; D021241:Spectrometry, Mass, Electrospray Ionization
chemical_list: D010455:Peptides
keywords: biostability; chemostability; drug delivery; multiple drug delivery; peptidyl delivery system; prodrug; sequential drug release