PEG-b-PPS diblock copolymer aggregates for hydrophobic drug solubilization and release: cyclosporin A as an example

Details

Serval ID
serval:BIB_6C1E5550C13E
Type
Article: article from journal or magazin.
Collection
Publications
Institution
Title
PEG-b-PPS diblock copolymer aggregates for hydrophobic drug solubilization and release: cyclosporin A as an example
Journal
Molecular Pharmaceutics
Author(s)
Velluto D., Demurtas D., Hubbell J. A.
ISSN
1543-8384
Publication state
Published
Issued date
2008
Volume
5
Number
4
Pages
632-642
Language
english
Abstract
Micelles formed from amphiphilic block copolymers have been explored in recent years as carriers for hydrophobic drugs. In an aqueous environment, the hydrophobic blocks form the core of the micelle, which can host lipophilic drugs, while the hydrophilic blocks form the corona or outer shell and stabilize the interface between the hydrophobic core and the external medium. In the present work, mesophase behavior and drug encapsulation were explored in the AB block copolymeric amphiphile composed of poly(ethylene glycol) (PEG) as a hydrophile and poly(propylene sulfide) PPS as a hydrophobe, using the immunosuppressive drug cyclosporin A (CsA) as an example of a highly hydrophobic drug. Block copolymers with a degree of polymerization of 44 on the PEG and of 10, 20 and 40 on the PPS respectively (abbreviated as PEG44-b-PPS10, PEG44-b-PPS20, PEG44-b-PPS40) were synthesized and characterized. Drug-loaded polymeric micelles were obtained by the cosolvent displacement method as well as the remarkably simple method of dispersing the warm polymer melt, with drug dissolved therein, in warm water. Effective drug solubility up to 2 mg/mL in aqueous media was facilitated by the PEG- b-PPS micelles, with loading levels up to 19% w/w being achieved. Release was burst-free and sustained over periods of 9-12 days. These micelles demonstrate interesting solubilization characteristics, due to the low glass transition temperature, highly hydrophobic nature, and good solvent properties of the PPS block
Keywords
Capsules , chemistry , Cryoelectron Microscopy , Cyclosporine , Hydrophobicity , Magnetic Resonance Spectroscopy , Micelles , Microscopy,Electron,Transmission , Molecular Structure , Polyethylene Glycols , Polymers , Solubility , Solvents , Sulfides , Switzerland , Water
Pubmed
Web of science
Create date
29/01/2009 23:13
Last modification date
20/08/2019 15:26
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