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A smart flower-like polymeric micelle for pH-triggered anticancer drug release.

Authors
 Kyung Taek Oh  ;  Young Taik Oh  ;  Nam-Muk Oh  ;  Kwangmyung Kim  ;  Don Haeng Lee  ;  Eun Seong Lee 
Citation
 INTERNATIONAL JOURNAL OF PHARMACEUTICS, Vol.375(1-2) : 163-169, 2009 
Journal Title
 INTERNATIONAL JOURNAL OF PHARMACEUTICS 
ISSN
 0378-5173 
Issue Date
2009
MeSH
Antibiotics, Antineoplastic/administration & dosage* ; Antibiotics, Antineoplastic/chemistry ; Doxorubicin/administration & dosage* ; Doxorubicin/chemistry ; Drug Delivery Systems ; Hydrogen-Ion Concentration ; Hydrophobic and Hydrophilic Interactions ; Lactic Acid/chemistry ; Micelles ; Neoplasms/drug therapy ; Neoplasms/pathology ; Particle Size ; Polyesters ; Polyethylene Glycols/chemistry ; Polymers/chemistry*
Keywords
pH-sensitive flower-like micelle ; 3-Diethylamino propyl isothiocyanato-l-lysine ; pH-dependent drug release ; Tumor targeting
Abstract
Novel pH-responsive flower-like micelles were developed to provide the mechanism for pH-triggered drug release from drug carriers. The micelles (particle size: approximately 165 nm; critical micelle concentration (CMC): approximately 4 microg/ml), constructed from poly(N(epsilon)-(3-diethylamino)propyl isothiocyanato-L-lysine)-b-poly(ethylene glycol)-b-poly(L-lactide) [poly(DEAP-Lys)-b-PEG-b-PLLA], were designed to have a self-assembled flower-like arrangement consisting of two hydrophobic blocks [deprotonated poly(DEAP-Lys) block and PLLA block] and a petal-like hydrophilic PEG block at physiological pH. As the pH decreases to slightly acidic pH (<pH 7.0), as in tumor extracellular pH (pH(e)), the flower-like micelles undergo a change in the hydrophobicity of the micellar core. The protonation of poly(DEAP-Lys) changed the physical property of the polymer from hydrophobic to hydrophilic, resulting in disintegration of the micellar core. The co-presence of a pH-insensitive PLLA block in the micellar core affected the protonation of poly(DEAP-Lys), allowing the micelle to be stable at pH 7.0-7.4. In this study using doxorubicin (DOX) as the model drug, DOX release from the micelles accelerated in response to tumor pH(e).
Full Text
http://www.sciencedirect.com/science/article/pii/S0378517309001926
DOI
10.1016/j.ijpharm.2009.04.005
Appears in Collections:
1. College of Medicine (의과대학) > Dept. of Radiology (영상의학교실) > 1. Journal Papers
Yonsei Authors
Oh, Young Taik(오영택) ORCID logo https://orcid.org/0000-0002-4438-8890
URI
https://ir.ymlib.yonsei.ac.kr/handle/22282913/104091
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