Document Detail


Polymeric micelles with a pH-responsive structure as intracellular drug carriers.
MedLine Citation:
PMID:  16182401     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Polymeric micelles based on poly(L-lactide)-b-poly(2-ethyl-2-oxazoline)-b-poly(L-lactide) (PLLA-PEOz-PLLA) ABA triblock copolymers were designed as intracellular drug carriers. The PLLA-PEOz-PLLA micelles adopt a "flower-like" arrangement with A-blocks at the core and a B-block on the shell under neutral condition. The deformation of the core-shell structure is then promoted by the aggregation of PEOzs due to the formation of inter- and intra-hydrogen bonding between protonated nitrogen and carbonyl groups. The experiments on in vitro release have confirmed that the release of doxorubicin (DOX) from micelles was successfully inhibited at pH 7.4. In contrast, an accelerated release of DOX from micelles was observed at acidic conditions. The results of growth inhibition assay indicated that the cell-killing rate of DOX-loaded micelles gradually approached that of free DOX as increasing the concentration and the incubation time. The overlay of fluorescent images on CLSM observation clearly demonstrated the colocalization of DOX with acidic compartments, suggesting that the drug release was successfully triggered in the acidic organelles by means of micelle deformation.
Authors:
Chau-Hui Wang; Chun-Hung Wang; Ging-Ho Hsiue
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2005-09-22
Journal Detail:
Title:  Journal of controlled release : official journal of the Controlled Release Society     Volume:  108     ISSN:  0168-3659     ISO Abbreviation:  J Control Release     Publication Date:  2005 Nov 
Date Detail:
Created Date:  2005-10-24     Completed Date:  2006-01-24     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  8607908     Medline TA:  J Control Release     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  140-9     Citation Subset:  IM    
Affiliation:
Department of Chemical Engineering, National Tsing Hua University, Hsinchu, 300 Taiwan, ROC.
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MeSH Terms
Descriptor/Qualifier:
Antibiotics, Antineoplastic / chemistry,  pharmacology
Cell Survival / drug effects
Doxorubicin / chemistry,  pharmacology
Drug Carriers / chemistry*
Hela Cells
Humans
Hydrogen-Ion Concentration
Kinetics
Micelles
Oxazoles / chemistry
Polyesters / chemistry
Polymers / chemistry*
Solubility
Chemical
Reg. No./Substance:
0/Antibiotics, Antineoplastic; 0/Drug Carriers; 0/Micelles; 0/Oxazoles; 0/Polyesters; 0/Polymers; 23214-92-8/Doxorubicin; 25805-17-8/polyethyloxazoline; 26969-66-4/poly(lactide)

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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