Document Detail


Micelles of different morphologies--advantages of worm-like filomicelles of PEO-PCL in paclitaxel delivery.
MedLine Citation:
PMID:  17564817     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
PURPOSE: Worm-like and spherical micelles are both prepared here from the same amphiphilic diblock copolymer, poly(ethylene oxide)-b-poly (epsilon-caprolactone) (PEO [5 kDa]-PCL [6.5 kDa]) in order to compare loading and delivery of hydrophobic drugs. MATERIALS AND METHODS: Worm-like micelles of this degradable copolymer are nanometers in cross-section and spontaneously assemble to stable lengths of microns, resembling filoviruses in some respects and thus suggesting the moniker 'filomicelles'. The highly flexible worm-like micelles can also be sonicated to generate kinetically stable spherical micelles composed of the same copolymer. RESULTS: The fission process exploits the finding that the PCL cores are fluid, rather than glassy or crystalline, and core-loading of the hydrophobic anticancer drug delivery, paclitaxel (TAX) shows that the worm-like micelles load and solubilize twice as much drug as spherical micelles. In cytotoxicity tests that compare to the clinically prevalent solubilizer, Cremophor EL, both micellar carriers are far less toxic, and both types of TAX-loaded micelles also show fivefold greater anticancer activity on A549 human lung cancer cells. CONCLUSION: PEO-PCL based worm-like filomicelles appear to be promising pharmaceutical nanocarriers with improved solubilization efficiency and comparable stability to spherical micelles, as well as better safety and efficacy in vitro compared to the prevalent Cremophor EL TAX formulation.
Authors:
Shenshen Cai; Kandaswamy Vijayan; Debbie Cheng; Eliana M Lima; Dennis E Discher
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural; Research Support, U.S. Gov't, Non-P.H.S.     Date:  2007-06-13
Journal Detail:
Title:  Pharmaceutical research     Volume:  24     ISSN:  0724-8741     ISO Abbreviation:  Pharm. Res.     Publication Date:  2007 Nov 
Date Detail:
Created Date:  2007-09-27     Completed Date:  2007-11-29     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  8406521     Medline TA:  Pharm Res     Country:  United States    
Other Details:
Languages:  eng     Pagination:  2099-109     Citation Subset:  IM    
Affiliation:
Department of Chemical and Biomolecular Engineering, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA.
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MeSH Terms
Descriptor/Qualifier:
Antineoplastic Agents, Phytogenic / administration & dosage*
Cell Line, Tumor
Drug Delivery Systems*
Drug Stability
Humans
Micelles*
Paclitaxel / administration & dosage*,  chemistry,  pharmacology
Polyesters / administration & dosage*
Solubility
Chemical
Reg. No./Substance:
0/Antineoplastic Agents, Phytogenic; 0/Micelles; 0/Polyesters; 0/polyethylene oxide-polycaprolactone copolymer; 33069-62-4/Paclitaxel

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


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