Document Detail


PLGA and PHBV microsphere formulations and solid-state characterization: possible implications for local delivery of fusidic acid for the treatment and prevention of orthopaedic infections.
MedLine Citation:
PMID:  19384471     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
PURPOSE: To develop and characterize the solid-state properties of poly(DL-lactic-co-glycolic acid) (PLGA) and poly(3-hydroxybutyric acid-co-3-hydroxyvaleric acid) (PHBV) microspheres for the localized and controlled release of fusidic acid (FA).
METHODS: The effects of FA loading and polymer composition on the mean diameter, encapsulation efficiency and FA released from the microspheres were determined. The solid-state and phase separation properties of the microspheres were characterized using DSC, XRPD, Raman spectroscopy, SEM, laser confocal and real time recording of single microspheres formation.
RESULTS: Above a loading of 1% (w/w) FA phase separated from PLGA polymer and formed distinct spherical FA-rich amorphous microdomains throughout the PLGA microsphere. For FA-loaded PLGA microspheres, encapsulation efficiency and cumulative release increased with initial drug loading. Similarly, cumulative release from FA-loaded PHBV microspheres was increased by FA loading. After the initial burst release, FA was released from PLGA microspheres much slower compared to PHBV microspheres.
CONCLUSIONS: A unique phase separation phenomenon of FA in PLGA but not in PHBV polymers was observed, driven by coalescence of liquid microdroplets of a DCM-FA-rich phase in the forming microsphere.
Authors:
Chiming Yang; David Plackett; David Needham; Helen M Burt
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2009-04-21
Journal Detail:
Title:  Pharmaceutical research     Volume:  26     ISSN:  1573-904X     ISO Abbreviation:  Pharm. Res.     Publication Date:  2009 Jul 
Date Detail:
Created Date:  2009-06-02     Completed Date:  2009-08-17     Revised Date:  2010-12-03    
Medline Journal Info:
Nlm Unique ID:  8406521     Medline TA:  Pharm Res     Country:  United States    
Other Details:
Languages:  eng     Pagination:  1644-56     Citation Subset:  IM    
Affiliation:
Faculty of Pharmaceutical Sciences, The University of British Columbia, 2146 East Mall, Vancouver BCV6T1Z3, Canada.
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MeSH Terms
Descriptor/Qualifier:
Anti-Bacterial Agents / chemistry*
Calorimetry, Differential Scanning
Delayed-Action Preparations / chemistry*
Fusidic Acid / chemistry*
Glycolates / chemistry*
Kinetics
Microspheres*
Particle Size
Phase Transition
Polyesters / chemistry*
Powder Diffraction
Surface Properties
X-Ray Diffraction
Chemical
Reg. No./Substance:
0/Anti-Bacterial Agents; 0/Delayed-Action Preparations; 0/Glycolates; 0/Polyesters; 0/poly(3-hydroxybutyrate)-co-(3-hydroxyvalerate); 0/polylactic acid-polyglycolic acid copolymer; 6990-06-3/Fusidic Acid

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


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