Journal
JOURNAL OF PHARMACEUTICAL SCIENCES
Volume 99, Issue 8, Pages 3389-3397Publisher
ELSEVIER SCIENCE INC
DOI: 10.1002/jps.22106
Keywords
adriamycin; star-shaped poly lactide-co-glycolide; 3-cyclodextrin, micro- and nanoparticles
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The star-shaped poly(lactide-co-glycolide (PLGA)-beta-cyclodextrin (PLGA-beta-CD) copolymer was synthesized by reacting L-lactide, glycolide, and beta-cyclodextrin in the presence of stannous octoate as a catalyst. The structure of PLGA-beta-CD copolymer was confirmed with H-1-NMR, C-13-NMR, and FT-IR spectra Adriamycin (ADR), which is an antitumor antibiotic, was encapsulated within micro- and nanoparticles made of PLGA-beta-CD with a modified double emulsion method. Relatively low amount of beta-CD and catalyst were used in order to obtain high molecular weight polymers. Differential scanning calorimetry (DSC) was used to determine the thermal properties of star-shaped copolymers. The reduction of interactions between the star-shaped polyester molecules is due to their branched structure lowered 7', and T, compared to linear PLGA copolymers. Effects of the experimental parameters, such as copolymer composition, ADR concentration, copolymer concentration, and poly(vinyl alcohol) concentration, on particular size and encapsulation efficiency were investigated. An increase in the internal aqueous phase volume led to a decrease in particles average size. A decrease in the polymer concentration resulted in increasing the particle average size from 135.5 to 325.6 nm The high entrapment efficiency (EE) (about 65%) was obtained for 220 mu m particles. All of the release profiles indicated a close relationship between each formulation variable and the amount of ADR released. (C) 2010 Wiley-Liss, Inc and the American Pharmacists Association J Pharm Sci 99 3389-3397, 2010
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