Journal
INTERNATIONAL JOURNAL OF PHARMACEUTICS
Volume 397, Issue 1-2, Pages 194-200Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijpharm.2010.06.049
Keywords
Letrozole; Technetium-99m; PLGA nanoparticles; Biodistribution; Tumor uptake
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Funding
- Council of Scientific and Industrial Research, New Delhi
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Letrozole (LTZ) incorporated PLGA nanoparticles were prepared by solvent displacement technique and characterized by transmission electron microscopy, poly-dispersity index and zeta potential measurement. Radiolabeling of free LTZ and LTZ-loaded PLGA NPs was performed with technetium-99m with high labeling efficiency. The labeled complex showed good in vitro stability as verified by DTPA challenge test. The labeled complexes also showed significant in vivo stability when incubated in rat serum for 24h. Biodistribution studies of Tc-99m-labeled complexes were performed after intravenous administration in normal mice and Ehrlich Ascites tumor bearing mice. Compared to free LTZ, LTZ-loaded PLGA NPs exhibited significantly lower uptake by the organs of RES. The tumor concentration of LTZ-loaded PLGA NPs was 4.65 times higher than that of free LTZ at 4h post-injection. This study indicates the capability of PLGA nanopartcles in enhancing the tumor uptake of letrozole. (C) 2010 Elsevier B.V. All rights reserved.
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