Characterization of nitric oxide-releasing microparticles for the mucosal delivery
Jin-Wook Yoo
Division of Pharmaceutical Sciences, School of Pharmacy, University of Missouri, Kansas City, Missouri 64110
Search for more papers by this authorJae-Suk Lee
Department of Materials Science and Engineering, Gwangju Institute of Science and Technology (GIST), 1 Oryong-dong, Buk-gu, Gwangju 500-712, Korea
Search for more papers by this authorCorresponding Author
Chi H. Lee
Division of Pharmaceutical Sciences, School of Pharmacy, University of Missouri, Kansas City, Missouri 64110
Division of Pharmaceutical Sciences, School of Pharmacy, University of Missouri, Kansas City, Missouri 64110Search for more papers by this authorJin-Wook Yoo
Division of Pharmaceutical Sciences, School of Pharmacy, University of Missouri, Kansas City, Missouri 64110
Search for more papers by this authorJae-Suk Lee
Department of Materials Science and Engineering, Gwangju Institute of Science and Technology (GIST), 1 Oryong-dong, Buk-gu, Gwangju 500-712, Korea
Search for more papers by this authorCorresponding Author
Chi H. Lee
Division of Pharmaceutical Sciences, School of Pharmacy, University of Missouri, Kansas City, Missouri 64110
Division of Pharmaceutical Sciences, School of Pharmacy, University of Missouri, Kansas City, Missouri 64110Search for more papers by this authorAbstract
For the treatment of female sexual arousal disorder (FSAD), we developed microparticles made of PLGA containing nitric oxide (NO) donor (DETA NONOate) to efficiently deliver NO to vaginal mucosa. The NO-releasing microparticles were prepared by various emulsion methods. SEM and DSC studies were performed to examine the microparticles. The release studies were conducted under various conditions to optimize the loading dose in the microparticles. NO diffusivity through vaginal epithelial cells was evaluated and pharmacological activity of NO-releasing microparticles was examined by assessment of intracellular cGMP level in vaginal cells. Through the modified double emulsion solvent evaporation method (w/o/wa), the acid labile DETA NONOate was stabilized during the fabrication process and homogenous morphology and high entrapment efficiency were achieved. DETA NONOate was protected under the acidic conditions of the vagina and NO was released from the microparticles in a controlled manner. A significant amount of NO produced from DETA NONOate penetrated through the vaginal epithelial cells. The intracellular cGMP level increased with the treatment of NO-releasing microparticles in vaginal cells. These findings suggest that NO-releasing microparticles could improve the vaginal blood perfusion and open up the possibilities of novel treatment of FSAD. © 2009 Wiley Periodicals, Inc. J Biomed Mater Res, 2010
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