Premium
Characterization of nitric oxide‐releasing microparticles for the mucosal delivery
Author(s) -
Yoo JinWook,
Lee JaeSuk,
Lee Chi H.
Publication year - 2009
Publication title -
journal of biomedical materials research part a
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.849
H-Index - 150
eISSN - 1552-4965
pISSN - 1549-3296
DOI - 10.1002/jbm.a.32434
Subject(s) - nitric oxide , microparticle , materials science , emulsion , intracellular , plga , drug delivery , biomedical engineering , biophysics , nanoparticle , nanotechnology , chemistry , chemical engineering , biochemistry , medicine , organic chemistry , biology , engineering
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/w a ), 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