A nanohybrid system for taste masking of sildenafil

Ji Hee Lee, Goeun Choi, Yeon Ji Oh, Je Won Park, Young Bin Choy, Mung Chul Park, Yeo Joon Yoon, Hwa Jeong Lee, Hee Chul Chang, Jin Ho Choy

Research output: Contribution to journalArticle

26 Scopus citations

Abstract

A nanohybrid was prepared with an inorganic clay material, montmorillonite (MMT), for taste masking of sildenafil (SDN). To further improve the taste-masking efficiency and enhance the drug-release rate, we coated the nanohybrid of SDN-MMT with a basic polymer, polyvinylacetal diethylaminoacetate (AEA). Powder X-ray diffraction and Fourier transform infrared experiments showed that SDN was successfully intercalated into the interlayer space of MMT. The AEA-coated SDN-MMT nanohybrid showed drug release was much suppressed at neutral pH (release rate, 4.70 ± 0.53%), suggesting a potential for drug taste masking at the buccal cavity. We also performed in vitro drug release experiments in a simulated gastric fluid (pH = 1.2) and compared the drug-release profiles of AEA-coated SDN-MMT and Viagra®, an approved dosage form of SDN. As a result, about 90% of SDN was released from the AEAcoated SDN-MMT during the first 2 hours while almost 100% of drug was released from Viagra®. However, an in vivo experiment showed that the AEA-coated SDN-MMT exhibited higher drug exposure than Viagra®. For the AEA-coated SDN-MMT, the area under the plasma concentration- time curve from 0 hours to infinity (AUC0-∞) and maximum concentration (Cmax) were 78.8 ± 2.32 μg · hour/mL and 12.4 ± 0.673 μg/mL, respectively, both of which were larger than those obtained with Viagra® (AUC0-∞ = 69.2 ± 3.19 μg · hour/mL; Cmax = 10.5 ± 0.641 μg/mL). Therefore, we concluded that the MMT-based nanohybrid is a promising delivery system for taste masking of SDN with possibly improved drug exposure.

Original languageEnglish
Pages (from-to)1635-1649
Number of pages15
JournalInternational Journal of Nanomedicine
Volume7
DOIs
StatePublished - 5 Dec 2012

Keywords

  • Montmorillonite
  • Nanohybrids
  • Polyvinylacetal diethylaminoacetate
  • Sildenafil citrate
  • Taste masking

Cite this

Lee, J. H., Choi, G., Oh, Y. J., Park, J. W., Choy, Y. B., Park, M. C., Yoon, Y. J., Lee, H. J., Chang, H. C., & Choy, J. H. (2012). A nanohybrid system for taste masking of sildenafil. International Journal of Nanomedicine, 7, 1635-1649. https://doi.org/10.2147/IJN.S28264