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A nanohybrid system for taste masking of sildenafil

Title
A nanohybrid system for taste masking of sildenafil
Authors
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.
Ewha Authors
이화정윤여준최진호
SCOPUS Author ID
이화정scopus; 윤여준scopus; 최진호scopus
Issue Date
2012
Journal Title
International Journal of Nanomedicine
ISSN
1176-9114JCR Link
Citation
vol. 7, pp. 1635 - 1649
Indexed
SCI; SCIE; SCOPUS WOS scopus
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. © 2012 Lee et al, publisher and licensee Dove Medical Press Ltd.
DOI
10.2147/IJN.S28264
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약학대학 > 약학과 > Journal papers
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