A nanohybrid system for taste masking of sildenafil

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 (R), an approved dosage form of SDN. As a result, about 90% of SDN was released from the AEA-coated SDN-MMT during the first 2 hours while almost 100% of drug was released from Viagra (R). However, an in vivo experiment showed that the AEA-coated SDN-MMT exhibited higher drug exposure than Viagra (R). For the AEA-coated SDN-MMT, the area under the plasma concentration-time curve from 0 hours to infinity (AUC(0-infinity)) and maximum concentration (C-max) were 78.8 +/- 2.32 mu g.hour/mL and 12.4 +/- 0.673 mu g/mL, respectively, both of which were larger than those obtained with Viagra (R) (AUC(0-infinity) = 69.2 +/- 3.19 mu g.hour/mL; C-max = 10.5 +/- 0.641 mu g/mL). Therefore, we concluded that the MMT-based nanohybrid is a promising delivery system for taste masking of SDN with possibly improved drug exposure.