title: A nanohybrid system for taste masking of sildenafil.
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 AEA-coated 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 (AUC(0-∞)) and maximum concentration (C(max)) 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(®) (AUC(0-∞) = 69.2 ± 3.19 μg · hour/mL; C(max) = 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.
authors.affiliation: Center for Intelligent Nano-Bio Materials (CINBM), Department of Bioinspired Science, Ewha Womans University, Seoul, Korea.
authors.forename: Ji-Hee
authors.initials: JH
authors.lastname: Lee
authors.forename: Goeun
authors.initials: G
authors.lastname: Choi
authors.forename: Yeon-Ji
authors.initials: YJ
authors.lastname: Oh
authors.forename: Je Won
authors.initials: JW
authors.lastname: Park
authors.forename: Young Bin
authors.initials: YB
authors.lastname: Choy
authors.forename: Mung Chul
authors.initials: MC
authors.lastname: Park
authors.forename: Yeo Joon
authors.initials: YJ
authors.lastname: Yoon
authors.forename: Hwa Jeong
authors.initials: HJ
authors.lastname: Lee
authors.forename: Hee Chul
authors.initials: HC
authors.lastname: Chang
authors.forename: Jin-Ho
authors.initials: JH
authors.lastname: Choy
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001546:Bentonite / Q000737:chemistry; D003692:Delayed-Action Preparations / Q000008:administration & dosage / Q000737:chemistry; D004285:Dogs; D004337:Drug Carriers / Q000737:chemistry; D004355:Drug Stability; D008297:Male; D058726:Nanoconjugates / Q000008:administration & dosage* / Q000737:chemistry; D050997:Nanomedicine; D010879:Piperazines / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics; D011145:Polyvinyls / Q000737:chemistry; D033362:Powder Diffraction; D011687:Purines / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics; D000068677:Sildenafil Citrate; D017550:Spectroscopy, Fourier Transform Infrared; D013450:Sulfones / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics; D013649:Taste
chemical_list: D003692:Delayed-Action Preparations; D004337:Drug Carriers; D058726:Nanoconjugates; D010879:Piperazines; D011145:Polyvinyls; D011687:Purines; D013450:Sulfones; C405622:polyvinylacetal diethylaminoacetate; D001546:Bentonite; D000068677:Sildenafil Citrate