title: A novel application of electrospinning technique in sublingual membrane: characterization, permeation and in vivo study.
abstract: Isosorbide dinitrate-polyvinylpyrrolidone (ISDN-PVP) electrospinning fibers were formulated and explored as potentially sublingual membrane. The addition of polyethylene glycol (PEG) to the formulation improved flexibility and reduced fluffiness of the fiber mat. The scanning electron microscopy (SEM) demonstrated that the fibers tended to be cross-linking, and the crosslinking degree increased with the increase of PEG amount. The differential scanning calorimetry (DSC) indicated that ISDN existed in non-crystalline state in the fibers (except at the highest drug content). The infrared spectroscopy suggested that ISDN had better compatibility with the ingredients owing to the hydrogen bonding (or hydrophobic interactions). The fibers were highly favorable for the fabrication of sublingual membrane due to neutral pH, large folding endurance and rapid drug release (complete dissolution within 120 s). The permeation study of ISDN through both dialysis membrane (DM) and porcine sublingual mucosa (SM) were carried out. A significant relationship of drug permeation rate through DM and SM was built up, which indicated that DM could be used to partly simulate SM and assess formulation. The pharmacokinetic study in rats demonstrated that the electrospinning fiber membrane had a higher Cmax and lower Tmax compared to the reference preparation, and the relative bioavailability of the fiber membrane was 151.6%.
authors.affiliation: a School of Pharmacy, Shenyang Pharmaceutical University , Shenyang , China ;
authors.forename: Jianting
authors.initials: J
authors.lastname: Chen
authors.affiliation: a School of Pharmacy, Shenyang Pharmaceutical University , Shenyang , China ;
authors.forename: Xiaoyu
authors.initials: X
authors.lastname: Wang
authors.affiliation: b Department of Forensic Medicine, National Police University , Shenyang , China.
authors.forename: Wenji
authors.initials: W
authors.lastname: Zhang
authors.affiliation: a School of Pharmacy, Shenyang Pharmaceutical University , Shenyang , China ;
authors.forename: Shihui
authors.initials: S
authors.lastname: Yu
authors.affiliation: a School of Pharmacy, Shenyang Pharmaceutical University , Shenyang , China ;
authors.forename: Jinwu
authors.initials: J
authors.lastname: Fan
authors.affiliation: a School of Pharmacy, Shenyang Pharmaceutical University , Shenyang , China ;
authors.forename: Bingchao
authors.initials: B
authors.lastname: Cheng
authors.affiliation: a School of Pharmacy, Shenyang Pharmaceutical University , Shenyang , China ;
authors.forename: Xinggang
authors.initials: X
authors.lastname: Yang
authors.affiliation: a School of Pharmacy, Shenyang Pharmaceutical University , Shenyang , China ;
authors.forename: Weisan
authors.initials: W
authors.lastname: Pan
mesh_terms: D000286:Administration, Sublingual; D000818:Animals; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical / Q000379:methods; D065546:Drug Liberation / Q000502:physiology; D006860:Hydrogen Bonding; D006863:Hydrogen-Ion Concentration; D057927:Hydrophobic and Hydrophilic Interactions; D007548:Isosorbide Dinitrate / Q000737:chemistry* / Q000378:metabolism*; D008297:Male; D009060:Mouth Floor / Q000378:metabolism*; D010539:Permeability; D011092:Polyethylene Glycols / Q000737:chemistry; D011205:Povidone / Q000737:chemistry* / Q000378:metabolism*; D051381:Rats; D017208:Rats, Wistar; D013552:Swine; D013678:Technology, Pharmaceutical / Q000379:methods*
chemical_list: D011092:Polyethylene Glycols; D011205:Povidone; D007548:Isosorbide Dinitrate
keywords: Bioavailability; electrospinning; isosorbide dinitrate; permeation; sublingual membrane