title: Bioenhanced sublingual tablet of drug with limited permeability using novel surfactant binder and microencapsulated polysorbate: In vitro/in vivo evaluation.
abstract: Formulation of sublingual tablets of drugs with limited permeability poses a great challenge due to their poor absorption. In this study, bioenhanced sublingual tablets (BESTs) of zolmitriptan were prepared using novel surfactant binder (Pluronic® p123/Syloid® mixture) to enhance tablet disintegration and dissolution. Microencapsulated polysorbate 80 (Sepitrap™ 80) were included in the composition of BESTs to enhance the drug transport through the sublingual mucosa. Tablets were evaluated for in vitro/in vivo disintegration, in vitro dissolution and ex vivo permeation. Solubility studies confirmed that phosphate buffer; pH 6.8 could be used as dissolution medium for sublingual tablets of zolmitriptan. BEST-5 containing Pluronic® p123/Syloid® mixture and Sepitrap™ 80 exhibited the shortest in vitro/in vivo disintegration times (<30s), the highest dissolution at early time dissolution points and the highest enhancement of drug transport through mucosal membrane. The in vivo pharmacokinetic study using human volunteers showed a significant increase in the rate and extent of sublingual absorption with less variations of Tmax after sublingual administration of both BEST-5 and Zomig-ZMT ODT. Our results proposed that Pluronic® p123/Syloid® mixture and Sepitrap™ 80 could be promising for the development of sublingual tablets for rapid onset of action of drugs with limited permeability.
authors.affiliation: Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Kasr El-aini Street, Cairo 11562, Egypt.
authors.forename: Doaa Ahmed
authors.initials: DA
authors.lastname: El-Setouhy
authors.affiliation: Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Kasr El-aini Street, Cairo 11562, Egypt. Electronic address: dremadbasalious@cu.edu.eg.
authors.forename: Emad B
authors.initials: EB
authors.lastname: Basalious
authors.affiliation: Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Kasr El-aini Street, Cairo 11562, Egypt.
authors.forename: Nevine Shawky
authors.initials: NS
authors.lastname: Abdelmalak
mesh_terms: D000286:Administration, Sublingual; D000818:Animals; D019540:Area Under Curve; D002645:Chickens; D004339:Drug Compounding; D005079:Excipients / Q000737:chemistry*; D064368:Healthy Volunteers; D006801:Humans; D065568:Oral Mucosal Absorption; D023303:Oxazolidinones / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D010539:Permeability; D011060:Poloxalene / Q000737:chemistry*; D011136:Polysorbates / Q000737:chemistry*; D012822:Silicon Dioxide / Q000737:chemistry*; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry*; D013607:Tablets; D014018:Tissue Distribution; D014363:Tryptamines / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics
chemical_list: D005079:Excipients; D023303:Oxazolidinones; D011136:Polysorbates; D013501:Surface-Active Agents; D013607:Tablets; D014363:Tryptamines; C464484:pluronic block copolymer P123; C089750:zolmitriptan; D012822:Silicon Dioxide; D011060:Poloxalene
keywords: Bioenhancer; Limited permeability; Microencapsulated solubilizer; Pluronic® p123/Syloid® mixture; Sublingual; Surfactant binder