title: Fabrication and evaluation of Phytomenadione as a nanostructure lipid carrier for enhancement of bioavailability.
abstract: Owing to its limited aqueous solubility, Phytomenadione (vitamin K) undergoes a low bioavailability (50%) with a large inter-individual variability after oral administration. Therefore, the aim of this work was to incorporate vitamin K into nanostructure lipid carrier systems to improve its aqueous solubility and bioavailability. Phytomenadione was used as a liquid lipid; Precirol ATO5, and Compritol ATO were used as solid lipids; Labrasol and Cremophore EL as water soluble surfactants; Capryol 90 and Lauroglycol as lipid soluble surfactants. Eight formulas were prepared and characterized for their particle sizes, zeta potential, entrapment efficiencies, and drug release. Those formulas had particle sizes ranging from 25.4 to 68.3 nm. The best formula, consisting of 15% Phytomenadione, 45% Precirol ATO5, 30% Cremophore EL, and 10% Lauroglycol 90, was selected for stability study and characterized by the techniques mentioned above and scanning electron microscopy. It had the highest drug loading and an acceptable in vitro release profile (94.54% within 30 min). This formula was also chemically and physically stable, and it recorded a relative bioavailability of 645.5% in rabbits compared to the commercial conventional tablet. This formula could be a promising carrier regarding its ease of preparation, dosage form versatility and enhanced bioavailability.
authors.affiliation: a Department of Pharmaceutics, Faculty of Pharmacy , King Abdulaziz University , Jeddah , Saudi Arabia.
authors.forename: Bader Mubarak
authors.initials: BM
authors.lastname: Aljaeid
authors.affiliation: a Department of Pharmaceutics, Faculty of Pharmacy , King Abdulaziz University , Jeddah , Saudi Arabia.|b Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy , Beni-Suef University , Beni-Suef , Egypt.
authors.forename: Khaled Mohamed
authors.initials: KM
authors.lastname: Hosny
mesh_terms: D000818:Animals; D000933:Antifibrinolytic Agents / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D001682:Biological Availability; D004337:Drug Carriers / Q000737:chemistry*; D065546:Drug Liberation; D008055:Lipids / Q000737:chemistry*; D053758:Nanoparticles / Q000737:chemistry*; D011817:Rabbits; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry; D013607:Tablets; D013816:Thermodynamics; D010837:Vitamin K 1 / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*; D014815:Vitamins / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*
chemical_list: D000933:Antifibrinolytic Agents; D004337:Drug Carriers; D008055:Lipids; D013501:Surface-Active Agents; D013607:Tablets; D014815:Vitamins; D010837:Vitamin K 1
keywords: Compritol; Phytomenadione; Precirol ATO5; bioavailability; nanostructure lipid carrier