Characterization and Systemic Delivery of Dibenzoylmethane via the Intranasal Route.

Intranasal (IN) administration is known to be noninvasive with the potential to carry a drug or vaccine directly to the blood, bypassing first-pass metabolism in the liver and the harsh environment of the gastrointestinal system. Orally administered dibenzoylmethane (DBM) has been shown experimentally to be neuroprotective in animal models of tauopathy and prion disease and effective in the treatment of certain forms of cancers. The purpose of this study was to prepare, characterize, and test formulations of DBM designed for IN administration.

Evaluation of triazole-chelated lanthanides as chemically stabile bioimaging agents.

Europium (Eu), dysprosium (Dy), samarium (Sm), and terbium (Tb) complexes were prepared using the neutral tridentate chelator 2,6-bis(1-benzyl-1,2,3-triazol-4-yl)pyridine and one equivalent of each lanthanide salt. The physicochemical, aerodynamic, and in vitro cellular properties of each lanthanide metal complex were studied to determine their viability as cell surface fluorescent probes. Each compound was characterized by electrospray ionization mass spectroscopy (ESI-MS), ultraperformance liquid chromatography (UPLC), differential scanning calorimetry (DSC), and thermogravimetic analysis (TGA).

Treatment options for refractory and difficult to treat seizures: focus on vigabatrin.

Complex partial seizures are often refractory to current pharmacological therapies. These difficult to treat seizures are typically managed using multiple antiepileptic drugs (AEDs). AEDs as a group are frequently associated with significant adverse drug effects, multiple drug interactions, and numerous potential clinical complications due to their individual pharmacokinetic profiles and unique drug properties.

Safety and efficacy of vigabatrin for the treatment of infantile spasms.

In 2009, vigabatrin became the first FDA approved medication for the treatment of infantile spasms in the United States. There are few well-designed prospective studies comparing the drug to placebo or other modalities used in the treatment of infantile spasms. The available data have demonstrated that vigabatrin is efficacious in the treatment of infantile spasms regardless of underlying etiology, but that it is particularly beneficial in patients with a diagnosis of tuberous sclerosis.

Vigabatrin: a comprehensive review of drug properties including clinical updates following recent FDA approval.

Background: Vigabatrin (Sabril) was approved in the USA in mid-2009 for the adjunctive treatment of refractory complex partial seizures and as treatment of infantile spasms. Vigabatrin's more than 30-year history of research and development is condensed into a clinically relevant review pertaining to this 2009 approval.

Methods/discussion: A review of the scientific literature was conducted with special focus given to the drug molecule, its mechanism of action, its effects on living systems (e.

Advances in the pulmonary delivery of poorly water-soluble drugs: influence of solubilization on pharmacokinetic properties.

Background: Pulmonary drug delivery is an accepted route of drug administration for the management of lung conditions and diseases as well as an evolving route of administration for the systemic delivery of agents. Many inhaled drugs pose formulation and delivery challenges in part because of poor aqueous solubility. The influence of poor aqueous solubility and formulation-based solubility enhancements on the pharmacokinetic profile of inhaled agents was reviewed.

Dose tolerability of chronically inhaled voriconazole solution in rodents.

Invasive pulmonary aspergillosis (IPA) is a fungal disease of the lung associated with high mortality rates in immunosuppressed patients despite treatment. Targeted drug delivery of aqueous voriconazole solutions has been shown in previous studies to produce high tissue and plasma drug concentrations as well as improved survival in a murine model of IPA. In the present study, rats were exposed to 20 min nebulizations of normal saline (control group) or aerosolized aqueous solutions of voriconazole at 15.

Characterization and pharmacokinetic analysis of aerosolized aqueous voriconazole solution.

Invasive fungal infections in immunocompromised patients have high mortality rates despite current treatment modalities. This study was designed to evaluate the suitability of an aqueous solution of voriconazole solubilized with sulfobutyl ether-beta-cyclodextrin for targeted drug delivery to the lungs via nebulization. A solution was prepared such that the inspired aerosol dose was isotonic with an acceptable mass median aerodynamic diameter of 2.

Inhaled voriconazole for prevention of invasive pulmonary aspergillosis.

Targeted airway delivery of antifungals as prophylaxis against invasive aspergillosis may lead to high lung drug concentrations while avoiding toxicities associated with systemically administered agents. We evaluated the effectiveness of aerosolizing the intravenous formulation of voriconazole as prophylaxis against invasive pulmonary aspergillosis caused by Aspergillus fumigatus in an established murine model. Inhaled voriconazole significantly improved survival and limited the extent of invasive disease, as assessed by histopathology, compared to control and amphotericin B treatments.